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Dictionary of drugs: L

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Dictionary of drugs L

An immunoconjugate consisting of the recombinant form of the cytokine interleukin-2 (IL-2) fused to a human single-chain Fv (scFv) antibody fragment directed against the extra-domain B (ED-B) of fibronectin (L19), with potential immunopotentiating and antineoplastic activities. The L19 moiety of L19-IL2 monoclonal antibody-cytokine fusion protein binds to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. In turn, the IL-2 moiety may locally activate natural killer (NK) cells and macrophages, and may induce T cell cytotoxic immune responses against ED-B fibronectin-expressing tumor cells. This may specifically decrease the proliferation of ED-B-expressing tumor cells. ED-B is predominantly expressed during angiogenesis and tumor growth.

A prodrug in which a peptide is covalently conjugated with the anthracycline antineoplastic antibiotic doxorubicin. This complex is hydrolyzed by the enzyme prostate-specific antigen (PSA), resulting in the formation of doxorubicin and leucine-doxorubicin. Selective targeting of these drugs to prostate tumor cells occurs because the hydrolyzing PSA enzyme is localized to the prostate gland. Doxorubicin and leucine-doxorubicin intercalate into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. These agents also produce toxic free-radical intermediates and interact with cell membrane lipids causing lipid peroxidation.

An antibody-drug conjugate (ADC) containing labetuzumab, a mildly reduced, anti-CEACAM5 humanized monoclonal antibody, conjugated to the potent topoisomerase I inhibitor SN-38, with antineoplastic activity. The monoclonal antibody moiety of antibody-drug conjugate IMMU-130 selectively binds to carcinoembryonic cell adhesion molecule 5 (CEACAM5), which is abundantly expressed on the surface of a majority of solid tumors. Upon internalization and proteolytic cleavage, SN-38, the active metabolite of irinotecan, inhibits the activity of topoisomerase I in the tumor cells, eventually inhibiting both DNA replication and transcription and leading to tumor cell apoptosis.

Brand name for theophylline

A functionalized amino acid compound specifically synthesized as an anticonvulsive drug to use as add-on therapy for partial-onset seizures with antinociceptive and neuroprotective activities. Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels without affecting fast inactivation, thereby stabilizing hyperexcitabe neuronal membranes. Furthermore, this agent binds to collapsin response mediator protein 2 (CRMP2; DPYSL2), a cytosolic phosphoprotein expressed in most tissues. In the nervous system, CRMP2 acts as a mediator of growth cone collapse and modifies axon number, length, and neuronal polarity.

A vaginal tablet containing a low dose of the estrogen hormone estriol and lyophilized lactobacillus acidophilus, with hormone replacement and vaginal flora restoring activity. Upon vaginal application, estriol may restore estrogen levels locally and may relieve symptoms caused by estrogen deficiency; the Lactobacillus acidophilus may be able to restore the vaginal Lactobacillus flora.

A nutritional supplement containing probiotic cultures of Lactobacillus acidophilus (L. acidophilus), L. rhamnosus Streptococcus thermophilus, Bifidobacterium lactis, (B. lactis), B. longum and B. bifidum, with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function.

A lozenge containing an extract from the Lactobacillus brevis (L. brevis) with potential anti-inflammatory activity. As L. brevis CD2 contains high levels of arginine deiminase, which catalyzes the conversion of arginine to citrulline and ammonia, administration of this lozenge leads to hydrolysis of arginine in the oral cavity. The growth of bacteria, which depends on arginine, is halted, polyamine biosynthesis is reduced and the production of nitric oxide (NO) is reduced. The reduction in NO generation may further prevent inflammation in the oral cavity. Therefore, this agent may be able to reduce chemo- and radiotherapy-induced mucositis.

A proprietary dietary supplement. Lactobacillus fermented extract is made from soymilk fermented by several strains of lactobacillus and yeast via a symbiotic co-culturing technology. The composition of the agent includes amino acids, vitamins, minerals, fatty acids, isoflavones, and saponins. Lactobacillus fermented extract may support healthy intestinal function.

A powder-based, probiotic supplement drink containing the non-pathogenic microorganisms Lactobacillus plantarum 299v, Lactobacillus acidophilus, and Bifidobacterium lactis, with potential immunomodulating and protective activities. Upon oral ingestion, the naturally-occurring bacterial components in this dietary supplement may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization in the GI tract, the bacteria may form a protective intestinal barrier which may prevent damage to the mucosal epithelia caused by toxins and attachment of potential pathogens, thereby protecting against infections. In addition, this agent may reduce the secretion of proinflammatory cytokines and may potentiate natural and acquired immunity.

A nutritional supplement containing the probiotic bacterium Lactobacillus plantarum 299 (Lp 299) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, Lp 299 adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299 stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.

A nutritional supplement containing a strain of the probiotic bacterium Lactobacillus plantarum 299v (Lp 299v) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, L. plantarum strain 299v adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299v stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.

A tablet containing a strain of the probiotic Gram-positive, naturally-occurring bacterium Lactobacillus reuteri (L. reuteri), with potential antimicrobial, immunomodulatory and protective activities. Upon oral administration of the L. reuteri probiotic tablet, the Lactobacillus strain may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization of the GI tract, this bacterium adheres to human intestinal epithelial cells, and activates intestinal epithelial proliferation; both of these processes promote the formation and maintenance of a protective barrier, thereby preventing the attachment of harmful pathogens. L. reuteri produces lactic acid and other substances during fermentation, and creates an acidic environment that is unfavorable for pathogens, thereby further protecting the intestinal mucosa against pathogen-induced damage and loss of integrity of the intestinal mucosal barrier. Dietary supplementation with this bacterium has been shown to decrease intestinal inflammation and enhance innate and acquired immunity. Lactobacillus reuteri is naturally found in the GI tract.

A live specific strain of the species, Lactobacillus rhamnosus (a subspecies of Lactobacillus casei) with probiotic activity. When administered orally, Lactobacillus rhamnosus GG adheres to the mucous membrane of the intestine and may help to restore the balance of the GI microflora; promote gut-barrier functions; diminish the production of carcinogenic compounds by other intestinal bacteria; and activate the innate immune response and enhance adaptive immunity, especially during infections.

A water-based multi-strain probiotic composed of an extract of germinated barley containing the four live, activated lactic acid bacteria strains Lactobacillus rhamnosus, L. acidophilus, L. plantarum, and Enterococcus faecium, with potential immunomodulatory and anti-inflammatory activities. Upon oral administration of Lactobacillus rhamnosus/L. acidophilus/L. plantarum/Enterococcus faecium aqueous probiotic supplement, these four live bacteria modulate the composition of the normal gastrointestinal (GI) microflora, by increasing the beneficial bacteria and decreasing the harmful bacteria, and helps maintain adequate colonization of the GI tract, thereby improving digestion and preventing GI disturbances. These bacteria and the butyric acid produced by them create an environment unfavorable to pathogens by adhering to human epithelial cells, protecting epithelium by maintaining the tight junction integrity and forming a protective mucosal barrier. This prevents attachment of pathogens and reduces the risk of infection, and potentially reduces the severity of mucositis. By restoring gut microbiota, these bacteria may restore or enhance intestinal immune responses.

A nutritional supplement containing the probiotic Lactobacillus strains L. rhamnosus, L. jensenii, L. crispatus and L. gasseri with protective and immunomodulating activities. The bacteria in this probiotic supplement colonize the vaginal tract and help to maintain as well as restore the composition of the normal, healthy vaginal flora. The four Lactobacillus species form a protective barrier that helps both to maintain the integrity of the vaginal tract and prevent the attachment of pathogenic bacteria and other harmful substances, thereby protecting against genitourinary infections.

A probiotic supplement containing the bacteria Lactobacillus (L.) rhamnosus and L. reuteri, with potential restorative and protective activities. Upon oral administration of the L. rhamnosus and L. reuteri probiotic supplement, the bacteria may restore and provide balance to the microbiota in the breast tissue. This may reduce or prevent inflammation, and may protect against the invasion of harmful bacteria and infection in the breast. In addition, the bacteria may restore the natural balance of the vaginal flora. This may prevent the invasion of harmful bacteria and yeast, and may prevent bacterial and yeast infections. This supplement may also relieve symptoms such as vaginal itching, odor and discharge, and may improve vaginal discomfort.

A capsule containing a strain of the probiotic bacterium Lactobacillus with potential antimicrobial and immunomodulatory activities. As a dietary supplement, Lactobacillus, a naturally-occurring bacterium, may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. Because it produces lactic acid and hydrogen peroxide and other substances during fermentation, this bacterium creates an acidic environment that is unfavorable for pathogens. In addition, during colonization of the GI tract, this bacterium adheres to human epithelial cells and forms a protective barrier, thereby preventing the attachment of pathogens. Dietary supplementation with this bacterium has been shown to enhance innate and acquired immunity.

A peptide derived from human lactoferrin, with potential lytic and immunostimulating activities. Upon transdermal injection directly into the tumor, LTX315 may bind to the tumor cell membranes and subsequently lyse tumor cells, thereby inducing tumor cell necrosis. In turn, presentation of the tumor antigens to the immune system may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells. This may trigger an immune response against tumor associated antigens on tumors distant from the primary tumor. Human lactoferrin, a 692 amino acid glycoprotein, belongs to the transferrin family of metal-binding proteins.

Originally, the name laetrile was the contraction of laevo-mandelonitrile glucoside, a cyanogenic glycoside found naturally in some plants. Over the years the meaning of laetrile has changed. There are now preparations called Laetrile where amygdalin is the major constituent. Laetrile and amygdalin are often used interchangeably, but are different agents. Cyanide and benzaldehyde are metabolites of both laetrile and amygdalin. Both metabolites may possess antineoplastic properties. Laetrile has been used as an anticancer treatment in humans worldwide, but scientific evidence does not support its effectiveness. It is not approved for use in the United States.

An amino acid analogue and antibiotic derived from the bacterium Streptomyces alanosinicus with antimetabolite and potential antineoplastic activities. L-alanosine inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate, an intermediate in purine metabolism. L-alanosine-induced disruption of de novo purine biosynthesis is potentiated by methylthioadenosine phosphorylase (MTAP) deficiency. The clinical use of this agent may be limited by its toxicity profile. MTAP is a key enzyme in the adenine and methionine salvage pathways.

A suspension-based oral spray containing multilamellar lipid vesicles in which the lipids mimic the lipidic composition of endogenous extra-alveolar lamellar bodies, with muco-restorative and protective activity against radiotherapy (RT)-induced xerostomia (RIX). Upon sublingual administration of the lamellar body mimetic LMS-611 using a spray, the lipids in this agent mimic the natural secretions of endogenous lamellar bodies. This makes mucus more fluid and may prevent dryness of the mouth. This restores saliva functions and makes it easier to chew, swallow and talk, and also prevents xerostomia-induced infections, tooth decay and tooth enamel decay. RT decreases saliva secretion by causing the destruction of the parotid and submandibular serous salivary glands and lamellar bodies. This results in thicker and more visco-adhesive saliva, which causes various xerostomia-induced symptoms; intact lamellar bodies maintain the fluidity of mucus and lubricate the mouth.

Brand name for lamotrigine

A synthetic nucleoside analogue with activity against hepatitis B virus (HBV) and HIV. Intracellularly, lamivudine is phosphorylated to its active metabolites, lamiduvine triphosphate (L-TP) and lamiduvine monophosphate (L-MP). In HIV, L-TP inhibits HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleoside analogue into viral DNA. In HBV, incorporation of L-MP into viral DNA by HBV polymerase results in DNA chain termination. L-TP is a weak inhibitor of mammalian DNA polymerases alpha and beta, and mitochondrial DNA polymerase.

A synthetic phenyltriazine with antiepileptic and analgesic properties. Lamotrigine enhances the action of gamma-aminobutyric acid, an inhibitory neurotransmitter, which may result in a reduction of pain-related transmission of signals along nerve fibers. This agent may also inhibit voltage-gated sodium channels, suppress glutamate release, and inhibit serotonin reuptake.

Brand name for digoxin

The acetate salt of a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide binds to somatostatin receptors (SSTR), specifically SSTR-2 and also to SSTR-5 with a lesser affinity. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland. Furthermore, lanreotide has an acute effect on decreasing circulating total and free insulin-like growth factor 1 (IGF-I). This agent is usually given as a prolonged-release microparticle or Autogel formulation for the treatment of acromegaly and to relieve the symptoms of neuroendocrine tumors.

A prolonged-release depot suspension of microparticles containing the acetate salt of lanreotide, a synthetic peptide analog of the naturally occurring somatostatin, and copolymers. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent has a much longer duration of action than natural somatostatin and is selective towards the inhibition of growth hormone.

Brand name for lanreotide long-acting aqueous gel

A long-acting aqueous gel preparation of lanreotide, a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the release of various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent also decreases circulating total and free insulin-like growth factor 1 (IGF-I). Lanreotide exhibits a high binding affinity for somatostatin receptor 2 (SSTR-2) and a lesser binding affinity for SSTR-5. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland.

The ditosylate salt of lapatinib, a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.

A chemotherapy regimen consisting of lapatinib and letrozole that is used as a treatment for advanced hormone receptor (HR) positive, HER-2/neu-positive breast cancer.

A cell-based vaccine targets tumors expressing the HER2/neu marker. HER-2/neu is a growth factor receptor, and its overexpression has been associated with a number of cancers including breast, ovarian, colon and lung cancers. APC8024 comprise of autologous antigen-presenting peripheral blood mononuclear cells (APCs) that have been exposed to HER2/neu protein and can be administered to the patient. These cells may stimulate an antitumor T-cell response to cancer cells expressing HER2/neu.

Brand name for levodopa

A proprietary tablet formulation containing an extract from Largetrifoliolious Bugbane rhizome (Shengma), the dried root of Cimicifuga sp., with potential use for relieving menopausal symptoms. The Largetrifoliolious bugbane rhizome supplement contains total saponins, including phytoestrogens that can modulate estrogen receptor signaling. This supplement is used to reduce disease symptoms, such as sweating, toothache, headache, ulcers, and insomnia. In women, this supplement may be used to reduce symptoms related to menopause.

An amino acid and herbal supplement with libido-enhancing activity. L-arginine/korean ginseng/Ginkgo biloba/damiana-based supplement contains a blend of the amino acid L-arginine and the herbs Korean ginseng, Ginkgo biloba, and damiana (Turnera aphrodisiaca) in addition to 14 other vitamins and minerals. The semi-essential amino acid L-arginine is a precursor for nitric oxide (NO); Korean ginseng may enhance the conversion of L-arginine into NO by NO synthase; and Ginkgo biloba may promote microvascular circulation. This agent may increase NO production, resulting in vasodilatation and an enhanced circulation critical to sexual function and arousal. The damiana component may exert an anxiolytic effect and stimulate sexual behavior.

Brand name for levodopa

A sulfonyl hydrazine prodrug with antineoplastic activity. Laromustine releases the DNA chloroethylating agent 90CE after entering the blood stream; 90CE chloroethylates alkylates the 06 position of guanine, resulting in DNA crosslinking, strand breaks, chromosomal aberrations, and disruption of DNA synthesis. Intracellular metabolism of this agent also releases methyl isocyanate which inhibits 06-alkyl-guanine transferase, an enzyme involved with DNA repair.

A semi-synthetic derivative of the taxane 10-deacetylbaccatin III with potential antineoplastic activities. Larotaxel binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. Larotaxel penetrates the blood brain barrier.

An orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.

Brand name for olaratumab

Brand name for furosemide

Brand name for asparaginase

Brand name for hydromorphone hydrochloride

Brand name for fentanyl citrate pectin-based nasal spray

An orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in specific cancer cells harboring certain EGFR mutations. Compared to some other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors with T790M- or L858R-mediated drug resistance. In addition, lazertinib penetrates the blood-brain barrier (BBB). This agent shows minimal activity against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities, which occur during the use of non-selective EGFR inhibitors and inhibit wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

Brand name for L-carnitine L-tartrate

A dietary supplement containing the levo-enantiomers of carnitine and tartrate with potential chemoprotective and antioxidant activities. L-carnitine L-tartrate increases fatty acid oxidation and reduces purine catabolism and free radical formation, which may prevent exercise fatigue, muscle weakness, chemotherapy-induced peripheral neuropathy, and hyperlipoproteinemia. L-carnitine, the biologically active form of carnitine, is a carrier molecule that transports activated long-chain fatty acids (LCFAs)from the cytosol to mitochondria where fatty acids are oxidized, resulting in ATP production,. L-tartrate, a salt of tartaric acid, is a potent antioxidant.

A non-essential amino acid. In hepatocytes, L-citrulline is synthesized in the urea cycle by the addition of carbon dioxide and ammonia to ornithine. L-citrulline is converted into L-arginine by the enzymes argininosuccinate synthetase and argininosuccinate lyase in the presence of L-aspartate and ATP. Subsequently, L-arginine is converted to nitric oxide by nitric oxide synthase and L-citrulline is regenerated as a by-product .

A radioimmunoconjugate containing the recombinant humanized monoclonal antibody trastuzumab conjugated with the bifunctional chelating agent TCMC ((1,4,7,10-Tetra-(2-Carbamoyl Methyl)-Cyclododecane), and radiolabeled with the alpha-emitting isotope lead Pb 212, with potential anti-tumor activity. Upon administration, the antibody moiety of lead Pb 212 TCMC-trastuzumab binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2); after internalization, the radioisotope moiety delivers a cytotoxic dose of alpha radiation to the HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed on the cell surface of a variety of cancer cell types.

An orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Upon oral administration and after intracellular uptake, ledipasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of hepatocellular carcinoma (HCC).

A tablet containing a fixed dose combination of ledipasvir, an inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, and the prodrug sofosbuvir, an inhibitor of HCV NS5B polymerase, with activity against HCV. Upon oral administration of ledipasvir/sofosbuvir and intracellular uptake, ledipasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. Sofosbuvir is converted to its active triphosphate form, and competes with uridine triphosphate for incorporation into RNA, thereby inhibiting NS5B polymerase and preventing viral replication. This may eradicate HCV and prevent HCV-mediated tumorigenesis. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. The HCV NS5B protein, an RNA-dependent RNA polymerase, is essential for the replication of the viral HCV RNA genome. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of certain tumors.

A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation.

A thalidomide analog with potential antineoplastic activity. Lenalidomide inhibits TNF-alpha production, stimulates T cells, reduces serum levels of the cytokines vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), and inhibits angiogenesis. This agent also promotes G1 cell cycle arrest and apoptosis of malignant cells.

A broad-spectrum, carbapenem antibiotic with bactericidal activity. Lenapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. This inhibition weakens the bacterial cell wall and leads to lytic cell death in a wide range of Gram-positive and Gram-negative aerobic and anaerobic pathogens.

A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.

Autologous CD34+ hematopoietic stem cells transduced with Lenti-D lentiviral vector encoding the human ATP-binding cassette, sub-family D, member 1 (ABCD1) cDNA, for the potential treatment of childhood cerebral adrenoleukodystrophy (CCALD). Upon administration of the lenti-D/ABCD1-transduced autologous hematopoietic stem cells, the cells proliferate, and some travel to the brain and differentiate into microglial cells. The expressed ABCD1 restores the function of ALD protein (ALDP) and aids in the treatment of CCALD. In CCALD, the ABCD1 gene is mutated, leading to the inability of patients to metabolize very long chain fatty acids in cells of the brain.

Brand name for autologous beta-A(T87Q)-globin gene-transduced CD34-positive cells

Autologous, CD34-positive hematopoietic progenitor cells (HPCs) transduced with a lentiviral vector encoding three anti-human immunodeficiency virus (HIV) genes: a short hairpin RNA (shRNA) that targets human chemokine receptor 5 (CCR5), a human/rhesus macaque chimeric tripartite motif-containing protein 5 alpha isoform (TRIM5alpha), and a TAT activation response (TAR) decoy, as well as a pre-selective cell-surface marker, which is a truncated and mutated form of human CD25, used to potentially provide resistance against human immunodeficiency virus (HIV) infection. Human autologous CD34-positive HPCs are isolated and transduced ex vivo with the lentiviral vector. Upon pre-selection, purification using CD25 immunomagnetic separation, and subsequent administration of effectively transduced HPCs, the HPCs display 3 separate mechanisms of action against HIV infection: CCR5 shRNA binds to CCR5 mRNA and inhibits the expression of CCR5, a HIV-1 co-receptor that mediates HIV attachment and host cell entry; TRIM5alpha prevents HIV genome integration upon cell entry; and the TAR decoy binds to the HIV TAT protein and prevents TAT-dependent viral gene transcription, thereby preventing HIV replication. Upon transfer of the lentivirus vector CCR5 shRNA/TRIM5alpha/TAR decoy-transduced autologous CD34-positive HPCs into the patient, the HPCs are resistant to HIV entry and replication and could provide long-term protection against both HIV infection and HIV-associated cancers.

Autologous, CD34-positive hematopoietic progenitor cells (HPCs) transduced with rHIV7-shI-TAR-CCR5RZ, a lentiviral vector encoding three anti-human immunodeficiency virus (HIV) RNA genes, with potential antineoplastic activity. The 3 RNA products produced by the lentivirus are: a short hairpin RNA (shRNA) targeted to an exon of the HIV-1 genes tat/rev, designated as shI; a decoy for the HIV TAT reactive element, designated as TAR; a ribozyme targeting the host cells CCR5 chemokine receptor, designated as CCR5RZ. Upon administration, lentivirus vector rHIV7-shI-TAR-CCR5RZ-transduced hematopoietic progenitor cells expressing the 3 species of RNAs display 3 seperate mechanims of action: the shRNA blocks the transcription of tat/rev, the TAR decoy binds to the TAT protein that is essential for HIV replication, and CCR5RZ catalyzes CCR5 which is needed for viral attachment and entry into the host cells. Altogether, infusion of these HPCs may ultimately inhibit HIV replication and suppress HIV infection.

A synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. Lenvatinib mesylate blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis.

Brand name for lenvatinib mesylate

A recombinant monoclonal antibody against the cytokine granulocyte macrophage colony-stimulating factor (GM-CSF), with potential immunomodulating activity. Upon administration, lenzilumab binds to and neutralizes GM-CSF. This prevents GM-CSF binding to the GM-CSF receptor, which is a heterodimeric protein expressed on myeloid progenitor cells, and prevents GM-CSF-mediated signaling. This may induce apoptosis in and inhibit proliferation of cancer cells that overproduce GM-CSF. GM-CSF plays a key role in the differentiation and proliferation of monocytes, macrophages and granulocytes; elevated levels of GM-CSF are associated with certain autoimmune diseases, inflammatory diseases, and cancers.

Brand name for liposomal paclitaxel

A yeast cell-derived recombinant polypeptide related to the naturally occurring, leech-derived anticoagulant hirudin. Lepirudin directly binds to and inactivates thrombin, producing dose-dependent increases in the activated partial thromboplastin time (aPTT) and prothrombin time (PT). The mechanism of action of this agent is independent of antithrombin III and is not inhibited by platelet factor 4. Natural hirudin, a family of highly homologous isopolypeptides, is produced in trace amounts by the leech Hirudo medicinalis.

A recombinant chimeric dual G-CSF and IL-3 receptor agonist. Leridistim binds with high affinity to both the interleukin-3 (IL-3) and granulocyte colony-stimulating factor (G-CSF) receptors, thereby stimulating the production and maturation of neutrophils, platelets, and lymphocytes after chemotherapy.

The hydrochloride salt of a 2-piperazinylbenzimidazole-derivative serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting.

Brand name for fluvastatin sodium

Brand name for ethinyl estradiol/levonorgestrel

An orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3.

An orally bioavailable, non-nucleoside, 3,4-dihydroquinazolinyl acetic acid and inhibitor of the pUL56 subunit of the viral terminase complex of cytomegalovirus (CMV), with potential CMV-specific antiviral activity. Upon oral administration, letermovir binds to the pUL56 subunit of the viral terminase complex of CMV and prevents the cleavage of concatemeric DNA into monomeric genome length DNA. As this agent interferes with viral DNA processing and subsequent viral DNA packaging into procapsids, CMV replication is blocked and CMV infection is prevented.

A nonsteroidal inhibitor of estrogen synthesis with antineoplastic activity. As a third-generation aromatase inhibitor, letrozole selectively and reversibly inhibits aromatase, which may result in growth inhibition of estrogen-dependent breast cancer cells. Aromatase, a cytochrome P-450 enzyme localized to the endoplasmic reticulum of the cell and found in many tissues including those of the premenopausal ovary, liver, and breast, catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis.

A chemotherapy regimen consisting of letrozole and palbociclib that is used as a treatment for estrogen receptor (ER) positive and HER-2/neu-negative metastatic or advanced breast cancer. (NCI Thesaurus]]

An orally bioavailable leucine enriched essential amino acid dietary supplement with potential anti-cachexia activity. Leucine-enhanced essential amino acid nutritional supplement may stimulate the mammalian target of rapamycin (mTOR) signaling pathway, which may promote protein synthesis in muscle cells. Although the exact mechanism by which leucine and other essential amino acids stimulate mTOR has yet to be fully elucidated, leucine may stimulate mTOR by inhibiting adenosine monophosphate protein kinase (AMPK), which negatively controls mTOR signaling.

An active metabolite of folic acid (also called folinic acid and citrovorum factor), which does not require metabolism by dihydrofolate reductase, the molecular target of folate antagonist-type chemotherapeutic drugs. Leucovorin calcium counteracts the toxic effects of these medications, 'rescuing' the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity.

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with corpses of apoptotic leukemic cells, with potential immunostimulatory and antineoplastic activities. Upon vaccination, autologous dendritic cells pulsed with leukemic apoptotic corpse may activate the immune system to mount an anti-tumoral cytotoxic T-lymphocyte (CTL) response against leukemic cells expressing leukemia-associated antigens, which may result in leukemic cell lysis and inhibition of tumor cell growth. Apoptotic tumor cell corpses contain an array of tumor associated antigens (TAAs).

Brand name for chlorambucil

Brand name for sargramostim

The acetate salt of a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. This agent reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.

Brand name for IL-2 plasmid DNA/lipid complex

The orally bioavailable hydrochloride salt of the synthetic imidazothiazole derivative levamisole with anthelminthic and immunostimulating activities. In immunosuppressed states, levamisole may restore immune function by: 1) stimulating antibody formation, 2) stimulating T-cell activation and proliferation, 3) potentiatiating monocyte and macrophage phagocytosis and chemotaxis and 4) increasing neutrophil mobility, adherence, and chemotaxis.

Brand name for levofloxacin

A pyrrolidine with antiepileptic activity. The exact mechanism through which levetiracetam exerts its effects is unknown but does not involve inhibitory and excitatory neurotransmitter activity. Stereoselective binding of levetiracetam was confined to synaptic plasma membranes in the central nervous system with no binding occurring in peripheral tissue. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity.

Brand name for vardenafil hydrochloride

Brand name for ethinyl estradiol/levonorgestrel

The hydrochloride salt of levobupivacaine, an amide derivative with anesthetic property. Levobupivacaine reversibly binds voltage-gated sodium channels to modulate ionic flux and prevent the initiation and transmission of nerve impulses (stabilizing neuronal membrane), thereby resulting in analgesia and anesthesia. In comparison with racemic bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action.

An amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain.

The dihydrochloride salt form of the active levorotatory enantiomer of cetirizine, levocetirizine; a third generation, non-sedating, selective histamine H1 receptor antagonist, with antihistamine, anti-inflammatory and potential anti-angiogenic activities. Levocetirizine competes with endogenous histamine for binding at peripheral H1-receptor sites on the effector cell surface. This prevents the negative symptoms associated with histamine release and an allergic reaction. In addition, as histamine plays an important role in angiogenesis during an allergic inflammatory reaction, blocking the action of histamine may modulate the expression of proangiogenic factors and thus may prevent angiogenesis. As a third-generation histamine H1 receptor antagonist, levocetirizine has fewer side effects than most second-generation antihistamines.

An amino acid precursor of dopamine with antiparkinsonian properties. Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. When in the brain, levodopa is decarboxylated to dopamine and stimulates the dopaminergic receptors, thereby compensating for the depleted supply of endogenous dopamine seen in Parkinson's disease. To assure that adequate concentrations of levodopa reach the central nervous system, it is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, thereby diminishing the decarboxylation and inactivation of levodopa in peripheral tissues and increasing the delivery of dopamine to the CNS.

A broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth.

An orally available levorotary enantiomer of ketoconazole with potential steroidogenesis inhibitory activity. Following oral administration, levoketoconazole inhibits three cytochrome P450 family enzymes involved in glucocorticoid biosynthesis, 11beta-hydroxylase (CYP11B1), 17alpha-hydroxylase/17,20-lyase (CYP17A1) and steroid 21-hydroxylase (CYP21A2), which reduces the circulating levels of glucocorticoids. Therefore, this agent may normalize the high concentration of cortisol in the blood seen in patients with Cushing syndrome. Compared to racemic ketoconazole, the levo form is a more potent inhibitor of glucocorticoid synthesis. Additionally, this enantiomer is less likely to inhibit cholesterol 7alpha-hydroxylase (CYP7A1); therefore, its use may reduce the risk of hepatoxicity. Cushing syndrome is caused by high levels of cortisol in the blood either due to excessive production and secretion of corticosteroids, which is often the result of adrenocorticotropic hormone (ACTH)-secreting pituitary or adrenocortical neoplasms, or the use of synthetic corticosteroids.

A levo isoform of leucovorin calcium with antineoplastic activity. Levoleucovorin is an active metabolite of folic acid, which does not require metabolism by dihydrofolate reductase. This agent counteracts the toxic effects of other folic acid derivative agents, rescuing the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity.

A synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) with antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2.

The levorotatory form of norgestrel and synthetic progestogen with progestational and androgenic activity. Levonorgestrel binds to the progesterone receptor in the nucleus of target cells, thereby stimulating the resulting hormone-receptor complex, initiating transcription, and increasing the synthesis of certain proteins. This results in a suppression of luteinizing hormone (LH) activity and an inhibition of ovulation, as well as an alteration in the cervical mucus and endometrium.

A long-acting, hormone-releasing, intrauterine device consisting of a small, T-shaped, polyethylene frame and a reservoired synthetic progesterone with progestational and potential antineoplastic activities. After insertion of this system into the uterus, the device slowly and gradually releases the hormone. Levonorgestrel acts by binding to the progesterone receptor in the nuclei of target cells, resulting in transcription activation and an alteration in protein synthesis. Subsequently, luteinizing hormone (LH) activity and ovulation are suppressed. Levonorgestrel may also exhibit antiproliferative activity in endometrial tissue.

Brand name for levodopa

Brand name for ethinyl estradiol/levonorgestrel

The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.

The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.

Brand name for levothyroxine sodium

Brand name for aminolevulinic acid hydrochloride

Brand name for escitalopram oxalate

A fully human monoclonal agonistic antibody directed against tumor necrosis factor-alpha (TNF-alpha)-related apoptosis-inducing ligand receptor-2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural ligand TRAIL, lexatumumab binds to and activates TRAIL-R2, which may trigger apoptosis in and inhibit the growth of TRAIL-R2-expressing tumor cells. TRAIL-R2, also known as death receptor 5 (DR5), is a member of the TNF receptor family and is expressed on many malignant cell types.

An orally bioavailable small-molecule with tubulin-inhibiting, vascular-disrupting, and potential antineoplastic activities. Lexibulin inhibits tubulin polymerization in tumor blood vessel endothelial cells and tumor cells, blocking the formation of the mitotic spindle and leading to cell cycle arrest at the G2/M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death.

Brand name for regadenoson

The levo-enantiomer of an orally bioavailable polyphenolic aldehyde, derived primarily from unrefined cottonseed oil, with potential antineoplastic activity. Mimicking the inhibitory BH3 (Bcl-2 homology 3) domain of endogenous antagonists of Bcl-2, L-gossypol binds to and inhibits various anti-apoptotic Bcl-2 proteins, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. This agent has greater affinity for Bcl-2 proteins than racemic gossypol.

Brand name for mesalamine

The orally active fumarate salt of the benzimidazole derivative liarozole with potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis.

Brand name for cemiplimab-rwlc

An immunoradioconjugate containing metuximab, an antibody fragment targeting the hepatocellular cancer (HCC)-associated antigen HAb18G/CD147, that is conjugated to the radioisotope iodine I 131, with potential antineoplastic activity. Upon administration, the metuximab moiety of licartin targets and binds to HAb18G/CD147 on HCC cells; upon internalization, the radioisotope I 131 delivers a cytotoxic dose of gamma radiation, thereby causing selective destruction of HAb18G/CD147-expressing cells. HAb18G/CD147, a member of CD147 family, is overexpressed in HCC and fibroblasts and its expression is associated with cancer cell progression and increased adhesion, invasion and metastasis.

A derivative of the phenol chalconoid, found in and extracted from the roots of Glycyrrhiza species G. glabra and inflata, with potential anti-inflammatory, antibacterial, and anticancer activities. Upon administration, licochalcone A inhibits the phosphatidylinositol-3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway and inhibits the activity of c-Jun N-terminal kinase 1 (JNK-1), a member of the mitogen-activated protein kinase (MAPK) family that plays a role in the MAPK-mediated signaling pathway. Inhibition of the PI3K/Akt/mTOR- and MAPK-signaling pathways induces cell cycle arrest and apoptosis, decreases migration and invasion of cancer cells, and inhibits tumor cell proliferation. Licochalcone A also prevents the production of reactive oxygen species (ROS), and reduces oxidative stress through the nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway.

An inhibitor of the sodium-dependent glucose co-transporter (sodium-glucose transporter; sodium-glucose transport protein; sodium-glucose linked transporter; SGLT) family members 1 and 2 (SGLT1/2) with antihyperglycemic activity. By binding to and blocking SGLT1/2, licogliflozin suppresses the reabsorption of glucose in the proximal tubule within the kidneys and enhances urinary excretion of glucose. This normalizes blood glucose levels. SGLT1/2, parts of a transport system expressed in the proximal renal tubules, mediate the majority of renal glucose reabsorption from tubular fluid.

An herbal extract derived from the root of the plant Glycyrrhiza glabra with potential anti-inflammatory, antioxidant, and antineoplastic activities. Licorice root extract contains glycoside glycyrrhizinic acid and numerous flavonoids. Glycyrrhizinic acid in licorice root extract is hydrolyzed to glycyrrhetic acid (GA); GA inhibits 11 beta-hydroxysteroid dehydrogenase, resulting in inhibition of the conversion of cortisol to the inactive steroid cortisone and elevated cortisol levels. In addition, GA inhibits 17,20-lyase and 17 beta-hydroxysteroid dehydrogenase, resulting in decreased conversions of 17-hydroxyprogesterone to androstenedione and androstenedione to testosterone. The primary antioxidant found in licorice root, the flavonoid glabridin, may inactivate or inhibit the activities of some cytochrome P450 enzymes. In tumor cells, beta-hydroxy-DHP, another flavonoid, may induce Bcl-2 phosphorylation, apoptosis, and G2/M cell cycle arrest.

Brand name for fluocinonide cream

The hydrochloride salt from of lidocaine, an aminoethylamide and a prototypical member of the amide class anesthetics. Lidocaine interacts with voltage-gated Na+ channels in the nerve cell membrane and blocks the transient increase in permeability of excitable membranes to Na+. This prevents the generation and conduction of nerve impulses and produces a reversible loss of sensation. Lidocaine hydrochloride also exhibits class IB antiarrhythmic effects. The agent decreases the flow of sodium ions into myocardial tissue, especially on the Purkinje network, during phase 0 of the action potential, thereby decreasing depolarization, automaticity and excitability.

An ophthalmic gel formulation containing the synthetic amide-type anesthetic lidocaine, with potential analgesic activity. Upon ophthalmic application, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in neuronal cell membranes. Lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses, which numbs the nerves, prevents the trigemino-cardiac reflex and produces a reversible local anesthesia.

A transdermal patch containing a 5 percent aqueous base solution of the synthetic amide-type anesthetic lidocaine with analgesic activity. Upon topical application and transdermal delivery, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in the neuronal cell membrane; lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses and produces a reversible local anesthesia.

A synthetic aminoethylamide with local anesthetic activity applied topically to either the skin or mucous membranes. Lidocaine stabilizes the neuronal cell membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the initiation and conduction of nerve impulses and producing a reversible loss of sensation.

Brand name for lidocaine patch 5%

A formulation composed of nanoparticles derived from the human papillomavirus (HPV-NPs) and conjugated to the infrared (IR)-activated fluorescent dye IR700 (IR-700), with potential antineoplastic activity. Upon intravitreal injection, the HPV-NPs target and bind to heparan-sulfated proteoglycans (HSPG) expressed by ocular melanoma cells. Upon irradiation with near-IR (NIR) light, the photosensitizer IR700 becomes activated, generates reactive oxygen species (ROS) and selectively damages the melanoma cell membrane, which induces necrosis of the melanoma cells while sparing the surrounding, healthy non-HSPG-expressing tissue, and potentially preserving vision. HSPGs are overexpressed on a variety of cancer cell types.

An attenuated oncolytic vaccinia virus encoding the light-emitting fusion protein Renilla luciferase-Aequorea green fluorescent protein (RUC-GFP) with potential bioluminescent and antineoplastic activities. Upon administration, light-emitting oncolytic vaccinia virus GL-ONC1 specifically enters tumor cells due to the permeable nature of the tumor vasculature. Once inside the cell, the virus replicates, resulting in tumor cell lysis and the release of mature viral particles into the tumor microenvironment. Released viral particles may then infect and destroy neighboring tumor cells. In addition, the release of tumor-associated antigens (TAAs) by lysed tumor cells into the bloodstream may activate the immune system to mount a cytotoxic T lymphocyte (CTL) response against the tumor. The expression of RUC-GFP by this agent allows for both detection and monitoring of virally infected tumor cells in vivo and vitro with luciferase-mediated bioluminescence imaging and fluorescence imaging techniques.

An oral dietary supplement containing a natural cyclic monoterpene and major component of the oil extracted from citrus peels with potential chemopreventive and antitumor activities. Although the mechanism of action has yet to be fully elucidated, limonene and its metabolites perillic acid, dihydroperillic acid, uroterpenol and limonene 1,2-diol may inhibit tumor growth through inhibition of p21-dependent signaling and may induce apoptosis via the induction of the transforming growth factor beta-signaling pathway. In addition, they inhibit post-translational modification of signal transduction proteins, resulting in G1 cell cycle arrest as well as differential expression of cell cycle- and apoptosis-related genes.

The acetate salt form of linaclotide, a synthetic, fourteen amino acid peptide and agonist of intestinal guanylate cyclase type C (GC-C), which is structurally related to the guanylin peptide family, with secretagogue, analgesic and laxative activities. Upon oral administration, linaclotide binds to and activates GC-C receptors located on the luminal surface of the intestinal epithelium. This increases the concentration of intracellular cyclic guanosine monophosphate (cGMP), which is derived from guanosine triphosphate (GTP). cGMP activates the cystic fibrosis transmembrane conductance regulator (CFTR) and stimulates the secretion of chloride and bicarbonate into the intestinal lumen. This promotes sodium excretion into the lumen and results in increased intestinal fluid secretion. This ultimately accelerates GI transit of intestinal contents, improves bowel movement and relieves constipation. Increased extracellular cGMP levels may also exert an antinociceptive effect, through an as of yet not fully elucidated mechanism, that may involve modulation of nociceptors found on colonic afferent pain fibers. Linaclotide is minimally absorbed from the GI tract.

A potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. The inhibition of DPP-4 by linagliptin appears to be longer lasting than that by some other DPP-4 inhibitors tested.

A synthetic oxazolidinone derivative, linezolid selectively inhibits an early step in bacterial protein synthesis and affects blood pressure through monoamine oxidase inhibition. It is effective against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus strains, coagulase-negative Staphylococci, vancomycin-resistant Enterococci, and penicillin-resistant Streptococcus pneumoniae strains.

An orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Linifanib inhibits members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families; it exhibits much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. This agent does not have a general antiproliferative effect due to its high dose requirement. However, linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as fms-related tyrosine kinase receptor-3 (FLT3).

A formulation of the 6-omega fatty acid derivative 2’-linoleyl carbonate (LOC) conjugated to paclitaxel, a taxane compound extracted from the Pacific yew tree Taxus brevifolia, with potential antineoplastic activity. Paclitaxel binds to and stabilizes tubulin, thereby interfering with the dynamics of microtubule assembly/disassembly and resulting in the inhibition of cell division. LOC enhances the uptake of paclitaxel by tumor cells, thereby concentrating this agent in tumor cells compared to normal cells, and may decrease its toxicity profile; fatty acids serve as energy sources and biochemical precursors for the fast growing tumor cells.

Brand name for roquinimex

An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGFR-1 stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

A humanized recombinant monoclonal antibody directed against CD33, a cell surface antigen found on myeloid leukemia blasts and early hematopoietic progenitor cells. Lintuzumab stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing CD33, resulting in a decrease in tumor burden. The humanized version of this monoclonal antibody exhibits less immunogenicity and improved binding affinity compared to its murine counterpart.

Brand name for linaclotide acetate

Brand name for baclofen

The sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4).

A long acting glyco-pegylated recombinant form of human granulocyte colony-stimulating factor (G-CSF), with hematopoietic activity. Similar to G-CSF, lipegfilgrastim binds to and activates specific cell surface receptors, and stimulates neutrophil progenitor proliferation and differentiation. Therefore, this agent may prevent the duration and incidence of chemotherapy-induced neutropenia. Compared to filgrastim, lipegfilgrastim has a prolonged plasma half-life.

A lipid nanoparticle encapsulating mRNAs encoding for the human co-stimulatory protein tumor necrosis factor ligand superfamily member 4 (TNFSF4; OX40 Ligand; OX40L), the pro-inflammatory cytokines interleukin-23 (IL-23) and interleukin-36gamma (IL-36gamma), with potential immunomodulatory and anti-tumor activities. Upon intratumoral (IT) injection of the lipid nanoparticle encapsulated mRNAs encoding human OX40L/IL-23/IL-36gamma mRNA-2752, the lipid nanoparticle binds to the plasma membrane of cells and releases the mRNAs into the cell. The OX40L mRNA is then translated by the cellular protein translation machinery to produce OX40L protein, which is then expressed on the plasma membrane of the cells that internalized the OX40L mRNA. OX40L binds to and activates signaling pathways downstream of its cognate receptor tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40), which is expressed on activated T-cells. OX40L/OX40 binding promotes increased cytokine production, which can induce proliferation of memory and effector T lymphocytes against the nearby tumor cells. The co-administration of IL-23 and IL-36gamma further stimulates anti-tumor immune responses. Altogether, this may enhance T cell mediated anti-tumor immune responses thereby killing of the tumor cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand superfamily, provides a co-stimulatory signal for the proliferation and survival of activated T-cells. IL-36gamma activates innate immune cells and promotes T-helper 1 (Th1) responses, whereas IL-23 has been implicated in Th1/Th17 immunity as well as in the modulation of antigen-presenting cells (APCs).

A proprietary formulation consisting of a lipid nanoparticle encapsulating a synthetic messenger RNA (mRNA) encoding the human co-stimulatory protein tumor necrosis factor ligand superfamily member 4 (TNFSF4; OX40 Ligand; OX40L), with potential immunomodulatory and antitumor activities. Although the mechanism of action has not been completely characterized, following intratumoral injection of lipid nanoparticle encapsulated OX40L mRNA-2416, the lipid nanoparticle moiety presumably binds to the plasma membrane of nearby cells and releases the OX40L mRNA into the cell. The OX40L mRNA is then translated by the cellular protein translation machinery to produce OX40L protein, which is then expressed on the plasma membrane of the cells that internalized the OX40L mRNA. OX40L binds to and activates signaling pathways downstream of its cognate receptor tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40), which is expressed on activated T cells. OX40L/OX40 binding promotes increased cytokine production, which can induce proliferation of memory and effector T lymphocytes. Altogether, this may enhance an immune response that promotes the killing of nearby tumor cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand family, provides a co-stimulatory signal for the proliferation and survival of activated T cells.

Brand name for ethiodized oil

Brand name for atorvastatin calcium

Brand name for heparin sodium

Brand name for therapeutic progesterone

An endotoxin and biologically active component of the Gram-negative bacterial cell wall that is a Toll-like receptor 4 (TLR4) agonist with potential immunostimulatory activity. Upon internalization, lipopolysaccharide (LPS) activates TLR4 which in turn activates the NFkappaB pathway, in addition to mitogen-activated protein kinases signaling pathways. This leads to the release of proinflammatory cytokines and stimulates an innate immune response against vaccine antigens.

A liposome-encapsulated formulation of the polyene antifungal antibiotic amphotericin B produced by the bacterium Streptomyces nodosus with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, and alters cell membrane integrity, resulting in leakage of intracellular components and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. Compared to amphotericin B alone, liposomal delivery of amphotericin B allows for a greater drug concentration in target tissues while decreasing systemic side effects.

A liposome-encapsulated form of the semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA and protein synthesis. This agent circumvents multidrug-resistance (MDR) transporters, including P-glycoprotein (P-gp). Liposomal annamycin is less toxic and shows improved antitumor activity compared to annamycin.

A sterically stabilized, pegylated liposomal formulation containing CKD602, a semi-synthetic analogue of campthotecin with potential antitumor activity. CKD602 inhibits the action of topoisomerase I, an enzyme that produces reversible single-strand breaks in DNA during DNA replication. CDK602 stabilizes the topoisomerase I and DNA complex, resulting in the inhibition of religation of DNA breaks, inhibition of DNA replication, and apoptotic cell death. The polyethylene glycol coating of liposomal belotecan allows for greater plasma circulation time, thus enhancing the concentration of CKD602 at the tumor site. Encapsulation of CKD602 preserves the active lactone form, resulting in an increased cytotoxic effect of CKD602.

A synthetic formulation in which the antineoplastic agent cisplatin is encapsulated in lipids. Liposomal cisplatin consists of small aggregates of cisplatin covered by a single lipid bilayer. Encasement in liposomes improves cisplatin's tumor bioavailability and toxicity profile. Liposomal encapsulation does not affect the pharmacological properties of cisplatin directly. Cisplatin forms highly reactive, charged, platinum complexes which bind to nucleophilic groups such as GC-rich sites in DNA, inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in apoptosis and cell growth inhibition.

The liposomal formulation of a c-raf-1 antisense oligonucleotide, with potential antineoplastic activity. Liposomal c-raf antisense oligonucleotide targets the translation initiation site of human c-raf-1 mRNA, thereby blocking the expression and production of Raf-1 protein and thus inhibits tumor cell growth and development. Raf-1 plays a key role in the RAF/MEK/ERK signaling pathway, which regulates mammalian cell proliferation and growth. The liposomal formulation increases the solubility of the c-raf antisense oligonucleotide, thus improving its pharmacodynamic profile.

A liposomal formulation containing curcumin, a poorly water-soluble polylphenol pigment isolated from the plant Curcuma longa, with potential antineoplastic, chemopreventive, antioxidant, anti-angiogenic and anti-inflammatory activities. Upon intravenous administration of liposomal curcumin, this agent blocks the formation of reactive-oxygen species, neutralizes free radicals, and exhibits anti-inflammatory properties as a result of inhibition of cyclooxygenases (COX) and other enzymes involved in inflammation. In addition, curcumin disrupts various cell signal transduction pathways involved in carcinogenesis, inhibits the activity of nuclear factor-kappa B (NF-kB), SRC, and annexin A2 (ANXA2), and reduces the expression of both matrix metalloproteinase-9 (MMP-9) and vascular endothelial growth factor receptor 2 (VEGFR2). This prevents and/or inhibits tumor cell formation and proliferation. Liposome encapsulation of curcumin improves its efficacy, when compared to the administration of unencapsulated curcumin.

A liposome-encapsulated form of the citrate salt of the anthracycline antineoplastic antibiotic daunorubicin. Daunorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Liposomal delivery of doxorubicin citrate improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects.

A formulation of the poorly soluble, semi-synthetic, second-generation taxane docetaxel encapsulated within liposomes, with antineoplastic activity. Upon intravenous administration, docetaxel binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. This liposomal formulation solubilizes docetaxel without the use of toxic solvents such as Tween 80, permitting the administration of larger doses of docetaxel while avoiding solvent-associated toxicity, including hypersensitivity reactions. In addition, liposomal delivery of docetaxel improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile.

A liposome-encapsulated formulation of the mesylate salt form of eribulin, a synthetic, macrocyclic ketone analogue of halichondrin B, a substance derived from the marine sponge genus Halichondria, with potential antineoplastic activity. Eribulin binds to the vinca domain of tubulin and inhibits both the polymerization of tubulin and the assembly of microtubules. This results in the inhibition of mitotic spindle assembly, the induction of cell cycle arrest at G2/M phase, as well as tumor cell apoptosis. Compared to the administration of eribulin alone, liposomal delivery of eribulin allows for a longer half-life, which allows increased drug concentration in target tissues while decreasing systemic toxicity.

A liposomal nanoparticle-based therapeutic vaccine composed of the cationic lipid R-DOTAP (R-enantiomer of 1,2-dioleoyl-3-trimethylammonium-propane chloride) encapsulating six human papillomavirus 16 (HPV-16) E6 and E7 peptides, with potential immunostimulating activity. Upon subcutaneous administration of the liposomal HPV-16 E6 and E7 multipeptide vaccine, the nanoparticles are taken up by antigen presenting cells (APCs), specifically dendritic cells (DCs), which may stimulate the immune system to induce a cytotoxic T-lymphocyte response (CTL) against HPV-16 E6 and E7-expressing tumor cells. HPV-16 E6 and E7 are oncoproteins that play a key role in the tumorigenesis of a variety of cancers.

A formulation in which liposomes are loaded with the cytokine interleukin-2 (IL-2). By activating cytotoxic T lymphocytes, such as lymphokine-activated killer cells, and increasing levels of the cytotoxic cytokines interferon-gamma (IFN-gamma) and transforming growth factor-beta (TGF-beta), IL-2 may exhibit antitumoral activity. Liposomal formulations of IL-2 may promote entry of the cytokine into target tumor cells and may be used as an immunoadjuvant in cancer vaccine therapy.

A liposome-encapsulated formulation of lurtotecan with antineoplastic activity. Lurtotecan, a semisynthetic analogue of camptothecin, selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex during S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks. This ultimately results in an inhibition of DNA replication, inducing double-stranded DNA breakages, obstruction of RNA and protein synthesis and triggering apoptosis. Furthermore, this agent also stimulates degradation of topoisomerase I, likely mediated through ubiquitin-proteasomal pathway. Liposomal delivery of lurtotecan improves its penetration and delivery into tumors while lowering systemic side effects.

A formulation composed of the hydrochloride salt form of the anthracenedione antibiotic mitoxantrone encapsulated within liposomes, with potential antineoplastic activity. Upon intravenous administration, mitoxantrone intercalates into and forms crosslinks with DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, which both results in DNA strand breaks and prevents DNA synthesis. This leads to the induction of apoptosis in the rapidly dividing cancer cells. The liposomal delivery of mitoxantrone improves drug penetration into tumors and decreases drug clearance, thereby increasing drug circulation and therapeutic efficacy while lowering the toxic effects.

A cancer vaccine comprised of a 43 amino acid epitope from glycoprotein MUC1 (mucin 1) and the synthetic Toll-like receptor 4 (TLR-4) agonist PET lipid A encapsulated in cholesterol/dipalmitoylphosphatidylcholine (DPPC)/dimyristoylphosphatidylglycerol (DMPG) liposomes, with potential immunostimulatory and antineoplastic activities. The MUC1 epitope is composed of two 20 amino glycosylated VNTR (various number tandem repeats) from human MUC1A and including 6 glycosylated sites modified by Tn (alfa-N-acetyl-D-galactosamine). Immunization of liposomal MUC1/PET-lipid A vaccine results in an antibody as well as a cytotoxic T-lymphocyte (CTL) response against hypoglycosylated MUC1 expressing tumor cells. The tumor associated antigen MUC1, a type І transmembrane protein, is overexpressed and aberrantly glycosylated in a variety of tumor cells. As a vaccine adjuvant, PET lipid A, also known as penta erythritol lipid A, stimulates both cellular and humoral responses to the vaccine antigen.

A synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile.

A liposomal formulation of the prodrug oxaliplatin, an organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group', with antineoplastic activity. After displacement of the labile oxalate ligand leaving group, the active oxaliplatin derivatives monoaquo and diaquo DACH platinum alkylate macromolecules, and form both inter- and intra-strand platinum-DNA crosslinks; inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity ensue. The DACH side chain appears to inhibit alkylating-agent resistance. A leaving group is an atom or a group of atoms that is displaced as a stable species taking with it its bonding electrons.

A liposome-encapsulated formulation of paclitaxel, a taxoid compound extracted from the Pacific yew tree Taxus brevifolia, with antineoplastic property. Paclitaxel binds to tubulin and interferes with the assembly/disassembly dynamics of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis via inactivation of the apoptosis inhibitor, B-cell Leukemia 2 (Bcl-2) protein. Paclitaxel liposome formulation potentially enhances delivery of higher doses of paclitaxel to the target tissues and exhibits lower systemic toxicity.

A therapeutic preparation consisting of the beta-emitting radioisotope rhenium Re 186 encapsulated in a nanoliposome, with potential antineoplastic activity. Upon intratumoral infusion of liposomal rhenium Re 186, the radioisotope releases radiation, which directly kills the tumor cells. The nanoliposomes facilitate the retention of the radioisotope by the tumor cells and localize the radiocytotoxicity to the tumor while sparing surrounding normal, healthy cells. Re-186 has a short half-life and a short path length, which contributes further to limiting the radiotoxicity to the tumor cells.

The liposomal formulation of SN-38 (7-ethyl-10-hydroxy-camptothecin), a biologically active metabolite of the prodrug irinotecan, with potential antineoplastic activity. SN-38 binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis. SN-38 has been reported to exhibit up to 1,000-fold more cytotoxic activity against various cancer cells in vitro than irinotecan. The liposomal formulation of SN-38 increases the solubility of SN-38, which is a relatively insoluble compound, and improves the pharmacodynamic profile as compared to SN-38 alone.

A topical lotion that contains the enzyme T4-bacteriophage endonuclease V encapsulated within liposomes. With topical liposomal delivery, the DNA repair enzyme T4-bacteriophage endonuclease V is transported into skin cells, where the enzyme enters cell nuclei and binds to and incises pyrimidine dimers, thereby catalyzing the first reaction step of the cellular excision repair pathway for removing DNA replication-inhibiting pyrimidine dimers produced within duplex DNA through exposure to ultraviolet (UV) irradiation. In vitro and in vivo studies indicate that T4N5 liposomes increases repair of DNA damage caused by UV irradiation.

The hydrochloride salt of a semisynthetic derivative of camptothecin mixed with sphingomyelin/cholesterol and sonicated to form small unilamellar vesicles containing topotecan, with potential antineoplastic activity. Liposomal opotecan hydrochloride mediates efficient drug delivery of topotecan into the cytosol from the endosome compartment. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery.

An intravenous formulation of tretinoin (vitamin A acid or all-trans retinoic acid) encased in liposomes. Tretinoin is a naturally occurring retinoic acid agent that binds to and activates retinoic acid receptors (RAR), effecting changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of carcinogenesis. This agent also inhibits telomerase, leading to telomere shortening and eventual apoptosis of certain tumor cell types. Liposome encapsulation extends the half-life of intravenously administered tretinoin.

A formulation of the tartrate salt form of vinorelbine, a semisynthetic vinca alkaloid, encapsulated within liposomes, with potential antineoplastic activity. Upon intravenous administration, vinorelbine binds to tubulin within tumor cells and prevents the formation of the mitotic spindle, resulting in cell cycle arrest, induction of apoptosis and an inhibition of tumor cell growth. Compared to the administration of vinorelbine alone, the liposomal formulation improves drug penetration into tumors and decreases drug clearance, thereby increasing vinorelbine's efficacy while lowering the toxicity profile.

A formulation of the citrate salt of the antineoplastic anthracycline antibiotic doxorubicin, encapsulated within liposomes, with antitumor activity. Doxorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and RNA synthesis. This agent also interacts with cell membrane lipids causing lipid peroxidation. Liposomal delivery of doxorubicin improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile.

A liposomal formulation containing a nucleotide that mimics the human tumor suppressor microRNA (miRNA) miR-34, with potential antineoplastic activity. Upon administration, liposome-encapsulated MRX34 mimics miR-34 by inhibiting the expression of a variety of oncogenes including MYC, MET, BCL2, and beta-catenin. This induces cell cycle arrest, senescence and apoptosis in susceptible tumor cells. miR-34 is downregulated in most solid and hematologic malignancies and regulates the expression of a variety of genes. This miRNA plays an important role in the inhibition of cancer cell stemness, metastasis and cancer cell survival.

A systemic gene therapy anti-cancer agent composed of cationic liposomes, which encapsulates plasmid DNA encoding for the tumor suppressor gene RB94 and is complexed with anti-transferrin receptor single chain antibody fragment (TfRscFv), with potential antineoplastic activity. Upon systemic administration of liposome-encapsulated RB94 plasmid DNA gene therapy agent SGT-94, the TfRscFv portion of this agent selectively targets the tumor cells expressing transferrin receptors. TfRscFv binding to the transferrin receptor allows receptor-mediated endocytosis and transfection, followed by the expression of RB94 gene. This induces tumor cell apoptosis through an as-of-yet unknown pathway. RB94 is a modified, N-terminal truncated form of the full-length protein retinoblastoma gene RB110, and exerts enhanced antitumor activity. The transferrin receptor (TfR) functions in cellular iron uptake through its interaction with transferrin, and is overexpressed in a variety of tumor types.

A topical hydrophilic gel containing a recombinant form of the human Cu/Zn superoxide dismutase (SOD1), a cytoplasmic antioxidant enzyme, encapsulated in liposomes with potential anti-inflammatory and adjuvant activities. Upon application of liposome-encapsulated recombinant human Cu/Zn SOD as a thin film on the irradiated area, the recombinant SOD1 is released and scavenges free oxygen radicals, thereby protecting cells from oxidative stress. This may prevent radiation-induced dermatitis as well as other types of skin reactions.

A liposomal formulation containing the antisense oligodeoxynucleotide (ODN) growth factor receptor-bound protein 2 (Grb2), with potential antineoplastic activity. Upon administration, liposome-incorporated Grb2 antisense oligodeoxynucleotide binds directly to and blocks Grb2 mRNA, thereby preventing Grb2 protein synthesis, leading to inhibition of cell proliferation of cancer cells overexpressing Grb2. Grb2, an adaptor protein involved in growth signaling pathways, is upregulated in certain tumor cells.

Brand name for camptothecin analogue TLC388

Brand name for phenprocoumon

A long-acting, fatty acylated glucagon-like peptide-1 (GLP-1) analog administered subcutaneously, with antihyperglycemic activity. Liraglutide's prolonged action and half-life of 11-15 hours are attributed to the attachment of the fatty acid palmitic acid to GLP-1 that reversibly binds to albumin. Albumin binding protects liraglutide from immediate degradation and elimination and causes GLP-1 to be released from abumin in a slow and consistent manner. This agent may cause thyroid C-cell tumors and increases the risk of acute pancreatitis.

A long-acting, fatty acylated glucagon-like peptide-1 (GLP-1) analog administered subcutaneously, with antihyperglycemic activity. Liraglutide's prolonged action and half-life of 11-15 hours are attributed to the attachment of the fatty acid palmitic acid to GLP-1 that reversibly binds to albumin. Albumin binding protects liraglutide from immediate degradation and elimination and causes GLP-1 to be released from abumin in a slow and consistent manner. This agent may cause thyroid C-cell tumors and increases the risk of acute pancreatitis.

A fully human monoclonal antibody against killer-cell immunoglobulin-like receptors (KIR), with potential antineoplastic activity. Upon administration, lirilumab binds to KIR, thereby preventing the binding of KIR ligands to KIR on natural killer (NK) cells. By blocking these inhibitory receptors, NK cells become activated and attack cancer cells leading to tumor cell death. KIR, a member of the immunoglobulin superfamily, is expressed on the surface of NK cells.

The dimesylate form and prodrug of the d-isomer of amphetamine, a non-catecholamine sympathomimetic amine with central nervous system (CNS) stimulating activity. Upon administration, lisdexamphetamine is converted to dextroamphetamine through cleavage of the lysine group. Dextroamphetamine acts by facilitating the release of catecholamines, particularly noradrenaline and dopamine, from its storage sites in nerve terminals in the CNS, and inhibits their uptake within the mesocorticolimbic system, a major component of the brain reward system, resulting in measurable behavioral changes such as euphoria, mental alertness and excitement and appetite suppression. As a CNS stimulant, this agent may increase blood pressure.

An orally bioavailable, long-acting angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Lisinopril, a synthetic peptide derivative, specifically and competitively inhibits ACE, which results in a decrease in the production of the potent vasoconstrictor angiotensin II and, so, diminished vasopressor activity. In addition, angiotensin II-stimulated aldosterone secretion by the adrenal cortex is decreased which results in a decrease in sodium and water retention and an increase in serum potassium.

A preparation of a defined ratio of CD4+ and CD8+ autologous T lymphocytes transduced with a lentiviral vector expressing a chimeric antigen receptor (CAR) containing an anti-CD19 single chain variable fragment (scFv) fused to the signaling domain of 4-1BB (CD137), the zeta chain of the TCR/CD3 complex (CD3-zeta), and a truncated form of the human epidermal growth factor receptor (EGFRt), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, lisocabtagene maraleucel is directed to and induce selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. Devoid of both ligand binding domains and tyrosine kinase activity, the expressed EGFRt both facilitates in vivo detection of the administered, transduced T cells and can promote elimination of those cells through a cetuximab-induced antibody dependent cellular cytotoxicity (ADCC) response. The 4-1BB costimulatory signaling domain enhances both proliferation of T cells and antitumor activity.

A cancer vaccine containing a live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding a fusion protein composed of the tumor-associated antigen (TAA) human prostate-specific antigen (PSA) fused to a fragment of the immunostimulant listeriolysin O (LLO) protein, with potential immunostimulatory and antineoplastic activities. Upon administration of the Lm-LLO-PSA vaccine ADXS31-142, the expressed LLO-PSA is processed by antigen presenting cells (APCs), presented to the immune system by both major histocompatibility complex (MHC) I and II molecules, and activates the immune system to exert both an innate and adaptive immune response involving the recruitment and activation of T-lymphocytes against PSA-expressing tumor cells as well as the inhibition of tumor-infiltrating T regulatory cells (T regs) and myeloid-derived suppressor cells (MDSCs). This eventually results in tumor cell lysis.

Brand name for lithium carbonate

The carbonate salt of lithium, a soft alkali metal, with antimanic and hematopoietic activities. Lithium interferes with transmembrane sodium exchange in nerve cells by affecting sodium, potassium-stimulated adenosine triphosphatase (Na+, K+-ATPase); alters the release of neurotransmitters; affects cyclic adenosine monophosphate (cAMP) concentrations; and blocks inositol metabolism resulting in depletion of cellular inositol and inhibition of phospholipase C-mediated signal transduction. The exact mechanism through which lithium exerts its mood-stabilizing effect has not been established. In addition, lithium stimulates granulocytopoiesis and appears to increase the level of pluripotent hematopoietic stem cells by stimulating the release of hematopoietic cytokines and/or directly acting on hematopoietic stem cells.

Brand name for lithium carbonate

Brand name for lithium carbonate

Brand name for lithium carbonate

An inhibitor of the kinesin-related motor protein Eg5 with potential antineoplastic activity. Litronesib selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and consequently cell death in tumor cells that are actively dividing. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein that plays an essential role during mitosis, particularly in the regulation of spindle dynamics, including assembly and maintenance.

A live, attenuated measles vaccine with potential antineoplastic activity. Upon subcutaneous administration, live attenuated measles virus vaccine may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against measles-positive tumor cells. Measles virus has been shown to be present in some non-small cell lung cancers.

A probiotic containing live, cultivated, freeze-dried lactic acid bacteria with gastrointestinal (GI) protective, anti-inflammatory, immunomodulating and potential antitumor properties. Oral administration of probiotic bacteria help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier, interfere with the attachment of pathogenic bacteria and other harmful substances and may bind to and degrade carcinogens. This may prevent inflammation and possibly cancer. In addition, these bacteria produce lactic acid, thereby creating an acidic environment that is unfavorable for pathogens.

A proprietary, live-attenuated, double-deleted (LADD) strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding multiple, as of yet undisclosed, tumor-associated antigens (TAAs), with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, live-attenuated double-deleted Listeria monocytogenes bacteria JNJ-64041809 is taken up by antigen-presenting cells (APCs), including dendritic cells (DCs). The TAAs are subsequently expressed by the APCs and then processed and presented to the immune system by both major histocompatibility complex (MHC) class I and II molecules. This activates the immune system and leads to the recruitment and activation of cytotoxic T lymphocytes (CTLs) against the TAA-expressing tumor cells, eventually resulting in tumor cell lysis. Two genes contributing to the virulence of Lm have been removed to minimize the risk of infection.

A cancer vaccine containing a live-attenuated strain of the bacterium Listeria monocytogenes (Lm) encoding human papillomavirus (HPV) type 16 E7 fused to a non-hemolytic listeriolysin O protein with potential immunostimulatory and antineoplastic activities. Upon vaccination, Listeria expresses the HPV 16 E7 antigen and activates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against cancer cells expressing HPV 16 E7. This may result in tumor cell lysis. In addition, the Listeria vector itself may induce a potent immune response. HPV 16 E7, a cell surface glycoprotein and tumor associated antigen, is overexpressed in the majority of cervical cancer cells.

A proprietary, live-attenuated, double-deleted (LADD) strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding the tumor-associated antigens (TAAs) epidermal growth factor receptor mutant form EGFRvIII and human mesothelin, with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, the live-attenuated Listeria monocytogenes encoding EGFRvIII-mesothelin vaccine JNJ-64041757 is taken up by antigen-presenting cells (APCs), including dendritic cells (DCs). EGFRvIII and mesothelin are subsequently expressed by the APCs and then processed and presented to the immune system by both major histocompatibility complex (MHC) class I and II molecules. This activates the immune system and leads to the recruitment and activation of cytotoxic T-lymphocytes (CTLs) against EGFRvIII- and mesothelin-expressing tumor cells, eventually resulting in tumor cell lysis. EGFRvIII and mesothelin are overexpressed in many types of cancer. Two genes contributing to the virulence of Lm have been removed to minimize the risk of infection.

A live-attenuated, double-deleted strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding a mutant form of the tumor-associated antigens, epidermal growth factor receptor (EGFRvIII) and the cancer/testis antigen NY-ESO-1, with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, live-attenuated Listeria monocytogenes encoding EGFRvIII-NY-ESO-1 vaccine targets dendritic cells and expresses EGFRvIII and NY-ESO-1. This promotes both a potent innate immune response and an adaptive immune response involving the recruitment and activation of T lymphocytes against EGFRvIII and NY-ESO-1-expressing tumor cells, which results in tumor cell lysis.

A recombinant Listeria-based cancer vaccine containing a live-attenuated strain of the facultative intracellular bacterium Listeria monocytogenes (Lm) expressing human mesothelin with potential immunostimulatory and antineoplastic activities. Upon administration of this vaccine, Listeria invade professional phagocytes within the immune system and express mesothelin, which may activate a cytotoxic T-lymphocyte (CTL) response against mesothelin-expressing tumor cells, resulting in tumor cell lysis. In addition, the Listeria vector itself may induce a potent innate and adaptive immunity unrelated to mesothelin expression. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancers, including pancreatic, ovarian and lung cancers, and malignant mesotheliomas.

An orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities. Upon oral administration, LXRbeta agonist RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells. LXRbeta, a member of the oxysterol receptor family, which is in the nuclear receptor family of transcription factors, plays a key role in cholesterol transport, glucose metabolism and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor cell types. The expression of the ApoE protein becomes silenced in human cancers as they grow, become invasive, and metastasize; ApoE silencing is related to reduced survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers to evade the immune system and recruit blood vessels.

A 2-amino acid compound with immunomodulatory activity. L-leucyl-L-leucine methyl ester (LLME) is a lysosomotropic agent entering cells via receptor-mediated endocytosis. LLME undergoes a condensation process catalyzed by dipeptidyl peptidase I (DPPI) in lysosomes. Condensation of LLME leads to lysosomal rupture and DNA fragmentation in DPPI-expressing immune cells such as cytotoxic T-cells and natural killer cells. Therefore, this agent may be able to decrease the incidence of graft versus host disease (GVHD) via cytotoxic T-cell depletion. Furthermore, LLME has the potential for augmenting antibody production when used in pretreatment of peripheral blood mononuclear cells (PBMCs), possibly by interfering with gene expression of inflammatory factors.

A nutritional supplement containing the biologically active L-isomer of the essential amino acid lysine, with potential anti-mucositis activity. Upon oral intake, L-lysine promotes healthy tissue function, growth and healing and improves the immune system. L-Lysine promotes calcium uptake, is essential for carnitine production and collagen formation. As collagen is essential for connective tissue maintenance, this agent may also help heal mucosal wounds. This may help decrease and prevent mucositis induced by radiation or chemotherapy.

An intravenous (IV) amino acid (AA) solution containing the cationic amino acids L-lysine and L-arginine, with radioprotective activity. Upon IV administration of the AA solution, L-lysine and L-arginine are specifically taken up by the kidneys. This protects the kidneys from toxicity by certain co-administered radio-labeled peptides as they compete with radio-labeled peptides for renal uptake. This reduces uptake of the radio-labeled peptides by the kidneys and decreases their renal retention. It also increases the target-to-kidney ratio of the radio-labeled peptides, thereby reducing radiation exposure to the kidneys and preventing nephrotoxicity.

A chimeric protein consisting of the Fv portion of a monoclonal antibody attached to a fragment of Pseudomonas exotoxin A without its cell-binding region. LMB-1 immunotoxin targets B3, a Lewis Y-related carbohydrate epitope found on some solid tumors. The antibody attaches to the tumor cell and the exotoxin stops protein synthesis by inactivating elongation factor 2.

A fusion protein consisting of the Fv portion of a monoclonal antibody attached to a 38-kDa fragment of the Pseudomonas exotoxin A (with amino acids 365-380 deleted). LMB-2 immunotoxin targets the interleukin 2 receptor (also known as IL-2R or CD25) which is expressed on activated normal T and B cells and macrophages and on the cells of various hematologic malignancies. The antibody attaches to the IL-2R on the cell membrane, facilitating the entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.

A single chain chimeric protein consisting of a monoclonal antibody fragment attached to a portion of the Pseudomonas exotoxin A. LMB-7 immunotoxin attaches to B3, a Lewis Y-related carbohydrate epitope on some solid tumor cells. The antibody attaches to the cell and the exotoxin inhibits protein synthesis by inactivating elongation factor 2.

A recombinant disulfide stabilized anti-Lewis Y IgG immunotoxin containing a 38 KD toxic element derived from the Pseudomonas aeruginosa exotoxin A and a monoclonal antibody fragment, designed to target adenocarcinomas expressing Lewis Y. LMB-9 immunotoxin attaches to tumor cells, facilitating he entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.

A cancer vaccine containing a live, highly attenuated strain of the Gram-positive bacterium Listeria monocytogenes (LmddA) encoding a fusion protein composed of a chimeric peptide comprised of three highly immunogenic epitopes of the human tumor-associated antigen (TAA) HER2/neu (chHER2) fused to a non-hemolytic fragment of the immunostimulant listeriolysin O (LLO) protein, with potential immunostimulatory and antineoplastic activities. Upon administration of the LmddA-LLO-chHER2 vaccine ADXS31-142, the LmddA is taken up by phagocytic cells; then the listeriolysin portion of the expressed LLO-chHER2 can form pores in the phagolysosomes and the fusion protein can escape into the cytosol. In turn, the LLO-chHER2 is processed and presented to the immune system by the major histocompatibility complex (MHC) I on the phagocytic cells. Antigen presentation activates the immune system to exert an immune response involving the recruitment and activation of T lymphocytes against HER2-expressing tumor cells, and inhibits tumor-infiltrating T regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSCs). This eventually results in tumor cell lysis. HER2/neu, a tyrosine kinase receptor belonging to the epidermal growth factor receptor (EGFR) family, is overexpressed in various tumor cell types.

A preparation containing L-menthol with potential anti-peristaltic activity. Upon spraying directly onto the gastric mucosa, L-menthol preparation NPO-11 may relax gastrointestinal smooth muscle. This may result in a suppression of gastric peristalsis and may be beneficial during upper GI endoscopic procedures.

A nutritional supplement containing the biologically active form of the B9 vitamin folate, 5-methyltetrahydrofolate (L-methylfolate), with potential antineoplastic activity. Upon administration, L-methylfolate is able to provide methyl groups allowing an increase in the level of DNA methylation in the promoter regions of certain tumor-promoting genes, thereby reversing the DNA hypomethylation of these genes and inactivating them. This may result in a decrease of both tumor cell proliferation and tumor progression. In addition, administration of L-methylfolate may sensitize tumor cells to the cytotoxic effects of other chemotherapeutic agents. Unlike folic acid, L-methylfolate is able to cross the blood brain barrier and could be beneficial in the treatment of brain tumors. DNA hypomethylation of certain genes leads to chromosome instability and contributes to tumor development.

A preparation of allogeneic cytotoxic T-lymphocytes (CTL) made specifically reactive to three Epstein-Barr virus (EBV) proteins, latent membrane protein (LMP) 1, BamH1-A rightward frame-1 (BARF1) and EBV nuclear antigen 1 (EBNA1), with potential antineoplastic activity. Administration of LMP1/BARF1/ EBNA1-specific CTLs to patients with LMP1/BARF1/EBNA1-positive tumors may result in a specific CTL response against the tumor cells expressing these antigens, which can result in both cell lysis and the inhibition of tumor cell proliferation. LMP1, BARF1 and EBNA1 are expressed in various, EBV-associated malignancies, including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.

A preparation of cytotoxic T lymphocytes (CTL) transfected with a chimeric antigen receptor (CAR) specifically recognizing the Epstein-Barr virus (EBV) latent membrane protein 1 (LMP1; LMP-1), with potential antineoplastic activity. Upon administration of the LMP1-specific CAR-expressing T lymphocytes to patients with LMP1-positive tumors, the CTLs specifically target and lyse tumor cells expressing LMP1, thereby inhibiting tumor cell proliferation. The tumor-associated antigen (TAA) LMP1 is expressed in various malignancies, including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.

A peptide cancer vaccine containing amino acid residues 340-349 of the Epstein-Barr virus (EBV) latent membrane protein-2 (LMP-2) with potential immunostimulating and antineoplastic activities. Vaccination with LMP-2:340-349 peptide may boost the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.

A peptide cancer vaccine containing amino acid residues 419-427 of the latent membrane protein-2 (LMP-2) of the Epstein-Barr virus (EBV) with potential immunostimulating and antineoplastic activities. Vaccination with the LMP-2:49-427 peptide vaccine may boost the immune system to mount a specific cytotoxic T-lymphocyte response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.

A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to Epstein-Barr virus (EBV) latent membrane protein-2A (LMP2A), with potential antineoplastic activity. T-lymphocytes are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP2A. Subsequently, LMP2A-specific CTLs are exposed to EBV infected cells transfected with adenovirus encoding LMP2A, thereby further stimulating CTLs. Administered to patients with EBV-positive tumors, LMP2A-specific CTLs target LMP2A-positive cells, resulting in cell lysis and inhibition of cancer cell proliferation. EBV LMP2A may be expressed in various malignancies, including nasopharyngeal carcinoma and Hodgkin and non-Hodgkin lymphomas.

A proprietary, personalized plasmid DNA-based cancer vaccine composed of a live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) carrying a proprietary plasmid vector encoding multiple, patient-specific, immunogenic neoepitopes fused to a truncated form of the immunostimulant listeriolysin O (tLLO), with potential immunostimulatory and antineoplastic activities. Upon administration of the Lm-tLLO-neoantigens vaccine ADXS-NEO, the ADXS-NEO is taken up by antigen presenting cells (APCs), such as dendritic cells (DCs), and the expressed tLLO-neoantigens fusion protein is processed and presented to the immune system by both major histocompatibility complex (MHC) I and II molecules. This activates the immune system to exert both innate and adaptive immune responses involving the recruitment and activation of T lymphocytes against the tumor-associated antigens (TAAs) specifically expressed by the patient's tumor cells, and inhibits the immunosuppressive tumor-infiltrating T-regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSCs) within the tumor microenvironment (TME). This results in tumor cell lysis. The various unique mutation-derived TAAs that are used in ADXS-NEO are identified from a biopsy of the patient's tumor.

A third-generation, water-soluble platinum compound with potential antineoplastic activity. Lobaplatin forms highly reactive, charged, platinum complexes that bind to nucleophilic groups such as GC- and AG-rich sites in DNA, inducing intrastrand DNA cross-links. These cross-links will ultimately result in induction of apoptosis and cell growth inhibition. Compared to first and second generation platinum compounds, lobaplatin appears to be more stable, less toxic, have a better therapeutic index and may overcome tumor resistance.

A synthetic analog of bradykinin. Lobradimil is a potent, specific bradykinin B-2 receptor agonist that stimulates B-2 receptors expressed on the surface of brain capillary endothelial cells, thereby reversibly increasing the permeability of the blood-brain barrier (BBB). Compared to bradykinin, this agent possesses enhanced receptor selectivity, greater plasma stability, and a longer half-life.

Brand name for etodolac

A folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide ribonucleotide formyltransferase (GARFT), the enzyme that catalyzes the first step in the de novo purine biosynthetic pathway, thereby inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. The agent has been shown to be active against tumors that are resistant to the folate antagonist methotrexate.

A nitrosourea with antineoplastic activity. Lomustine alkylates and crosslinks DNA, thereby inhibiting DNA and RNA synthesis. This agent also carbamoylates DNA and proteins, resulting in inhibition of DNA and RNA synthesis and disruption of RNA processing. Lomustine is lipophilic and crosses the blood-brain barrier.

A synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers.

An orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist; binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Unlike many other antiprogestins such as mifepristone, this agent does not appear to convert to an agonist in the presence of protein kinase A (PKA) activators and shows high antiprogestagenic activity on both progesterone receptor (PR) isoforms PR-A and PR-B.

A peptide vaccine consisting of a combination of seven synthetic long peptides (SLPs), which are each about 30 amino acids in size, and derived from cancer-testis antigens (CTA) and melanocytic differentiation proteins (MDP), with potential immunostimulating and antitumor activities. Upon administration, long peptide vaccine 7 may stimulate the host immune system to mount a cytotoxic T-cell lymphocyte (CTL) response against tumor cells expressing these peptides. CTA and MDP are overexpressed in a variety of cancer cell types.

A long-acting release (LAR) formulation containing pasireotide, a synthetic long-acting cyclohexapeptide, with somatostatin-like activity. Upon intramuscular administration of the LAR formulation of pasireotide, this somatostatin analog strongly binds to and activates somatostatin receptor (SSTR) subtypes 1, 2, 3, and 5. This leads to an inhibition in the secretion of human growth hormone (hGH) and results in decreased production of insulin-like growth factor (IGF-1), which may inhibit IGF-1-mediated cell signaling pathways. This may lead to an inhibition in tumor cell growth and an increase in apoptosis in IGF-1-overexpressing tumor cells. In addition, this agent causes a reduction in adrenocorticotropic hormone (ACTH), which leads to an inhibition of cortisol secretion. ACTH-producing tumors cause hypersecretion of cortisol which results in many unwanted symptoms. This agent may also block other key survival pathways such as the phosphatidylinositol 3-kinase (PI3K) and the mitogen-activated protein kinase (MAPK) signaling pathways. Pasireotide also inhibits vascular endothelial growth factor (VEGF) secretion, thereby decreasing angiogenesis and tumor cell growth in VEGF-overexpressing tumor cells. The long-acting form of pasireotide allows for less frequent administration as compared to the original form of this agent. SSTRs are overexpressed by some neuroendocrine and non-neuroendocrine tumor cells.

Brand name for trifluridine and tipiracil hydrochloride

The hydrochloride salt form of loperamide, a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity. Loperamide acts on the mu-receptors in the intestinal mucosa. This leads to a decrease in gastrointestinal motility by decreasing the circular and longitudinal smooth muscle activity of the intestinal wall. This slows intestinal transit and allows for more water and electrolyte absorption from the intestines. Loperamide is not significantly absorbed from the gut and does not cross the blood-brain barrier. Therefore it has no central nervous system effects.

Brand name for gemfibrozil

A protease inhibitor used against human immunodeficiency virus (HIV). Lopinavir competitively inhibits the HIV-1 protease, an enzyme that mediates the cleavage of Gag, Gag-Pol and Nef precursor polypeptides into their mature proteins, including protease, reverse transcriptase, and integrase. Inhibition of HIV-1 protease prevents cleavage of the viral polyprotein precursor and results in the release of immature, noninfectious virions.

Brand name for ciclopirox olamine lotion

Brand name for allopurinol sodium

A piperidine histamine H1-receptor antagonist with anti-allergic properties and without sedative effects. Loratadine blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial smooth muscle, and gastrointestinal smooth muscle, including vasodilatation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscle. Loratadine does not cross the blood-brain barrier and does not cause central nervous system effects.

A benzodiazepine with anxiolytic, anti-anxiety, anticonvulsant, anti-emetic and sedative properties. Lorazepam enhances the effect of the inhibitory neurotransmitter gamma-aminobutyric acid on the GABA receptors by binding to a site that is distinct from the GABA binding site in the central nervous system. This leads to an increase in chloride channel opening events, a facilitation of chloride ion conductance, membrane hyperpolarization, and eventually inhibition of the transmission of nerve signals, thereby decreasing nervous excitation.

Brand name for lorlatinib

Brand name for hydrocodone/acetaminophen

An orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. Upon administration, lorlatinib binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, lorlatinib is able to cross the blood brain barrier. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.

An immunoconjugate of a humanized murine monoclonal antibody (huN-901) and DMI, a semi-synthetic derivative of the plant-derived ansa macrolide maytansine. The antibody moiety of lorvotuzumab mertansine selectively attaches to CD56 antigen, a neural cell adhesion molecule (NCAM)) expressed on the surface of cells of small cell lung cancer (SCLC) and other neuroendocrine (NE) tumors. Thus, the DMI conjugate is targeted specifically to CD56-expressing tumor cells, where it inhibits tubulin polymerization and assembly, resulting in inhibition of mitosis and cell cycle arrest in the S phase.

The potassium salt of losartan, a non-peptide angiotensin II receptor antagonist with antihypertensive activity. Losartan selectively and competitively binds to the angiotensin II receptor (type AT1) and blocks the binding of angiotensin II to the receptor, thus promoting vasodilatation and counteracting the effects of aldosterone. Converted from angiotensin I by angiotensin-converting enzyme (ACE), angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, decreasing sodium excretion and increasing potassium excretion, and acts as a vasoconstrictor in vascular smooth muscle.

Brand name for benazepril hydrochloride

Brand name for clotrimazole

A lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering and potential antineoplastic activities. Lovastatin is hydrolyzed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in cholesterol biosynthesis. In addition, this agent may induce tumor cell apoptosis and inhibit tumor cell invasiveness, possibly by inhibiting protein farnesylation and protein geranylgeranylation, and may arrest cells in the G1 phase of the cell cycle. The latter effect sensitizes tumor cells to the cytotoxic effects of ionizing radiation.

Brand name for live-attenuated Listeria monocytogenes cancer vaccine ADXS11-001

Brand name for omega-3-acid ethyl esters

Brand name for enoxaparin sodium

Brand name for itraconazole

A peptide-drug conjugate containing the taxane paclitaxel covalently linked to the proprietary 19 amino acid peptide angiopep-2, in a 3:1 ratio, with potential antineoplastic activity. Upon administration, LRP-1-targeted peptide-drug conjugate GRN1005, via angiopep-2 moiety, binds to LRP-1 (low density lipoprotein receptor-related protein 1), which is highly expressed in blood brain barrier (BBB) and glioma cells. This binding allows the transcytosis of the agent across the BBB and the delivery of the cytotoxic agent paclitaxel. Compared to paclitaxel alone, GRN1005 is able to increase the concentration of paclitaxel in the brain and is also able to specifically deliver paclitaxel to LRP-1-overexpressing tumor cells, both in the brain and in the periphery.

An orally available inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, CC-90011 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family that is overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.

An orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, GSK2879552 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the dimethylated form of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.

An orally-available, irreversible inhibitor of lysine-specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, IMG-7289 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; thus, inhibition of LSD1 also promotes H3K9 methylation and decreases transcription of these genes. Altogether, this may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family is overexpressed in certain tumor cells and plays a key role in the regulation of gene expression, tumor cell growth and survival.

An orally available inhibitor of lysine-specific histone demethylase 1 (KDM1A; LSD1), with potential antineoplastic activity. Upon administration, RO7051790 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9, which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in the regulation of gene expression, tumor cell growth and survival.

A bicyclic fatty acid derived from prostaglandin E1 and a chloride channel activator with laxative activity. Upon intake, lubiprostone specifically binds to and activates the type 2 chloride channel (ClC-2) in the apical membrane of the gastrointestinal epithelium. This produces an efflux of chloride ions, thereby drawing water into the gastrointestinal lumen. The resulting increased amounts of intestinal fluid soften the stool, increase motility, and improve bowel movements.

Brand name for belagenpumatucel-L

An orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APEX1 or APE1), with anti-schistosomal and potential antineoplastic activity. Lucanthone intercalates DNA and interferes with the activity of topoisomerases I and II during replication and transcription, thereby inhibiting the synthesis of macromolecules. In addition, this agent specifically inhibits the endonuclease activity of APE1, without affecting its redox activity, resulting in unrepaired DNA strand breaks which may induce apoptosis. Therefore, lucanthone may sensitize tumor cells to radiation and chemotherapy. Furthermore, lucanthone inhibits autophagy through the disruption of lysosomal function. The multifunctional nuclease APE1 is a key component for DNA repair; its expression is often correlated with tumor cell resistance to radio- and chemotherapy.

A monoclonal antibody directed against the B-cell surface antigen CD40 with potential antineoplastic activity. Lucatumumab binds to and inhibits CD40, thereby inhibiting CD40 ligand-induced cell proliferation and triggering cell lysis via antibody-dependent cellular cytotoxicity (ADCC) in cells overexpressing CD40. CD40, an integral membrane protein found on the surface of B lymphocytes, is a member of the tumor necrosis factor receptor superfamily and is highly expressed in a number of B-cell malignancies.

Brand name for ranibizumab

A novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. Lucitanib inhibits VEGFR-1, -2, -3 and FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.

Brand name for therapeutic progesterone

A solution composed of iodine and potassium iodide, which can be used as a reagent and antiseptic, with potential use in cancer diagnosis. The iodine in Lugol’s solution selectively binds to alpha-1,4 glucans found in polysaccharides, such as glycogen. Lugol’s solution reacts with glycogen in normal, healthy non-keratinized, squamous epithelium and the iodine-glucan complex stains the glycogen-containing cells dark brown. Cancer cells are devoid of glycogen, so these cells will stay unstained. The presence of cancer cells can be detected by the degree of staining and the neoplastic cells can be surgically removed. High-grade intraepitheial neoplasia has almost no glycogen-containing epithelium.

Brand name for ferumoxsil oral suspension

Brand name for beta carotene

Brand name for moxetumomab pasudotox-tdfk

Brand name for eszopiclone

A tumor-associated antigen derived from the cell surface antigen of lung cancer cells. Lung tumor-associated antigen could be used as a diagnostic marker or as a form of immunotherapy targeted against lung cancer cells.

A proprietary, lung-targeted, site specific immunomodulator (SSI), with potential immunostimulating and antineoplastic activities. Although the exact type and composition of the lung-targeted immunomodulator QBKPN has yet to be fully disclosed, upon subcutaneous administration, this agent is able to activate a local innate immune response in the lung tissue. This results in an increased number of M1 macrophages, which induces a shift from M2 to M1 macrophage dominance in the tumor microenvironment, and stimulates the recruitment of other immune cells. The M1 macrophages exert antitumor activity and eradicate lung cancer cells through phagocytosis. QBKPN does not induce a systemic immune response or affect other organs or tissues. Altogether, this SSI may decrease tumor cell growth in the lungs. SSIs contain specific, inactivated components of pathogens, such as bacteria and/or viruses, which normally cause an acute infection in the specific organ or tissue of interest.

Brand name for leuprolide acetate

Brand name for leuprolide acetate

A synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. Lurbinectedin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.

A semisynthetic analogue of camptothecin with antineoplastic activity. Lurtotecan selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA replication, double strand DNA breakage and triggering of apoptosis. Independent from DNA replication inhibition, lurtotecan also inhibits RNA synthesis, multi-ubiquitination and degradation of topoisomerase I and chromatin reorganization.

A soluble, recombinant fusion protein composed of a modified form of the extracellular domain of human activin receptor type IIb (ActRIIb) and linked to the human IgG1 Fc domain, with red blood cell stimulating activity. Upon subcutaneous administration, luspatercept inhibits several ligands in the transforming growth factor (TGF)-beta superfamily. This prevents activation of a variety of TGF-beta superfamily members involved in late stage erythropoiesis and results in an increased differentiation and proliferation of erythroid progenitors. Luspatercept acts at a different, later stage than erythropoietin. This agent ultimately enhances red blood cell production and prevents anemia.

Brand name for lutetium Lu 177-dotatate

Brand name for therapeutic progesterone

A naturally-occurring flavonoid, with potential anti-oxidant, anti-inflammatory, apoptosis-inducing and chemopreventive activities. Upon administration, luteolin scavenges free radicals, protects cells from reactive oxygen species (ROS)-induced damage and induces direct cell cycle arrest and apoptosis in tumor cells. This inhibits tumor cell proliferation and suppresses metastasis.

A radioimmunoconjugate comprised of a human monoclonal antibody (huMAb-5B1) against the carbohydrate antigen sialyl Lewis A (carbohydrate antigen 19-9; CA19-9) that is conjugated to the chelator 2-(p-isothiocyanatobenzyl)-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-A-DTPA) and labeled with the beta-emitting radioisotope lutetium Lu 177 (Lu 177), with radioisotopic activity and potential use as an antineoplastic radiotherapeutic and an imaging agent in both planar imaging and single-photon emission computed tomography (SPECT). The antibody moiety of Lu 177 anti-CA19-9 monoclonal antibody 5B1 targets and binds to CA19-9-expressing tumor cells. This may promote killing of CA19-9-expressing tumor cells through the local induction of both complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). Additionally, upon binding and internalization, the Lu 177 moiety can deliver a cytotoxic dose of beta radiation to the CA19-9-expressing tumor cells. Furthermore, the radioisotope moiety may be imaged using planar imaging and SPECT, thus allowing evaluation of the pharmacokinetic profile of the agent, and the imaging and quantification of CA19-9-expressing tumor cells, respectively. CA19-9, a Lewis-type carbohydrate antigen overexpressed on a number of different tumor cell types, plays a key role in tumor cell survival and metastasis.

A radioconjugate of biotin conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with the beta-emitting isotope lutetium Lu 177 (Lu-177) that can be used for radioimmunotherapeutic purposes. Lutetium Lu 177 DOTA-biotin could be used in pre-targeting radioimmunotherapy, which pretreats the lesion with oxidized avidin that binds to protein amino groups on cells. As avidin binds to biotin, the radioisotope can be selectively delivered to cancer cells leading to tumor cell eradication.

A radioconjucate consisting of CTT1403, a phosphoramidate-based irreversible inhibitor of human prostate-specific membrane antigen with an albumin binding moiety, connected via click chemistry to lutetium Lu 177-dodecanetetraacetic acid-azide (177Lu-DOTA-N3), with potential antineoplastic activity. Upon administration, lutetium Lu 177-DOTA-N3-CTT1403 targets and binds to PSMA expressed on tumor cells via its CTT1403 moiety, and upon internalization, delivers cytotoxic beta radiation directly to PSMA-expressing tumor cells. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on most prostate tumor cells. The albumin binding motif extends circulation half-life thereby improving tumor cell uptake of the radioconjugate.

A radioimmunoconjugate, which consists of a monoclonal antibody against the cell-surface antigen CD37 covalently linked, via the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. The antibody moiety of lutetium Lu 177 DOTA-tetulomab binds to CD37 on tumor B-cells. Upon internalization, the radioisotope moiety delivers a cytotoxic dose of beta radiation to CD37-expressing tumor cells. CD37, a transmembrane glycoprotein, is overexpressed in B-cell malignancies.

A radioimmunoconjugate consisting of a humanized monoclonal antibody directed against the extracellular domain of prostate-specific membrane antigen linked to a beta-emitting radioisotope (lutetium-177). This radioimmunoconjugate binds to tumor cells that express the extracellular domain of prostate-specific membrane antigen, delivering beta particle radiation selectively to tumor cells expressing this antigen and so limiting the exposure of normal tissues to ionizing radiation.

A radioconjugate composed of PP-F11N, a gastrin analog, conjugated to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and potential use as an imaging agent for scintigraphy. Following intravenous administration, the PP-F11N moiety binds to the cholecystokinin-2 (CCK-2) receptor. Subsequently, the CCK-2 receptor-expressing tumor cells can be visualized scintigraphically. In addition, the radioisotope moiety delivers a cytotoxic dose of beta radiation to CCK-2 receptor-expressing tumor cells. CCK-2 receptors are expressed on a variety of tumor cell types.

A radioconjugate consisting of the somatostatin antagonistic peptide satoreotide tetraxetan (JR11) that is linked, via the chelating agent dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and imaging activity during positron emission tomography/computed tomography (PET/CT). Upon administration, lutetium Lu 177-DOTA-JR11 binds to somatostatin receptors (SSTRs), with high affinity for SSTR2, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most normal tissues express low levels of SSTRs.

A radioimmunoconjugate consisting of capromab linked to lutetium Lu 177 via the bifunctional macrocyclic chelator methoxy-tetraazacyclododecane-tetraacetic acid (MeO-DOTA) with potential antineoplastic activity. Lutetium Lu 177-capromab binds to human prostate specific membrane antigen (PSMA) expressed on tumor cell surfaces via its capromab moiety and, upon internalization, delivers cytotoxic beta radiation directly to PSMA-expressing tumor cells. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells.

A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide lutetium (Lu) 177. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered Lu-177-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; Lu-177 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically.

A radioconjugate consisting of Evans blue (EB) modified, tyrosine-containing somatostatin analog, Tyr3-octreotate (TATE), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecane tetraacetic acid (DOTA), and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging and antineoplastic activities. Upon intravenous administration, Lutetium Lu 177-DOTA-EB-TATE binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTRs (SSTR2s), present on the cell membranes of many neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR2-positive cells. The incorporation of an albumin-binding moiety through EB modification allows Lutetium Lu 177-DOTA-EB-TATE to reversibly bind to endogenous albumin, potentially extending half-life and increasing targeted accumulation of the drug in tumors. SSTRs, especially SSTR2s, are expressed at relatively higher levels in many tumor cell types and tumor blood vessels, compared to normal tissues.

A radioconjugate consisting of the neurotensin receptor type 1 (NTR1) antagonist, IPN01087 (3BP-227), that is linked, via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and imaging activity during positron emission tomography/computed tomography (PET/CT). Upon administration, lutetium Lu 177-DOTA-IPN01087 binds to NTR1 expressed on certain tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to NTR1-expressing cells. NTR1, a G-protein coupled receptor, is highly expressed in ductal pancreatic adenocarcinoma but not in normal pancreatic tissue.

A radioconjugate consisting of the somatostatin analog octreotate labeled with lutetium Lu 177 with receptor ligand, beta-emitting radioisotope, and potential antineoplastic activities. Lutetium Lu 177-DOTA-octreotate binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Lutetium Lu 177-DOTA-octreotate is produced by substituting the natural amino acid Thr for the alcohol Thr(ol) at the C terminus of the somatostatin analog octreotide and chelating the octreotate to Lu 177 via dodecanetetraacetic acid (DOTA).

A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177 with potential antineoplastic activities. Lutetium Lu 177 dotatate binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs.

A radioconjugate consisting of the somatostatin analogue edotreotide labeled with lutetium Lu 177 with potential antineoplastic activities. Lutetium Lu 177-edotreotide binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelated by the bifunctional, macrocyclic chelating agent dodecanetetraacetic acid (DOTA).

A radioconjugate consisting of the gastrin-releasing peptide receptor (GRPR) antagonist, NeoB, linked via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration, lutetium Lu 177 NeoB targets and binds to GRPRs present on certain tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to GRPR-expressing cells. GRPR, also known as bombesin receptor subtype 2, is a G protein-coupled receptor that is overexpressed in some cancer types.

A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of 177Lu-PSMA-617, the PSMA-617 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.

A radioimmunoconjugate consisting of the chimeric monoclonal antibody cG250 linked to the low energy beta-emitting radioisotope Lutetium 177, via the bifunctional macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), with potential antineoplastic activity. The antibody moiety of lutetium Lu-177 girentuximab binds to renal cell carcinoma (RCC) cells expressing the RCC-associated antigen G250; a cytotoxic dose of beta radiation is selectively delivered to G250-expressing RCC cells upon internalization of the radioimmunoconjugate.

A radioconjugate composed of PSMA-R2, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of 177Lu-PSMA-R2, the PSMA-R2 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on the majority of prostate tumor cells.

Brand name for motexafin lutetium

Brand name for motexafin lutetium

Brand name for fluvoxamine maleate

A whole-cell cancer vaccine, containing human acute myeloid leukemic (AML) blasts that have been genetically engineered to express a B7.1/IIL-2 fusion protein encoded by a self-inactivating lentiviral vector (LV), with potential antineoplastic and immunomodulating activities. Upon administration, LV.IL-2/B7.1-transduced AML blast vaccine may stimulate a host cytotoxic T lymphocyte (CTL) response against AML cells. The single fusion protein encoded by the LV is postsynthetically cleaved to produce biologically active membrane-anchored B7.1 and secreted IL-2 in AML blasts; combined expression of IL-2 and the co-stimulatory molecule B7.1 by AML blasts may increase stimulation of both allogeneic and autologous cytotoxic T cells.

A multipeptide vaccine consisting of peptides derived from lymphocyte antigen 6 complex locus K (LY6K) and type I and II vascular endothelial growth factor receptors (VEGFRs) with potential antineoplastic activity. Upon administration, LY6K/VEGFR1/VEGFR2 multipeptide vaccine may elicit an antitumor cytotoxic T-lymphocyte (CTL) immune response against LY6K-expressing tumor cells and/or VEGFR-expressing vascular endothelial cells involved in tumor angiogenesis. LY6K is a tumor-associated antigen (TAA) that occurs singly in glycosylphosphatidyl-inositol (GPI)-linked cell-surface glycoproteins or as three-fold repeated domain in the urokinase-type plasminogen activator receptor; VEGFRs are cell surface receptors that stimulate endothelial cell proliferation, invasion, angiogenesis, and vasculogenesis upon ligand binding and receptor activation.

Brand name for lycopene

A linear, unsaturated hydrocarbon carotenoid, the major red pigment in fruits such as tomatoes, pink grapefruit, apricots, red oranges, watermelon, rosehips, and guava. As a class, carotenoids are pigment compounds found in photosynthetic organisms (plants, algae, and some types of fungus), and are chemically characterized by a large polyene chain containing 35-40 carbon atoms; some carotenoid polyene chains are terminated by two 6-carbon rings. In animals, carotenoids such as lycopene may possess antioxidant properties which may retard ageing and many degenerative diseases. As an essential nutrient, lycopene is required in the animal diet.

Brand name for isosulfan blue

Brand name for epratuzumab

Killer cell lymphocytes activated in the presence of interleukin-2 (IL-2). Lymphokine-activated killer cells (LAKs) are cytotoxic effector cells with an exceptionally wide target cell spectrum including normal and malignant cells of different origins. LAK cells exhibit a profound heterogeneity with regard to phenotype surface marker expression; it remains to be determined if they represent a unique cell lineage.

A population of autologous cytotoxic T lymphocytes (CTLs) with potential immunomodulating and antitumor activities. White blood cells are grown ex-vivo and are exposed to dendritic cells (DCs) loaded with lymphoma tumor associated antigens (TAAs); the TAA-specific CTLs are further expanded ex-vivo before being introduced into the patient. Upon infusion with TAA-specific CTLs, these CTLs may help activate tumor-specific CTL responses in the patient, thereby specifically killing TAA-expressing cancer cells and eventually inhibiting tumor cell proliferation.

Brand name for technetium Tc 99m-labeled tilmanocept

Brand name for belimumab

Brand name for olaparib

A lozenge containing lyophilized black raspberry with potential antioxidant, pro-apoptotic and chemopreventive activities. In addition to vitamins, minerals, and phytosterols, black raspberries are rich in flavonols. Of the flavonols present in this agent, the anthocyanins appear to contribute significantly to this agent’s chemopreventive effects by inhibiting the activation of several signal transduction pathways, including the mitogen-activated protein kinase-mediated pathways, and certain transcription factors, such as nuclear factor kappa B (NF-kB), activator protein-1 (AP-1) complex, and nuclear factor in activated T-cells (NFAT). This in turn modulates the expression of downstream target genes that are upregulated in a variety of cancer cell types, including inducible nitric oxide synthase, cyclooxygenase-2, vascular endothelial growth factor and the anti-apoptotic protein survivin.

A saliva substitute (or artificial saliva) containing lyophilized black raspberry with potential antioxidant, pro-apoptotic and chemopreventive activities. In addition to vitamins, minerals and phytosterols, black raspberries are rich in flavonols of which the anthocyanins appear to contribute significantly to this agent’s chemopreventive effects. Anthocyanins inhibit the activation of several signal transduction pathways, including the mitogen-activated protein kinase-mediated pathways, and certain transcription factors, such as nuclear factor kappa B (NF-kB), activator protein-1 (AP-1) complex, and nuclear factor in activated T-cells (NFAT). This in turn modulates the expression of downstream target genes that are upregulated in a variety of cancer cell types, including inducible nitric oxide synthase, cyclooxygenase-2, vascular endothelial growth factor and the anti-apoptotic protein survivin.

Brand name for pregabalin

An orally available inhibitor of lysine-specific demethylase 1 (LSD1; lysine-specific histone demethylase 1A; KDM1A), with potential antineoplastic activity. Upon administration, INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. Altogether, this may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in the regulation of gene expression and in tumor cell growth and survival.

Brand name for mitotane

A temperature-sensitive liposomal formulation of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Upon intravenous administration, circulating thermosensitive liposomes are activated locally by increasing the tumor temperature to 40-41 degrees Celsius using an external heat source. The elevated temperature causes compositional changes in the liposomes, creating openings that allow for the release of encapsulated doxorubicin. Compared to non-thermosensitive liposomes, lyso-thermosensitive liposomes deliver higher concentrations of a cytotoxic agent to a heat-treated tumor site while sparing normal tissues unexposed to heat treatment.

 

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