Dictionary of drugs: M1
Dictionary of pharmaceutical drugs/medications sorted alphabetically
- A page 1 | A page 2 | A page 3
- C | C1 | C2
- M | M page 2
- S | page 2
- 0 - 9
A formulation composed of dissolvable small, adhesive-like patches composed of a biocompatible material which is coated with the anthracycline antibiotic doxorubicin, with potential antineoplastic and immunomodulating activities. Upon cutaneous administration of the microneedle-array-doxorubicin, the microneedles degrade once inserted into the skin and doxorubicin is released from the dissolvable microneedle array delivery device directly into the tumor microenvironment (TME). Doxorubicin is taken up by tumor cells and intercalates into DNA and interferes with topoisomerase II activity. This inhibits DNA replication and RNA synthesis, leading to tumor cell growth inhibition and apoptosis. This agent also interacts with cell membrane lipids causing lipid peroxidation. In addition, doxorubicin induces innate, adaptive, and tumor-specific effector and memory immune responses, thereby further killing the tumor cells. Delivery of doxorubicin using the microneedle array delivery system allows direct and specific administration of doxorubicin to the TME which may improve drug concentration into tumor cells and may reduce systemic toxicity, compared to the administration of systemic doxorubicin alone.
Brand name for ethinyl estradiol/levonorgestrel
Brand name for glyburide
An micronutrient-fortified fermented dairy product with potential positive immunomodulatory activity. Micronutrient-fortified probiotic yogurt contains various micronutrients in addition to beneficial microorganisms, such as strains of Lactobacillus. Probiotic Lactobacillus strains have been shown to protect against gastrointestinal and urogenital infections, to moderate diarrheal episodes, and to increase CD4 T-lymphocyte counts. In immunocompromised subjects, micronutrient supplementation may also increase CD4 T-lymphocyte counts.
An aroylindole derivative and tubulin polymerization inhibitor, with potential tubulin-inhibiting, vascular-disrupting and antineoplastic activities. Upon administration, tubulin polymerization inhibitor SCB01A binds at the colchicine binding site of tubulin and prevents its polymerization in tumor blood vessel endothelial cells and in tumor cells. This blocks the formation of the mitotic spindle and leads to both cell cycle arrest at the G2/M phase and tumor cell apoptosis. Also, this agent's effect on the tumor blood vessel endothelial cells leads to a disruption of the tumor vasculature and tumor blood flow, which deprives tumor cells of nutrients and induces tumor cell apoptosis.
An orally available, highly water-soluble lysine prodrug of the synthetic small molecule BAL27862 with potential antitumor activity. Upon administration of BAL101553 and conversion into the active form BAL27862, this agent binds to tubulin at a site distinct from the vinca-alkaloid-binding site, and prevents tubulin polymerization and destabilizes microtubules, ultimately leading to cell cycle arrest, blockage of cell division and an induction of cell death in cancer cells.
The hydrochloride salt of a short-acting benzodiazepine derivative with an imidazole structure and anxiolytic, amnestic, hypnotic, anticonvulsant and sedative properties. Midazolam binds to the benzodiazepine receptor at the gamma-aminobutyric acid (GABA) receptor-chloride ionophore complex in the central nervous system (CNS), resulting in increases in the opening of chloride channels, membrane hyperpolarization, and the inhibitory effect of GABA. This agent may also interfere with the reuptake of GABA, thereby causing accumulation of GABA in the synaptic cleft.
An oromucosal solution containing the maleate salt form of midazolam, a short-acting benzodiazepine derivative, with anxiolytic, hypnotic, anticonvulsant and sedative activities. Upon administration of the solution into the buccal cavity, midazolam exerts its effect by binding to the benzodiazepine receptor at the gamma-aminobutyric acid (GABA) receptor-chloride ionophore complex in the central nervous system (CNS). This leads to an increase in the permeability of chloride channels, membrane hyperpolarization and enhances the inhibitory effect of GABA in the CNS. Midazolam may also interfere with the reuptake of GABA, thereby causing accumulation of GABA in the synaptic cleft. The oromucosal formulation facilitates administration to patients that are unable to swallow. The ethanol in this formulation improves the buccal absorption of midazolam.
A synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.
A liposomal formulation containing a muramyl dipeptide (MDP) analogue with potential immunomodulatory and antineoplastic activities.. Muramyl tripeptide phosphatidylethanolamine (MTP-PE), a derivative of the mycobacterial cell wall component MDP, activates both monocytes and macrophages. Activated macrophages secrete cytokines and induce the recruitment and activation of other immune cells, which may result in indirect tumoricidal effects. Liposomal encapsulation of MTP-PE prolongs its half-life and enhances tissue targeting.
Brand name for mifepristone
A derivative of the synthetic progestin norethindrone with antiprogesterone activity. Mifepristone competitively binds to the progesterone receptor, resulting in inhibition of the effects of endogenous or exogenous progesterone. This agent also exhibits antiglucocorticoid and weak antiandrogenic activities.
A desoxynojirimycin derivative and inhibitor of alpha-glucosidase with antihyperglycemic activity. Miglitol binds to and inhibits alpha-glucosidase, an enteric enzyme found in the brush border of the small intestines that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents the breakdown of larger carbohydrates into glucose and decreases the rise in postprandial blood glucose levels. Compared to acarbose, miglitol is systemically absorbed.
A dendritic cell (DC)-based vaccine composed of program death ligands 1 and 2 (PDL1/L2)-silenced DCs and loaded with the recipient’s minor histocompatibility antigens (MiHA), with potential use for graft-versus-tumor (GVT) induction following allogeneic stem cell transplantation (allo-SCT). Donor DCs are electroporated ex vivo with MiHA mRNA and small interfering RNAs (siRNAs) designed to silence the expression of PD L1/L2. After allo-SCT and upon intravenous administration of the MiHA-loaded PD-L1/L2-silenced DC vaccine, the DCs induce the expansion and activation of MiHA-specific CD8-positive T-cells. These tumor antigen-reactive T-cells exert their GVT effect by killing MiHA-positive tumor cells. PD-L1/L2, co-inhibitory ligands expressed on DCs, play key roles in preventing MiHA-specific CD8-positive T-cell expansion; silencing enhances MiHA-specific CD8-positive T-cell expansion and activity and improves the GVT effect. The MiHA are human leukocyte antigen (HLA)-bound peptides and are exclusively expressed by the recipient’s hematopoietic tumor cells.
An orally available MDM2 (murine double minute 2) antagonist with potential antineoplastic activity. Upon oral administration, milademetan tosylate binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger protein and a negative regulator of the p53 pathway, is overexpressed in cancer cells; it has been implicated in cancer cell proliferation and survival.
A humanized monoclonal antibody directed against human CD74 with potential antineoplastic activity. Milatuzumab specifically binds to CD74 on CD74-positive cells. Although the exact mechanism through which this agent induces apoptosis is unknown, it may involve antibody-dependent cellular cytotoxicity (ADCC) or complement-mediated cytotoxicity (CMC). Alternatively, as CD74 is the cellular receptor for the cytokine migration-inhibitory factor (MIF), the cytotoxicity of this agent may be related to inhibition of CD74 activation by MIF. CD74, an integral membrane protein that functions as an MHC class II chaperone, may also be an accessory-signaling molecule; activation of CD74 may initiate cell survival mechanisms involving induction of a signaling cascade resulting in NFkB activation, entry of stimulated cells into the S phase of the cell cycle, elevation of DNA synthesis, cell division, and augmented expression of Bcl-xL.
An immunoconjugate consisting of milatuzumab, a humanized monoclonal antibody against CD74, conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. The milatuzumab moiety of this antibody-drug conjugate (ADC) selectively binds to CD74 on tumor cell surfaces; upon internalization, the doxorubicin moiety is released, where it intercalates between base pairs in the DNA helix and inhibits topoisomerase II, thereby preventing DNA replication and increasing double-strand breakage. As a result, this agent may inhibit the proliferation of cancer cells that overexpress CD74. CD74, an integral membrane protein and tumor associated antigen (TAA), is overexpressed in certain cancer cells and promotes survival in rapidly proliferating tumor cells.
An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. Milciclib maleate potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types. The neurotrophin receptor TRKA is mutated in a variety of cancer cell types.
Brand name for diethylstilbestrol
Brand name for magnesium hydroxide
An oral milk protein-based nutritional supplement. Milk protein-based energy drink is a flavored liquid that consists of milk protein, rapeseed and sunflower oils, carbohydrates, vitamins, minerals and trace-elements, providing 1.5kcal and 10 mg of protein per ml.
A substance derived from any of several Old World coarse prickly-leaved shrubs and subshrubs including the plant Silybum marianum. Milk thistle's active chemical component is silymarin, which is a combination of flavonoids such as silibinin, dehydrosilibinin, silychristin and silydianin. These compounds are antioxidants and may alter the membrane structure of the liver cell, thereby blocking the absorption of toxins; they may also stimulate the production of new liver cells. In addition, milk thistle may increase cellular adenosine triphosphate (ATP) levels, exhibiting dose-dependent cardiac myocyte cytoprotection against doxorubicin. The silibinin component of milk thistle has been shown to inhibit growth factor receptor-mediated mitogenic and cell survival signaling, thereby inhibiting tumor growth. (NCI04)
A nutritional supplement composed of a milled seed mixture, including milled flax, sesame and pumpkin seeds, in sour milk, with potential anti-inflammatory and lipid-regulating activities. The seeds contain high levels of fatty acids, including omega-3 and omega-6 polyunsaturated fatty acids (PUFAs), such as dihomo-gamma-linolenic acid (DGLA), alpha-linolenic acid (ALA), eicosapentaenoic acid (EPA), docosapentaenoic acid (DPA), and docosahexaenoic acid (DHA). Upon administration of the milled seed mix, the intake of PUFAs improves PUFA levels and may favorably change the n-6/n-3 PUFA ratio, decrease triglyceride (TG) levels, and improve body weight. In addition, the active ingredients in the milled seed mix may change the expression of inflammatory markers, such as C-reactive protein (CRP) and pro-inflammatory cytokines, including interleukin-6 (IL-6) and tumor necrosis factor alpha (TNF-a), thereby decreasing inflammation. The milled seed mix may also prevent oxidative stress and affect glycemic control. Tumors cause inflammatory states and unfavorably affect lipid and fatty acid metabolism.
A recombinant fusion protein derived from the coding sequences of two growth factors, interleukin-3 (IL-3) and granulocyte-macrophage colony-stimulating factor (GM-CSF). Milodistim exhibits greater receptor binding affinity and colony stimulating activity than its parent cytokines. This agent stimulates proliferation of immature hematopoietic cells and allows the stimulation and expansion of multi-lineage hematopoiesis from immature bone marrow progenitor cells.
An orally- and topically-active alkyl-phosphocholine compound with potential antineoplastic activity. Miltefosine targets cellular membranes, modulating cell membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. As an immunomodulator, miltefosine stimulates T-cells, macrophages and the expression of interleukin 3 (IL-3), granulocyte-macrophage colony stimulating factor (GM-CSF), and interferon gamma (INF-gamma).
A peptide-based vaccine containing a carbohydrate mimetic peptide (CMP) P10s fused to the pan HLA DR-binding epitope (PADRE) peptide, with immunomoadjuvant activity and potential antineoplastic activity. Upon injection of the mimotope-P10s-PADRE peptide vaccine, the P10s peptide, which mimics gangliosides and other tumor-associated carbohydrate antigens (TACA), both stimulates a cytotoxic T-lymphocyte (CTL) response towards cells expressing TACAs and induces the production of antibodies that are reactive with a broad set of TACAs. Additionally, the anti-TACA antibodies may interfere with cellular pathways involved in tumor cell survival and may induce antibody-dependent cellular cytotoxicity (ADCC) toward cells expressing TACAs. PADRE is a helper T-cell epitope that is able to increase the magnitude and duration of the CTL response.
Brand name for triptolide analogue
Brand name for minocycline hydrochloride
The hydrochloride salt of minocycline, a broad spectrum long-acting derivative of the antibiotic tetracycline, with antibacterial and anti-inflammatory activities. Minocycline binds to the bacterial 30S ribosomal subunit and interferes with the binding of tRNA to the ribosomal complex, thereby inhibiting protein translation in bacteria. In addition, minocycline inhibits the inflammatory enzyme 5-lipoxygenase (5LOX) and may impede T cell-microglia interactions; both activities may contribute to minocycline's neuroprotective effects. 5LOX catalyzes the synthesis of inflammatory mediators such as prostaglandins and leukotrienes.
A combination preparation containing the broad-spectrum, semi-synthetic tetracycline antibiotic minocycline and the chelator ethylenediaminetetraacetate (EDTA) with antimicrobial and antibiofilm activities. Minocycline exhibits bacteriostatic activity by binding to the bacterial 30S ribosomal subunit and preventing binding of aminoacyl-tRNA to the mRNA-ribosome complex during protein translation; this results in an inhibition of bacterial protein synthesis and, consequently, an inhibition of bacterial cell growth. EDTA may cause the dispersal and killing of biofilms by chelating metal ions important to the stabilization of biofilm structure. The two agents in this combination may act synergistically to eradicate bacteria embedded in biofilms.
Brand name for thiabendazole
A soluble, thapsigargin prodrug containing the cytotoxic analog of thapsigargin, 8-O-(12Aminododecanoyl)-8-O debutanoylthapsigargin (12-ADT) linked, via a carboxyl group, to the targeting peptide containing aspartic acid with potential antineoplastic activity. Upon intravenous administration, the non-toxic prodrug targets prostate specific membrane antigen (PSMA), a type II membrane carboxypeptidase, which is overexpressed in prostate cancer cells and in the neovasculature of most solid tumors but not in normal blood vessels. Mipsagargin is subsequently converted, through hydrolysis, into the active cytotoxic analog of thapsigargin 12-ADT-Asp. 12-ADT binds to and blocks the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump, thereby increasing the concentration of cytosolic calcium which leads to an induction of apoptosis. By preventing nutrient supply to tumor cells, mipsagargin may be able to inhibit tumor growth. Compared to thapsigargin alone, mipsagargin is able to achieve higher concentrations of the active agents at the tumor site while avoiding systemic toxicity.
An orally bioavailable agonist of the human beta-3 adrenergic receptor (ADRB3), with muscle relaxing, neuroprotective and potential antineoplastic activities. Upon oral administration, mirabegron binds to and activates ADRB3, which leads to smooth muscle relaxation. Mirabegron also restores sympathetic stimulation in mesenchymal stem cell (MSC) niches, inhibits JAK2-mutated hematopoietic stem cell (HSC) expansion and blocks the progression of myeloproliferative neoplasms (MPNs). Lack of sympathetic stimulation of the MSC and HSC niches is associated with the development of MPNs.
Brand name for Tc 99m sestamibi
Brand name for pramipexole dihydrochloride
A preparation of allogeneic platelets that have been treated with Mirasol, a proprietary pathogen reduction technology (PRT) system, and can potentially be used to improve symptoms associated with thrombocytopenia. Upon apheresis, platelets are treated with the patented PRT system, which includes treatment of the platelets with riboflavin (vitamin B2) and broad-spectrum ultraviolet (UV) light. The treatment causes irreversible changes to the RNA and DNA of a broad range of pathogens, including viruses, bacteria, parasites and white blood cells (WBCs), which prevents them from replicating and causing disease. After ex vivo treatment and upon transfusion, the Mirasol-treated allogeneic platelets may reduce thrombocytopenia and prevent bleeding. By preventing the replication of contaminating pathogens, Mirasol treatment improves transfusion safety. Inactivation of WBCs may reduce transfusion reactions and immunological complications in patients.
Brand name for methoxy polyethylene glycol epoetin beta
Brand name for levonorgestrel-releasing intrauterine system
A small molecule compound that depletes serum amyloid P component (SAP), with potential anti-amyloid activity. Upon injection, miridesap binds to circulating SAP, forming complexes that are rapidly cleared in the liver. SAP bound to amyloid deposits is in equilibrium with plasma SAP, and depletion of the latter should lead to the eventual removal of SAP from amyloid deposits as well. SAP is a universal component of amyloid deposits and contributes to the pathogenesis of amyloidosis.
A synthetic tetracyclic derivative of the piperazino-azepines with antidepressant activity. Although its mechanism of action is unknown, mirtazapine enhances central adrenergic and serotonergic transmission, possibly by acting as an antagonist at central presynaptic alpha 2 adrenergic inhibitory autoreceptors and heteroreceptors. This agent is a potent antagonist of 5-hydroxytryptamine type 2 (5-HT2), 5-HT3, and histamine 1 (H1) receptors, and a moderate anatgonist of peripheral alpha 1 adrenergic and muscarinic receptors.
An immunoconjugate consisting of the humanized monoclonal antibody M9346A against folate receptor 1 (FOLR1) conjugated, via the disulfide-containing cleavable linker sulfo-SPDB, to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. The anti-FOLR1 monoclonal antibody moiety of mirvetuximab soravtansine targets and binds to the cell surface antigen FOLR1. After antibody-antigen interaction and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, thereby inhibiting cell division and cell growth of FOLR1-expressing tumor cells. FOLR1, a member of the folate receptor family is overexpressed on a variety of epithelial-derived cancer cells. The sulfo-SPDB linker prevents cleavage in the bloodstream and may improve this agent’s efficacy in multidrug resistant tumor cells.
A nitroimidazole with radiosensitizing and antineoplastic properties. Exhibiting high electron affinity, misonidazole induces the formation of free radicals and depletes radioprotective thiols, thereby sensitizing hypoxic cells to the cytotoxic effects of ionizing radiation. This single-strand breaks in DNA induced by this agent result in the inhibition of DNA synthesis.
An extract of the whole plant Viscum album (mistletoe) with potential biological response modifier (BRM) activity. Mistletoe extract may both stimulate the antitumoral functions of the immune system and have a direct toxic effect on tumor cells.
Brand name for plicamycin
Brand name for sustained-release mitomycin C hydrogel formulation
A guanylhydrazone with potential antineoplastic activity. Mitoguazone competitively inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. Polyamines, specifically spermine and spermidine, are essential for thymidine kinase production, DNA synthesis, and cell proliferation.
A synthetic derivative of hexitol with antineoplastic and radiosensitizing properties. Mitolactol alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA and RNA synthesis.
A methylazirinopyrroloindoledione antineoplastic antibiotic isolated from the bacterium Streptomyces caespitosus and other Streptomyces bacterial species. Bioreduced mitomycin C generates oxygen radicals, alkylates DNA, and produces interstrand DNA cross-links, thereby inhibiting DNA synthesis. Preferentially toxic to hypoxic cells, mitomycin C also inhibits RNA and protein synthesis at high concentrations.
The tosylate salt form of T-1101, an inhibitor of mitosis, with potential antineoplastic activity. Upon oral administration, T-1101 inhibits mitosis, through an as of yet not elucidated mechanism of action, which leads to decreased tumor cell proliferation.
A pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. Mitosis-angiogenesis inhibitor (MAI) R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta‚ FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis.
A synthetic derivative of the insecticide dichlorodiphenyl trichloroethane (DDT) with anti-adrenocorticoid properties. Following its metabolism in the adrenal cortex to a reactive acyl chloride intermediate, mitotane covalently binds to adrenal proteins, specifically inhibiting adrenal cortical hormone production.
The hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.
The isethionate salt of mivobulin, a synthetic colchicine analogue with potential antineoplastic activity. Mivobulin isethionate binds to tubulin, thereby inhibiting microtubule polymerization and mitosis.
A cancer vaccine containing a mixture of killed bacteria with potential immunostimulatory and antineoplastic activities. Mixed bacteria vaccine (MBV or Coley’s toxins) consists of a pyrogenic bacterial lysate derived from Serratia marcescens and Streptococcus pyogenes; the active components in the lysate may be lipopolysaccharide (LPS), a component of the Gram-negative bacterial cell wall of Serratia, and streptokinase, an enzyme produced by Streptococcus pyogenes. LPS has been shown to stimulate the host humoral immune response and induce the release of various antitumor cytokines such as tumor necrosis factor (TNF) and interleukin-12 (IL-12).
A synthetic small molecule with potential antineoplastic activity. MK0731 selectively inhibits kinesin spindle protein (KSP), which may result in the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and apoptosis in tumor cells that overexpress KSP.
An orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus.
An orally bioavailable inhibitor of mitogen-activated protein kinase interacting serine/threonine-protein kinase 1 (MKNK1), with potential antineoplastic activity. Upon oral administration, MKNK1 inhibitor BAY 1143269 binds to MKNK1, thereby preventing its activation and the downstream MKNK1-mediated phosphorylation and activation of eukaryotic translation initiation factor 4E (eIF4E). As eIF4E enhances the synthesis of oncogenic proteins, preventing eIF4E activity inhibits the synthesis of tumor angiogenic factors and leads to both the inhibition of cellular proliferation and apoptosis in susceptible tumor cells. eIF4E, overexpressed in a variety of cancer cells, plays a key role in tumor cell proliferation and survival.
A fusion protein encoded by the MLL/MLLT1 fusion gene. This protein is comprised of the N-terminal half of the histone-lysine N-methyltransferase MLL protein, including the AT hook DNA binding domain and the DNA methyltransferase domain, fused to almost the entire protein ENL.
An immunoconjugate that consists of a humanized monoclonal antibody (MLN591), directed against prostate-specific membrane antigen linked to a maytansinoid (DM1). The monoclonal antibody moiety of MLN2704 binds to tumor cells expressing prostate-specific membrane antigen; MLN274 is then internalized into the tumor cell where the DM1 maytansinoid moiety binds to tubulin and inhibits tubulin polymerization and microtubule assembly, resulting in a disruption of microtubule activity and cell division, and cell death.
A selective mitogen-activated protein kinase (MAPK)-interacting protein kinase (MNK) types 1/2 inhibitor with potential antineoplastic activity. Upon administration, MNK1/2 inhibitor ETC-1907206 may inhibit MNK1/2-dependent phosphorylation of eukaryotic initiation factor 4E (eIF4E) and interfere with its role in mRNA translation. eIF4E is an oncoprotein that must be phosphorylated before it can promote the proliferation and progression of tumor cells. MNKs are a family of serine/threonine kinases that have been implicated in oncogenic transformation and tumor progression.
A third generation, cationic, lipophilic, manganese (Mn) and porphyrin-based mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with antioxidant and potential chemoprotective activities. Upon administration, MnSOD mimetic BMX-001 is internalized by cells and mimics the activity of MnSOD by scavenging reactive oxygen species (ROS), such as superoxide anion, hydrogen peroxide, and hydroxyl radical. This prevents oxidative damage to macromolecules such as DNA and minimizes oxygen free radical-related chemotoxicity in normal tissues. This agent was designed to be more lipophilic and less toxic than first and second generation Mn-porphyrin mimetics.
A plasmid DNA encoding human manganese superoxide dismutase (MnSOD) and liposomally encapsulated with potential chemoprotective activity. When administered orally and localizing in the esophagus, MnSOD-plasmid liposomes express MnSOD, which scavenges reactive oxygen species (ROS); MnSOD scavenging of ROS may result in a reduction in ROS-mediated lipid peroxidation, apoptosis, and micro-ulceration in the epithelial lining of the esophagus.
Brand name for meloxicam
Brand name for meloxicam
Brand name for meloxicam
Brand name for recombinant flt3 ligand
A rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. Overexpression of Class I HDACs 1, 2 and 3 has been found in many tumors and has been correlated with a poor prognosis.
A synthetic central nervous system stimulant with wakefulness-promoting activity. Modafinil appears to inhibit dopamine reuptake, resulting in an increase in extracellular dopamine. This agent exhibits pronounced wakefulness-promoting activity (without sympathomimetic activity) and may improve cognitive function in certain clinical settings.
Brand name for ethinyl estradiol/norethindrone
A dietary supplement containing the modified citrus pectin (MCP) derived from the soluble fiber of citrus fruit peels and a galectin-3 inhibitor with potential antioxidant, hypocholesterolemic, immunostimulatory, metal chelating, and anti-metastatic activities. MCP is a low molecular weight version of pectin composed of short, slightly-branched carbohydrate chains and is modified for enhanced absorbability. The bioactive fragments, most likely the galactan-containing portion, of pectin binds to galectin-3, a carbohydrate-binding protein involved in imflammation, heart disease and is upregulated on the surface of certain types of tumor cells. Binding of MCP may result in the suppression of cancer cell aggregation, adhesion, proliferation and metastasis. In addition, MCP decreases prostate specific antigen (PSA) levels and may remove heavy metals. Also, unsaturated oligogalacturonic acids in MCP may stimulate the immune system through the activation of natural killer cells, cytotoxic T-cells, and B-cells.
A cancer vaccine consisting of a proprietary, recombinant modified vaccinia Ankara (MVA) viral vector encoding an epitope of human epidermal growth factor receptor 2 (HER2) with potential antineoplastic activity. Upon administration, modified vaccinia Ankara (Bavarian Nordic)-HER2 vaccine may stimulate the host immune system to mount humoral and cytotoxic T lymphocyte responses against HER2-expressing tumor cells, resulting in tumor cell lysis. HER2, also known as ErbB-2, is a tyrosine kinase growth factor receptor and a member of the epidermal growth factor receptor family; it plays a significant role in the pathogenesis of some breast cancers.
A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the wild-type form of the tumor protein p53 (wt p53), with potential immunostimulating and antineoplastic activities. Upon subcutaneous vaccination with MVA vaccine expressing p53, the expressed p53 may stimulate the host immune system to mount a p53-specific cytotoxic T-lymphocyte (CTL) response against tumor cells expressing p53, resulting in tumor cell lysis. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attentuated, replication-defective vaccinia strain and is incapable of virion assembly. The p53 gene, a tumor suppressor gene, is mutated in many cancer cell types.
A modified version of vitamin D binding protein (VDBP; Gc protein) macrophage activator, with potential antineoplastic and anti-angiogenic activities. Upon administration, modified VDBP-macrophage activator EF-022, acting in a similar manner as VDBP-macrophage activating factor (GcMAF), is able to activate tumoricidal macrophages, thereby enhancing the killing and eradication of cancer cells. In addition, EF-022 may inhibit tumor cell proliferation, migration and angiogenesis. VDBP is a glycoprotein and precursor for macrophage activating factor (MAF), which promotes macrophage activation; however VDBP can be deglycosylated by serum alpha-N-acetylgalactosaminidase, which is secreted from cancerous cells, and cannot be converted to MAF. Thus, the macrophage activation cascade is often impaired in tumor cells and plays a key role in tumor immunosuppression. Modification of VDBP stabilizes MAF.
An orally available, modified-release formulation containing the calcitriol prohormone, calcifediol (25-hydroxyvitamin D), which can potentially be used for vitamin D supplementation. Upon oral administration of the modified-release calcifediol capsule, calcifediol is slowly and gradually released in the gastrointestinal tract. Then it is taken up by the body and converted, in the kidneys, to the active form calcitriol (1,25-dihydroxyvitamin D or 1,25 D). This form increases and normalizes vitamin D plasma levels, which, in turn, regulates calcium plasma levels, and normalizes elevated parathyroid hormone (PTH) levels by suppressing both PTH synthesis, and secretion. This formulation appears to have fewer side effects than supplementation with formulations containing active 1,25 D and does not stimulate the upregulation of vitamin D 24-hydroxylase (CYP24), a cytochrome P-450 family enzyme that inactivates vitamin D.
A recombinant immunoglobulin G1 (IgG1) monoclonal antibody directed against the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, modotuximab targets and binds to an epitope located in the extracellular domain (ECD) of EGFR, which causes internalization and degradation of EGFR, including the mutated EGFR variant III (EGFRvIII). This prevents EGFR-mediated signaling, thereby inhibition EGFR-dependent tumor cell proliferation. EGFR, a receptor tyrosine kinase, often is overexpressed on the cell surfaces of various solid tumor cell types.
Brand name for trilostane
Brand name for arfolitixorin
A nanoparticle-based metal-organic framework (MOF) compound composed of proprietary X-ray-absorbing metals, with potential radiosensitizing properties. Upon intratumoral administration and subsequent irradiation of the tumor site, RiMO-301 absorbs the X-ray photons and produces reactive oxygen species (ROS), such as hydroxyl radicals and singlet oxygen, which induces ROS-mediated DNA damage in the irradiated cancer cells leading to tumor cell lysis. In addition, RiMO-301 may also contain an as of yet unidentified immunomodulating agent loaded into the channels/pores of the construct that may induce an immune response against the tumor-associated antigens (TAAs) released by the lysed tumor cells, thereby locally killing additional tumor and non-tumor cells. MOFs, porous crystalline materials composed of metal clusters and organic linkers, generate ROS at much lower X-ray dosages than used in standard radiotherapy, which results in reduced radiation exposure and X-ray damage to normal, healthy cells.
A humanized monoclonal antibody directed against C-C chemokine receptor 4 (CCR4) with potential anti-inflammatory and antineoplastic activities. Mogamulizumab selectively binds to and blocks the activity of CCR4, which may inhibit CCR4-mediated signal transduction pathways and, so, chemokine-mediated cellular migration and proliferation of T cells, and chemokine-mediated angiogenesis. In addition, this agent may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against CCR4-positive T cells. CCR4, a G-coupled-protein receptor for C-C chemokines such MIP-1, RANTES, TARC and MCP-1, is expressed on the surfaces of some types of T cells, endothelial cells, and some types of neurons. CCR4, also known as CD194, may be overexpressed on adult T-cell lymphoma (ATL) and peripheral T-cell lymphoma (PTCL) cells.
A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, molibresib binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.
An element with atomic symbol Mo, atomic number 42, and atomic weight 95.94.
An orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with potential antineoplastic activity. Momelotinib competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types.
The furoate salt form of mometasone, a synthetic topical glucocorticosteroid receptor agonist with anti-inflammatory, anti-pruritic and vasoconstrictive properties. Mometasone furoate exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression. This results in synthesis of certain anti-inflammatory proteins, while inhibiting the synthesis of certain inflammatory mediators.. Specifically, mometasone furoate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from phospholipid membrane by phospholipase A2.
A humanized immunoglobulin G4 (IgG4) monoclonal antibody against the human natural killer (NK) and T-lymphocyte cell checkpoint inhibitor killer cell lectin-like receptor subfamily C member 1 (NKG2A), with potential antineoplastic activity. Upon administration, monalizumab binds to NKG2A and prevents the binding of NKG2A to its ligand human leukocyte antigen-E (HLA-E), which is overexpressed on tumor cells. This blocks the HLA-E-mediated inhibition of NKG2A-positive infiltrating NK and cytotoxic T-lymphocytes (CTLs) and induces a NK and CTL-mediated immune response against the cancer cells leading to their destruction. Human NKG2A, an inhibitory cell surface receptor covalently bound to CD94, is expressed by NK cells and CTLs. Stimulation of the CD94/NKG2A complex inhibits the cytotoxic activity of these cells. HLA-E, a nonclassical HLA class Ib molecule, is often overexpressed on tumor cells and is associated with poor prognosis.
A monobenzyl ether of hydroquinone with topical depigmentation activity. Although the exact mechanism of action of depigmentation is unknown, the metabolites of monobenzone appear to have a cytotoxic effect on melanocytes. Furthermore, the depigmentation effect might be mediated through the inhibition of tyrosinase, which is essential in the synthesis of melanin pigments, thereby causing permanent depigmentation of the skin.
An orally available inhibitor of monocarboxylate transporter 1 (MCT1), with potential antineoplastic activity. Upon oral administration, MCT1 inhibitor AZD3965 binds to MCT1 and prevents the transport of lactate into and out of the cell. This leads to an accumulation of lactate, intracellular acidification, and eventually cancer cell death. MCT1, a protein overexpressed on tumor cells, is responsible for the transport of monocarboxylates across the cell membrane and plays a key role in cell metabolism.
A cancer vaccine consisting of a humanized monoclonal antibody that mimics a tumor-associated antigen 791Tgp72 (also known as CD55). Vaccination with this agent may stimulate a host cytotoxic T-cell response against tumor cells expressing CD55, resulting in tumor cell lysis.
A vaccine consisting of a monoclonal antibody (MoAB) directed against an idiotype that mimics a human milk fat globule (HMFG) membrane epitope. Vaccination with monoclonal antibody 11D10 anti-idiotype vaccine induces anti-anti-idiotype antibodies (Ab3) that may react with breast cancer cell lines expressing the HMFG membrane epitope.
A murine monoclonal antibody directed against the ganglioside GD2 with potential antineoplastic activity. Monoclonal antibody 14G2A binds to the ganglioside GD2 and induces antibody-dependent cell mediated cytotoxicity and complement-dependent cytotoxicity against GD2-expressing tumor cells. GD2 is overexpressed in malignant melanoma, neuroblastoma, osteosarcoma, and small cell carcinoma of the lung.
A murine monoclonal antibody directed against the cell-surface, tumor-associated antigen ganglioside GD2. Vaccination with monoclonal antibody 3F8 may stimulate a host cytotoxic immune response against tumors that express ganglioside GD2.
A recombinant monoclonal antibody in which the heavy and light chain variable domains mimic a specific epitope of the tumor-associated protein carcinoembryonic antigen (CEA). This agent is used as a cancer vaccine against tumors that express CEA.
A humanized anti-idiotypic (anti-Id) monoclonal antibody (MoAb) that mimics the disialoganglioside GD2 with potential immunostimulating and antineoplastic activities. Upon administration, monoclonal antibody 4B5 anti-idiotype vaccine may elicit both cellular and humoral immune responses against GD2- expressing tumor cells. GD2 is a glycosphingolipid (ceramide and oligosaccharide) that may be highly expressed by melanomas and other neuroectodermal tumors, while only minimally expressed by normal tissues.
A murine IgG1 monoclonal antibody directed against the human transferrin (Tf) receptor. Monoclonal antibody A27.15 binds to the Tf receptor, blocking the binding of transferrin to the receptor and resulting in decreased tumor cell growth.
A humanized monoclonal antibody directed against the human A33 antigen. Monoclonal antibody A33 recognizes the human A33 antigen, a 43 KDa transmembrane glycoprotein of the immunoglobulin superfamily, which is highly and homogenously expressed in 95% of colorectal cancer metastases with only restricted expression in normal colonic mucosa.
A chimeric monoclonal antibody against a Lewis-A-like glycotope (AbGn-7 antigen) with potential immunomodulating and antineoplastic activities. Monoclonal antibody AbGn-7 targets and binds to the carbohydrate AbGn-7 antigen on the cell surface of tumor cells and may induce complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC), thereby killing AbGn-7-epitope positive tumor cells. AbGn-7 antigen is expressed on a variety of tumor cell types, including human colorectal, pancreatic and gastric tumor cells.
A therapeutic monoclonal antibody against an as-of-yet unidentified target expressed on mast cells and eosinophils. Upon administration, AK002 targets and binds to a receptor expressed on the surface of mast cells and eosinophils. This may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against cells overexpressing the undisclosed receptor. This may reduce abnormal proliferation of mast cells and eosinophils, which play a key role in allergic and inflammatory responses.
A monoclonal antibody targeting a not yet disclosed immunomodulatory receptor, with potential antineoplastic activities. Upon intravenous administration, monoclonal antibody ASP1948 binds to its not yet disclosed target, which may stimulate an immune-mediated response against tumor cells.
A humanized monoclonal antibody directed against parathyroid hormone-related protein (PTH-rP). As a poly-hormone with diverse biological roles, PTH-rP is expressed by normal tissues, acting in local tissue environments in a variety of ways; it is commonly overexpressed by breast, prostate, and other cancers, acting systemically by promoting bone resorption, inhibiting calcium excretion from the kidney, inducing hypercalcemia, and possibly playing a role in the formation of bony metastases. By blocking the effects of PTH-rP on calcium metabolism, monoclonal antibody CAL may inhibit cancer-related hypercalcemia.
A second-generation murine monoclonal antibody based on the antibody B72.3 that is directed against tumor-associated glycoprotein 72 (TAG72). TAG72 is expressed by gastric, breast, pancreatic, colorectal, and ovarian carcinoma cells.
A humanized CH2 domain-deleted second-generation monoclonal antibody based on the antibody B72.3 that is directed against tumor-associated glycoprotein 72 (TAG72). TAG72 is expressed by gastric, breast, pancreatic, colorectal, and ovarian carcinoma cells.
A humanized monoclonal antibody targeting glycolipids, with potential immunomodulating and antineoplastic activity. Upon administration, monoclonal antibody CEP-37250/KHK2804 targets and binds to a specific tumor antigen, thereby stimulating the immune system to exert an antibody-dependent cellular cytotoxicity (ADCC) against the tumor associated antigen (TAA)-expressing cancer cells. This agent has shown to be active in both wild-type and mutant K-RAS-expressing colorectal cancer cells.
A murine IgG1 monoclonal antibody directed against the human transferrin (Tf) receptor. Monoclonal antibody E2.3 binds to the Tf receptor, blocking the binding of transferrin to the receptor and resulting in decreased tumor cell growth.
A class of vaccines that consist of anti-idiotype monoclonal antibodies against the tumor-associated antigen disialoganglioside GD2 with potential antineoplastic activity. Vaccination with a monoclonal antibody GD2 anti-idiotype vaccine produces an immunoglobulin response against GD2 with subsequent destruction of GD2 positive tumor cells via antibody-dependent cellular cytotoxicity (ADCC). GD2 is overexpressed in melanoma, neuroblastoma, soft tissue sarcoma, and small cell carcinoma of the lung.
A murine monoclonal antibody with potential antineoplastic activity. Monoclonal antibody HeFi-1 binds to CD30, a cell surface antigen found on mitogen-activated B-cells and T-cells, and Reed-Sternberg cells. Monoclonal antibody HeFi-1 has been shown to arrest tumor growth and prevent metastasis in animal models.
A humanized monoclonal antibody directed against the Lewis Y antigen, a tumor-associated epithelial antigen, with potential antineoplastic activity. Following binding, monoclonal antibody Hu3S193 triggers an antibody-dependent cell-mediated cytotoxicity in cells expressing Lewis Y antigen.
A humanized monoclonal antibody directed against alpha fetoprotein with potential antineoplastic activity. Upon administration, monoclonal antibody HuAFP31 (mAb HuAFP31) binds to and stimulates a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein.
A humanized monoclonal antibody directed against MUC1, a mucin glycoprotein overexpressed in breast and other carcinomas. Monoclonal antibody HuHMFG1 stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing MUC1, resulting in a decrease in tumor burden.
A humanized monoclonal antibody directed against the pancreatic cancer antigen MUC1 with potential antineoplastic activity. Monoclonal antibody HuPAM4 (mAb HuPAM4) binds to cells expressing MUC1 antigen; mAb HuPAM4 may be useful as a carrier for radioisotopes and other antineoplastic therapeutic agents.
A murine IgG2a monoclonal antibody with potential antineoplastic activity. Monoclonal antibody L6 binds to the L6 antigen, a cell surface glycoprotein overexpressed in many carcinomas, and induces antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity against L6-expressing tumor cells. This agent may be conjugated with various toxins in order to target their cytotoxic activity to tumor cells expressing the L6 antigen.
A murine IgG2a monoclonal antibody directed against the HLA-Dr10 protein, a cell surface marker present on over eighty percent of lymphoma cells. When conjugated with a radioactive isotope, Lym-1 monoclonal antibody selectively transports the cytotoxic radioisotope to HLA-Dr10-expressing tumor cells, thereby sparing healthy B-cells and normal tissues. This agent also mediates antibody-dependent cytotoxicity thereby promoting Raji B-lymphoid cell lysis by human neutrophils.
A panadenocarcinoma murine monoclonal antibody with potential antineoplastic activity. Monoclonal antibody m170 may be conjugated with a radioactive element and used in radioimmunotherapy (RIT), a procedure that uses a tumor-specific monoclonal antibody to target radiation to cancer cells.
The F(ab)2 fragment of Me1-14, a murine IgG2a monoclonal antibody directed against proteoglycan chondroitin sulfate-associated protein expressed by gliomas and melanomas. By binding to proteoglycan chondroitin sulfate-associated protein, monoclonal antibody Me1-14 F(ab')2 conjugated to a radioisotope may localize gliomas and melanomas when used as a tracer in radioimaging applications; in radioimmunotherapeutic applications, this agent conjugated to a radioisotope may be used to deliver targeted radiotoxicity to these tumors.
A murine monoclonal antibody directed against the beta subunit of the interleukin-2 receptor (IL-2R), expressed on resting T-lymphocytes, natural killer (NK) cells, and some leukemic cell types. Monoclonal antibody Mik-beta-1 prevents the binding of IL-2 to IL-2R beta, thereby inhibiting the IL-2-mediated proliferation and activation of T-cells.
A humanized immunoglobulin G1 (IgG1) monoclonal antibody derived from an immunogenic preparation of tumor-associated antigens (TAAs) from pooled allogeneic colon cancer tissue extracts, with potential antineoplastic and immunomodulatory activities. Upon intravenous administration, monoclonal antibody NEO-201 targets and binds to malignant tissues with tumor-specific mutations in the membrane-anchored proteins, carcinoembryonic antigen-related cell adhesion molecules 5 and 6 (CEACAM5 and CEACAM6). This prevents the interaction between tumor cell CEACAM 5 and natural killer (NK) cell CEACAM1, and reverses CEACAM1-dependent inhibition of NK cytotoxicity. This may result in the activation of NKs and results in NK-mediated tumor cell killing. Additionally, monoclonal antibody NEO-201 may activate innate immune responses against tumor cells such as antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC). CEACAM 5, and 6 are members of the CEA family of proteins. These membrane proteins are over expressed in a variety of cancer cell types and play a key role in cell migration, invasion, and adhesion.
An IgG murine monoclonal antibody directed against the ganglioside GD3 glycolipid, located in the cell membranes of some tumor cells. Monoclonal antibody R24 binds to GD3-positive cells, thereby initiating antibody-dependent cytotoxicity against GD3-positive cells.
A chimeric monoclonal antibody directed against a primate-restricted N-linked carbohydrate epitope (glycotope) expressed on various human carcinomas with potential antineoplastic activity. Following binding, monoclonal antibody RAV12 disrupts sodium channels of tumor cells expressing this glycotope, resulting in cell and organelle swelling, loss of membrane integrity, and cell death.
A genetically-engineered, chimeric mouse-human, anti-CD30 monoclonal antibody with potential antineoplastic activity. Monoclonal antibody SGN-30 specifically binds to the receptor CD-30, a member of the tumor necrosis factor receptor super-family, which may be overexpressed on the surfaces of Hodgkin lymphoma cells and anaplastic-large cell lymphoma cells. After binding to CD30, this agent interferes with the G1 phase of the cell cycle, thereby inducing growth arrest and apoptosis in susceptible tumor cell populations.
A proprietary monoclonal antibody targeting an as of yet undisclosed tumor-associated antigen (TAA), with potential antineoplastic activity. Although the mechanism of action has not been elucidated presumably monoclonal antibody TRK-950 binds to a specific TAA on the cell surface of tumor cells and may induce complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). This may lead to the death of tumor cells expressing the TAA.
An orally available preparation derived from a single clone of Bifidobacterium spp. with potential immunomodulatory and antineoplastic activities. Upon oral administration, monoclonal microbial EDP1503 colonizes the gut and may, through a not yet fully elucidated mechanism, promote the activation of dendritic cells (DCs), and enhance the induction and infiltration of cytotoxic T-lymphocytes (CTLs) in the tumor microenvironment (TME). Bifidobacterium is a genus of anaerobic, Gram-positive bacteria, with some species being a commensal part of the human gastrointestinal tract and vaginal flora.
A fusion protein containing a modified form of human T-cell receptor (TCR) specific for the gp100 antigen and fused to an anti-CD3 single-chain antibody fragment, with potential antineoplastic activity. Upon direct intratumoral administration of IMCgp100 into the melanoma lesion, the TCR moiety of this agent targets and binds to the tumor associated antigen (TAA) gp100 presented on the melanoma tumor cell; the anti-CD3 fragment moiety binds to CD3- expressing T lymphocytes, thereby selectively cross-linking tumor cells and T-lymphocytes. This may lead to the recruitment of cytotoxic T lymphocytes (CTL) to the T lymphocyte/tumor cell aggregates and result in CTL-mediated death of gp100-expressing melanoma cancer cells.
Brand name for iron isomaltoside 1000
A modified form of lipid A, the biologically active part of Gram-negative bacterial lipopolysaccharide (LPS) endotoxin, and a Toll-like receptor 4 (TL= R4) agonist, with potential immunostimulatory activity. As a vaccine adjuvant, monophosphoryl lipid A (MPLA) stimulates both cellular and humoral responses to the vaccine antigen. Compared to LPS, MPLA exerts a similar immunostimulatory activity but with reduced toxicity.
A glycosphingolipid containing a sialic acid residue found in neuronal cell membranes, with potential neuroprotective and neuroregenerative activities. Upon administration, monosialotetrahexosylganglioside, also called GM-1, is able to both prevent neurologic damage and induce regeneration of damaged neurons through neurotrophic repair mechanisms, enhancement of the production of neutrophins, and augmenting neurite outgrowth. In addition, GM-1 exerts anti-excitotoxic activity, prevents necrosis, and improves neuronal recovery and function.
An water-in-oil (w/o) emulsion with immunomoadjuvant activity. Montanide ISA 51 VG appears to act by enhancing the immune system’s cytotoxic T-lymphocyte (CTL) response against antigen(s) in vaccines. The surfactant mannide monooleate in Montanide ISA 51 VG contains vegetable-grade (VG) oleic acid derived from olive oil.
A proprietary adjuvant, applicable for water-in-oil (W/O; 30/70 v/v) vaccine emulsion, with potential immunoadjuvant activity. Montanide ISA 720 is made of natural metabolizable non-mineral oil and a highly refined emulsifier from the mannide mono-oleate family; it is rapidly metabolized and eliminated, and may be used in various vaccines, including cancer vaccines. Upon administration, Montanide ISA 720 forms a depot at the injection site and is therefore capable of slowly releasing the antigen(s) from the injection site. This may result in enhanced cellular and humoral immune responses to the antigen vaccine.
The orally bioavailable monosodium salt of montelukast, a selective cysteinyl leukotriene receptor antagonist with anti-inflammatory and bronchodilating activities. Montelukast selectively and competitively blocks the cysteinyl leukotriene 1 (CysLT1) receptor, preventing binding of the inflammatory mediator leukotriene D4 (LTD4). Inhibition of LTD4 activity results in inhibition of leukotriene-mediated inflammatory events including: migration of eosinophils and neutrophils; adhesion of leukocytes to vascular endothelium, monocyte and neutrophil aggregation; increased airway edema; increased capillary permeability; and bronchoconstriction. The CysLT1 receptor is found in a number of tissues including spleen, lung, placenta, small intestine, and nasal mucosa, and in a variety of cell types including monocyte/macrophages, mast cells, eosinophils, CD34-positive hemopoietic progenitor cells, neutrophils and endothelial cells.
Brand name for fosfomycin tromethamine
A chemotherapy regimen consisting of mechlorethamine, vincristine (Oncovin), procarbazine and prednisone, used alone or in combination with radiation therapy for the treatment of stage I-IV Hodgkin lymphoma. Due to the increased risk of gonadal toxicity, this regimen has been widely replaced by the ABVD regimen. (NCI Thesaurus]]
An extract prepared from the fruit of Morinda citrifolia, a plant that yields various herbal preparations. Morinda citrifolia fruit juice has antioxidant properties and may prevent tumorigenesis via inhibition of DNA-carcinogen adduct formation.
The sulfate salt of morphine, an opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. Morphine binds to and activates specific opiate receptors (delta, mu and kappa), each of which are involved in controlling different brain functions. In the central nervous and gastrointestinal systems, this agent has widespread effects including analgesia, anxiolysis, euphoria, sedation, respiratory depression, and gastrointestinal system smooth muscle contraction.
A sustained-release tablet formulation containing the sulfate salt of the opiate alkaloid morphine with analgesic activity. Morphine binds to and activates the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of the endogenous opioids. Binding of morphine to opioid receptors stimulates exchange of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, morphine closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, which results in hyperpolarization of neuronal membranes and a reduction in neuronal excitability, and subsequently, analgesia and sedation.
A synthetic version of a monoacetyldiacylglyceride naturally occurring in various seed oils, bovine udder and milk fat, antlers of sika deer, with potential antineoplastic activity. Although the exact mechanism of action through which mosedipimod exerts its pharmacological effect has yet to be fully identified, upon administration, mosedipimod stimulates calcium influx into T lymphocytes and increases the production of various cytokines, including interleukin (IL) -2, IL-4, IL-12, interferon-gamma (IFN-g), and granulocyte-macrophage colony-stimulating factor (GM-CSF). This stimulates the proliferation of hematopoietic stem cells, bone marrow stromal cells and immune cells, including T and B lymphocytes, dendritic cells (DCs) and macrophages. Therefore, mosedipimod may stimulate the immune system to target cancer cells. In addition, mosedipimod enhances the cytolytic activity of natural killer (NK) cells and suppresses the expression of the transmembrane protein tumor cell toll-like receptor 4 (TLR-4) on cancer cells. As activation of TLR-4 enhances immunosuppression and stimulates cancer cell growth, blocking TLR-4 expression suppresses tumor cell proliferation.
A bispecific, humanized monoclonal antibody with potential antineoplastic activity. Anti-CD20/CD3 bispecific monoclonal antibody BTCT4465A contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen, and one for human CD20, a tumor-associated antigen (TAA) that is exclusively expressed on B cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, BTCT4465A binds to both T cells and CD20-expressing tumor B cells; this cross-links T cells to tumor cells, and may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B cells.
The orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.
A synthetic metallotexaphyrin with radiosensitizing and chemosensitizing properties. Motexafin gadolinium accumulates in tumor cells preferentially due to their increased rates of metabolism, generating reactive oxygen species (ROS) intracellularly and lowering the tumor cell apoptotic threshold to ionizing radiation and chemotherapy.
A pentadentate aromatic metallotexaphyrin with photosensitizing properties. Motexafin lutetium preferentially accumulates in tumor cells due to their increased rates of metabolism and absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen, resulting in local cytotoxic effects.
Brand name for ibuprofen
A vaccine consisting of a plasmid DNA encoding the murine melanoma-associated antigen gp100. Upon administration, expressed gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumor cells that express the gp100 antigen, resulting in tumor cell lysis.
A vaccine consisting of a plasmid DNA encoding the murine prostate-specific membrane antigen (PSMA). Upon administration, expressed PSMA may stimulate a cytotoxic T cell response against tumor cells that express PSMA, resulting in tumor cell lysis.
An agarose matrix containing mouse renal adenocarcinoma (RENCA) cells, with potential antineoplastic activity. The agarose-agarose macrobeads consist of two spherical agarose layers; the mouse RENCA cells are contained within the inner agarose layer. Upon placement into the abdominal cavity, the restricted mouse renal adenocarcinoma cells in the agarose macrobeads produce and release certain growth-retarding factors that inhibit the proliferation of the RENCA cells. Upon diffusion of these growth-slowing factors out of the agarose layers, these substances may inhibit cancer cell proliferation of proliferating tumors.
Brand name for meloxicam
Brand name for naloxegol
Brand name for meloxicam
A recombinant engineered chimeric gene derived from the murine gene encoding the variable region of monoclonal antibody MOv18 against folate-binding protein, which is often overexpressed in human ovarian cancer cells, and the gene encoding the Fc receptor for the gamma subunit of human IgG and IgE. Peripheral blood lymphocytes expressing the MOv-gamma gene may be used in the immunotherapeutic treatment of ovarian cancer.
A recombinant immunotoxin consisting of the Fv portion of the anti-CD22 antibody covalently fused to a 38 KDa fragment of Pseudomonas exotoxin-A (PE38) with potential antineoplastic activity. The Fv portion of anti-CD22 immunotoxin CAT-8015 binds to CD22, a cell surface receptor expressed on a variety of malignant B cells, thereby delivering the toxin moiety PE38 directly to tumor cells. Once internalized, PE38 induces caspase-mediated apoptosis via a mechanism involving mitochondrial damage and blocks translational elongation by binding to elongation factor 2 (EF-2). Moxetumomab pasudotox-tdfk exhibits a greater affinity for CD22 than its predecessor, anti-CD22 immunotoxin CAT-3888 (BL22 immunotoxin), and hence may be more effective against tumor cells expressing lower levels of CD22.
The hydrochloride salt of a fluoroquinolone antibacterial antibiotic. Moxifloxacin binds to and inhibits the bacterial enzymes DNA gyrase (topoisomerase II) and topoisomerase IV, resulting in inhibition of DNA replication and repair and cell death in sensitive bacterial species.
Brand name for plerixafor
A formulation containing pegylated liposomal nanoparticles encapsulating a prodrug of the poorly water-soluble, second-generation taxane analog docetaxel, with potential antineoplastic activity. Upon intravenous administration of the liposomal docetaxel prodrug MNK-010, docetaxel is slowly released into the systemic circulation and accumulates at the tumor site due to the unique characteristics of the tumor's vasculature. In turn, docetaxel is taken up by tumor cells, and subsequently binds to and stabilizes the beta-subunit of tubulin, thereby stabilizing microtubules and inhibiting microtubule disassembly. This results in cell cycle arrest and induces cell death. Compared to the administration of docetaxel alone, this formulation is able to increase the delivery of docetaxel into tumors, thereby increasing docetaxel's efficacy while minimizing its toxicity. In addition, this formulation solubilizes docetaxel without the use of toxic solvents, thereby permitting the administration of larger doses of docetaxel while avoiding solvent-associated toxicity.
An orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1, TTK), with potential antineoplastic activity. Upon administration, the Mps1 inhibitor BAY 1217389 selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC), accelerates mitosis, causes chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. Mps1, a kinase expressed in proliferating normal tissues and aberrantly overexpressed in a wide range of human tumors, is activated during mitosis and is essential for proper SAC functioning and chromosome alignment.
An orally bioavailable, selective inhibitor of the serine/threonine-protein kinase monopolar spindle 1 (Mps1; TTK), with potential antineoplastic activity. Upon administration, the Mps1 inhibitor BOS172722 binds to and inhibits the activity of Mps1, a core component of the spindle assembly checkpoint (SAC). Inhibition of Mps1 activity compromises spindle assembly checkpoint, increases chromosome missegregation errors and decreases cancer cell viability. Mps1, a dual-specificity protein kinase expressed in proliferating normal tissues and aberrantly overexpressed in certain tumor types, is activated during mitosis and is essential in proper SAC function and chromosomal alignment.
An orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase, with potential antineoplastic activity. Upon administration, the Mps1 kinase inhibitor BAY1161909 binds to and inhibits the activity of Mps1. This causes inactivation of the spindle assembly checkpoint (SAC), accelerated mitosis, chromosomal misalignment, chromosomal missegregation, mitotic checkpoint complex destabilization, and increased aneuploidy. This leads to the induction of cell death in cancer cells overexpressing Mps1. Mps1, a kinase expressed in proliferating normal tissues and aberrantly overexpressed in a wide range of human tumors, is activated during mitosis and is essential for SAC functioning and controls chromosome alignment.
An mRNA-based individualized, therapeutic personalized cancer vaccine (PCV) targeting twenty tumor-associated antigens (TAAs) that are specifically expressed by the patient's cancer cells, with potential immunostimulatory and antineoplastic activities. The cells from the patient's tumor are analyzed, and genetic sequencing is used to identify twenty neoantigen epitopes that may elicit the strongest immune response in the patient. The sequences encoding the twenty patient-specific epitopes are transcribed and loaded onto a single mRNA molecule. Upon administration, the mRNA-based PCV mRNA-4157 is taken up and translated by antigen presenting cells (APCs). Then, the expressed epitopes are presented via major histocompatibility complex (MHC) molecules on the surface of the APCs. This leads to an induction of both cytotoxic T-lymphocyte (CTL)- and memory T-cell-dependent immune responses that specifically target and destroy the patient's cancer cells that express these neoantigens.
An mRNA-based therapeutic personalized cancer vaccine (PCV) targeting up to fifteen tumor-associated antigens (TAAs) that are specifically expressed by a patient's cancer cells, with potential immunostimulatory and antineoplastic activities. The cells from the patient's tumor are analyzed and subjected to RNA sequencing to identify mutant and immunogenic epitopes. The neoantigen epitopes are screened to select those that induce a strong immune response in tumor- infiltrating lymphocytes (TILs) isolated from the patient. The selected mRNA sequences encoding up to fifteen neoantigen epitopes are incorporated in a proprietary formulation designed to maximize mRNA delivery and minimize mRNA-triggered immune responses. Upon administration, the mRNA-based PCV NCI-4650 is taken up and the mRNAs are translated by antigen presenting cells (APCs). Then, the expressed epitopes are presented via major histocompatibility complex (MHC) molecules on the surface of the APCs. This induces both cytotoxic T-lymphocyte (CTL)- and memory T-cell-dependent immune responses that specifically target and destroy the patient's cancer cells that express these neoantigens.
A melanoma vaccine consisting of mRNAs encoding five different melanoma tumor-associated antigens (TAAs) and a TriMix platform comprised of three mRNAs encoding for constitutively activated toll-like receptor 4 (caTLR4), CD40 ligand (CD40L), and CD70, with potential immunomodulatory and antineoplastic activities. Upon intranodal injection, mRNA based TriMix vaccine ECI-006 may stimulate the immune system to mount both humoral and cellular responses against tumor cells expressing the five TAAs specific to the vaccine, potentially decreasing cellular proliferation of cells expressing these antigens. The TriMix adjuvants CD40L and caTLR4 promote the generation of mature and active dendritic cells (DCs), and CD70 provides a costimulatory signal to CD27+ naive T cells, thereby supporting T-cell proliferation and inhibiting T-cell apoptosis.
An mRNA-based, personalized cancer vaccine consisting of a self-amplifying mRNA (SAM), formulated in a lipid nanoparticle (LNP), targeting twenty tumor-specific neoantigens (TSNAs) that have been identified through genetic sequencing of a patient’s tumor cells, with potential immunostimulatory and antineoplastic activities. Upon intramuscular administration of the mRNA-based tumor-specific neoantigen boosting vaccine GRT-R902, the mRNA is taken up and translated by antigen presenting cells (APCs). Then, the expressed epitopes are presented via major histocompatibility complex (MHC) molecules on the surface of APCs. This leads to an induction of both cytotoxic T-lymphocyte and memory T-cell dependent immune responses that specifically target and destroy the patient’s cancer cells that express these neoantigens. mRNA-based TSNA boosting vaccine is administered after a single dose of the adenoviral tumor-specific neoantigen priming vaccine GRT-C901. The combined immunotherapy product, consisting of priming and boosting vaccines, is referred to as GRANITE-001.
A non-small cell lung cancer (NSCLC) vaccine containing six modified mRNAs, which encode six different NSCLC associated antigens, with potential antitumor and immunomodulatory activities. Upon intradermal administration, mRNA-derived lung cancer vaccine BI 1361849 may stimulate the immune system to mount both humoral and cellular responses against NSCLC cells. The six tumor-associated antigens (TAAs) encoded by these mRNAs are frequently expressed by NSCLC cells and are minimally expressed or absent in normal, healthy cells.
A prostate cancer vaccine containing mRNAs encoding prostate specific antigen (PSA), prostate specific membrane antigen (PSMA), prostate stem cell antigen (PSCA) and six-transmembrane epithelial antigen of the prostate (STEAP), with potential antitumor activity. Upon administration, mRNA-derived prostate cancer vaccine CV9103 may stimulate the immune system to mount a cytotoxic T lymphocyte response (CTL) against PSA-, PSMA-, PSCA- and STEAP-expressing prostate tumor cells. The mRNA used in this vaccine is modified and formulated to have enhanced translational potency and adjuvant activities. .PSA, PSMA, PSCA and STEAP may be upregulated in prostate cancer cells; their expression in prostate cancer has been correlated with disease progression.
A prostate cancer vaccine containing six messenger RNAs (mRNAs) encoding for antigens upregulated in prostate cancer, including mRNAs for prostate specific antigen (PSA), prostate specific membrane antigen (PSMA), prostatic acid phosphatase (PAP), and mucin 1 (MUC1), with potential antineoplastic and immunomodulating activities. Upon intradermal administration of mRNA-derived prostate cancer vaccine CV9104, this agent enters cells, the mRNAs are translated into the respective prostate specific antigens and may cause the immune system to mount a cytotoxic T lymphocyte response (CTL) against PSA-, PSMA-, PAP- and MUC1-expressing prostate tumor cells. The mRNAs used in this vaccine are modified to have enhanced translational potency and adjuvant activities. PSA, PSMA, PAP and MUC1 are frequently upregulated in prostate cancer cells; their expression in prostate cancer has been correlated with disease progression.
Brand name for morphine sulfate
Brand name for morphine sulfate
The hydrochloride salt of a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor APTO-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.
An orally bioavailable, ATP-competitive, tetrahydroquinazoline (THQ)-based inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. Upon administration, GDC-0349 selectively binds to and inhibits the activity of mTOR, which may result in both the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase belonging to the phosphatidylinositol-3 (PI3K) kinase-related kinase (PIKK) family, plays an important role in the PI3K/Akt/mTOR signaling pathway that regulates cell growth and proliferation, and its expression or activity is frequently dysregulated in human cancers.
An inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor AZD8055 inhibits the serine/threonine kinase activity of mTOR, resulting in decreased expression of mRNAs necessary for cell cycle progression, which may induce cell cycle arrest and tumor cell apoptosis. mTOR phosphorylates transcription factors, such as S6K1 and 4E-BP1, which stimulate protein synthesis and regulate cell growth, proliferation, motility, and survival.
An orally available inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in human cancers.
An orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.
An active metabolite of NV-128, a novel flavonoid small molecule inhibitor of the mammalian Target of Rapamycin (mTOR), with potential antineoplastic activity. Upon administration, mTOR1/2 Kinase inhibitor ME-344 downregulates the PIK3/AKT/mTOR pathway and results in chromatin condensation in the absence of caspase activation. Consequently, this agent induces caspase-independent cell death in tumor cells with a de-regulated PIK3/AKT/mTOR pathway or chemotherapeutic resistant cells.
An orally bioavailable inhibitor of raptor-mammalian target of rapamycin (mTOR) complex 1 (mTOR complex 1; mTORC1) and rictor-mTOR complex 2 (mTOR complex 2; mTORC2), with potential antineoplastic activity. Upon oral administration, mTORC1/2 inhibitor LXI-15029 binds to the kinase domain of mTOR and inhibits both mTORC1 and mTORC2, in an ATP-competitive manner. This inhibits mTOR-mediated signaling and leads to both an induction of apoptosis and a decrease in the proliferation of mTORC1/2-expressing tumor cells. mTOR is a serine/threonine kinase that is upregulated in certain tumor cell types. It plays an important role in the PI3K/Akt/mTOR signaling pathway, which is often deregulated in cancer cells and promotes cell growth, survival, and resistance to chemotherapy and radiotherapy.
An orally bioavailable inhibitor of raptor-mammalian target of rapamycin (mTOR) complex 1 (mTOR complex 1; mTORC1) and rictor-mTOR complex 2 (mTOR complex 2; mTORC2), with potential antineoplastic activity. Upon oral administration, mTORC1/2 kinase inhibitor BI 860585 binds to the kinase domain of mTOR and inhibits both mTORC1 and mTORC2, in an ATP-competitive manner. This inhibits mTOR-mediated signaling and leads to both an induction of apoptosis and a decrease in the proliferation of mTORC1/2-expressing tumor cells. mTOR is a serine/threonine kinase that is upregulated in certain tumor cell types. It plays an important role in the PI3K/Akt/mTOR signaling pathway, which is often deregulated in cancer cells and promotes cell growth, survival, and resistance to chemotherapy and radiotherapy.
An orally bioavailable, lipid analogue and inhibitor of raptor-mammalian target of rapamycin (mTOR) (mTOR complex 1; mTORC1), rictor-mTOR (mTOR complex 2; mTORC2) and dihydrofolate reductase (DHFR) with potential antineoplastic activity. Upon oral administration, mTORC1/mTORC2/DHFR inhibitor ABTL0812 binds to and inhibits both mTORC1 and mTORC2, which may result in apoptosis and a decrease in proliferation in mTORC1/2-expressing tumor cells. mTOR is a serine/threonine kinase that is upregulated in some tumors; it plays an important role in the PI3K/Akt/mTOR signaling pathway which is often deregulated in cancer cells. In addition, ABTL0812 inhibits DHFR, an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, thereby blocking tetrahydrofolate synthesis, and resulting in both the depletion of nucleotide precursors and the inhibition of DNA, RNA and protein synthesis. This leads to autophagy-induced cell death and further inhibition of cell proliferation.
MUC-1 antigen is a mammary-type apomucin, a high molecular weight transmembrane glycoprotein, of which the extracellular domain is formed by a repeating 20 amino acid sequence (in tandem) with a high content of serine and threonine on which are O-linked carbohydrate chains. MUC-1 synthesis and secretion are features of glandular epithelial tissues; MUC-1 is overexpressed in lactating breast and in breast, ovary, lung, and prostate malignancies.
A cancer vaccine comprised of a synthetic peptide derived from the mucin 1 (MUC1) antigen with potential antineoplastic activity. Upon administration, MUC1 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the MUC1 antigen, resulting in decreased tumor growth. Overexpressed on many tumor cells, MUC1 antigen, a mammary-type apomucin, is a high-molecular-weight transmembrane glycoprotein.
A vaccine preparation containing mucus 1 (MUC1) peptide and the adjuvant poly-ICLC with potential immunostimulatory and antineoplastic activities. Upon administration, MUC1 peptide-poly-ICLC adjuvant vaccine may induce the host immune system to mount a cytotoxic T cell response against MUC1-expressing tumor cells. MUC1, a tumor associated antigen normally present on the lining of the human colon, may be overexpressed and/or mutated in a variety of cancer cell types. The adjuvant poly-ICLC, a ligand for toll-like receptor-3, induces the release of cytokines which may help boost the immune response against MUC1.
An antibody drug conjugate (ADC) consisting of a humanized IgG1 monoclonal antibody targeting the MUC16 protein (CA-125) conjugated to, via a cleavable linker, the antimicrotubulin agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. The monoclonal antibody moiety of DMUC5754A selectively binds to MUC16. After internalization of the drug conjugate and proteolytic cleavage of the linker, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M-phase growth arrest and tumor cell apoptosis. MUC16, a transmembrane protein, is overexpressed on the cell surface of more than 80 percent of ovarian cancer cells but not on healthy cells.
A peptide vaccine, containing human tumor-associated epithelial mucin (MUC1) conjugated with keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with MUC1-KLH conjugate vaccine may stimulate humoral and cytotoxic T-lymphocyte (CTL) responses against tumor cells expressing the MUC1 antigen. In this vaccine, MUC1 antigen is conjugated with KLH, an immunostimulant and a hapten carrier, to enhance immune recognition. MUC1 antigen, a membrane-bound glycoprotein expressed by most glandular and ductal epithelial cells, is overexpressed in an aberrant or deglycosylated form in various cancers such as those of the breast, prostate, and ovary.
A peptide vaccine containing the human tumor-associated antigen epithelial mucin (MUC1 antigen) conjugated with keyhole limpet hemocyanin (KLH) and combined with the nonspecific immunoadjuvant QS21 with potential antineoplastic activity. MUC1 antigen is linked with KLH, an immunostimulant and a hapten carrier, in order to enhance immune recognition; the co-administration of saponin-derived QS21 potentially amplifies the total immune response to the MUC1 antigen. Administration of MUC1-KLH vaccine/QS21 may result in both the production of antitumor antibodies and the stimulation of a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the MUC1 antigen. MUC1 antigen, a membrane-bound glycoprotein expressed by most glandular and ductal epithelial cells, is overexpressed as an aberrant or deglycosylated form in various cancers such as breast, prostate and ovarian cancers.
An optimized small peptide drug candidate targeting epithelial mucin (MUC1) with antineoplastic activity. MUC1-targeted peptide GO-203-2C interacts with oncoprotein MUC1 C-terminal subunit on the cell surface, thereby impeding cell-cell interactions, signaling, and metastasis. MUC1 antigen, a membrane bound glycoprotein expressed by most glandular and ductal epithelial cells, is over-expressed in many diverse human carcinomas including those of the breast, prostate, lung, colon, pancreas, and ovary, and has been associated with poor prognosis.
An oral rinse composed of a viscous, mucoadhesive hydrogel, with potential protective and antimucositis activities. Upon gargling with the oral viscous mucoadhesive hydrogel formulation in the oral cavity, the hydrogel forms a protective barrier over the oral mucosa, which prevents inflammation of the mucosal membranes and may decrease chemotherapy- and/or radiation-induced oral mucositis.
A viscous, oral hydrogel rinse intended for the management of oral mucositis/stomatitis. Mucoadhesive oral wound rinse consists of purified water, glycerin, benzyl alcohol, sodium saccharin, carbomer homopolymer A, potassium hydroxide, citric acid, polysorbate 60 and phosphoric acid. Upon gargling and rinsing with this solution, it forms a soothing protective hydrogel coating over the oral mucosa, thereby potentially preventing or reducing chemotherapy-induced mucositis.
An orally available, mucoadhesive lipid preparation consisting of paclitaxel, a compound extracted from the Pacific yew tree Taxus brevifolia, in a formulation that is comprised of a mixture of monoolein, tricarprylin, and Tween 80, with potential antineoplastic activity. Upon oral administration, DHP107 forms droplets and micelles in the intestine; these adhere to mucoepithelial cells in the gastrointestinal tract and are absorbed through lipid-based uptake mechanisms. Upon absorption, paclitaxel binds to and stabilizes tubulin molecules, which results in the inhibition of both microtubule depolymerization and cell division. This agent also induces apoptosis by both binding to and blocking the function of the apoptosis inhibitor protein B-cell Leukemia 2 (Bcl-2).The mucoadhesive paclitaxel formulation does not contain P-glycoprotein inhibitors, the solvent cremophor or any other toxic solvent.
Brand name for acetylcysteine
Brand name for mucoadhesive oral wound rinse
An orally available, small molecule inhibitor of AGC group kinases, with potential antineoplastic activity. AT13148 inhibits, in an ATP-competitive manner, the enzymatic activity of two AGC kinases, protein kinase B (PKB or AKT) and p70S6K which play key roles in the PI3K/PKB/mTOR signaling pathway. Blockade of this pathway leads to an inhibition of cell growth and the induction of apoptosis in susceptible tumor cells. PI3K/PKB/mTOR pathway is dysregulated in greater than 50% of tumors, and is often correlated with resistance and increased tumor survival. AGC group kinases are serine/threonine kinases that are regulated by secondary messengers such as cyclic AMP and lipids.
A supplement containing multiple, as of yet undisclosed, carotenoids, with potential chemopreventive activity. Upon oral administration of the multicarotenoid supplement MCS-8, the carotenoids may be able to exert their chemopreventive activity through multiple mechanisms of action.
A peptide vaccine containing five immunogenic peptide epitopes of the human folate receptor 1 (FOLR1; FR-alpha), with potential immunomodulating and antineoplastic activities. Upon intradermal administration, multi-epitope anti-folate receptor peptide vaccine TPIV 200 may induce a cytotoxic T-lymphocyte (CTL) response against FR-alpha-overexpressing tumor cells. FR-alpha is a high-affinity folate-binding protein and a member of the folate receptor family; this receptor is overexpressed in various cancer cell types.
A peptide vaccine containing five immunogenic peptide epitopes of the human folate receptor alpha (FR alpha or FOLR1), including FR30, FR56, FR76, FR113, and FR238, with potential immunomodulating and antineoplastic activity. Upon administration, the multi-epitope FR alpha peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against FR alpha-overexpressing tumor cells. FR alpha is a high-affinity folate-binding protein and a member of the folate receptor family; this receptor is overexpressed in a majority of ovarian cancers and in about 50% of breast cancers.
A peptide cancer vaccine consisting of a combination of peptides derived form several melanoma epitopes. Vaccination with multi-epitope melanoma peptide vaccine stimulates the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the corresponding antigens, resulting in tumor cell lysis. This vaccine may stimulate a broader CTL response compared to single-antigen vaccines.
A cell-based cancer vaccine comprised of autologous dendritic cells pulsed with multiple antigenic peptides derived from T-cell receptor gamma-chain alternate reading frame protein (TARP), with potential immunostimulatory and antineoplastic activities. Upon intradermal administration, multi-epitope (ME) TARP-pulsed autologous dendritic cell vaccine may stimulate anti-tumor cytotoxic T-lymphocyte (CTL) and antibody responses against TARP-expressing cancer cells, resulting in tumor cell lysis. The highly immunogenic nuclear protein TARP is expressed in a variety of cancer cell types.
Brand name for multisubtype natural human leukocyte interferon alpha
An orally available, multivalent herbal formulation containing a novel mixture of whole extracts from three commonly used Chinese medicinal herbs Ganoderma lucidum (lingzhi mushroom), Salvia miltiorrhiza (Chinese sage, or danshen) and Scutellaria barbata (ban zhi lian), with potential immunomodulating, antiangiogenic, anti-inflammatory, antiproliferative and antiviral activities. Although the exact mechanism of action remains to be fully elucidated due to the complexity of the multiple phytochemicals, multifunctional/multitargeted anticancer agent OMN54 appears to work in an additive and synergistic manner by acting on a variety of signaling pathways and on multiple targets, such as vascular endothelial growth factor, nuclear factor kappa B, interleukin-1beta, fibroblast growth factor, and epidermal growth factor.
A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with six synthetic glioblastoma (GBM) peptides: absent in melanoma 2 (AIM-2), melanoma-associated antigen 1 (MAGE-1), tyrosinase-related protein 2 (TRP-2), glycoprotein 100 (gp100), epidermal growth factor receptor 2 (HER-2), interleukin-13 receptor subunit alpha-2 (IL-13Ra2), with potential immunostimulatory and antineoplastic activities. Mononuclear cells obtained via leukapheresis are differentiated into DCs, and pulsed with the GBM-associated peptides. Upon administration, multi-glioblastoma-peptide-targeting autologous DC vaccine ICT-107 exposes the immune system to GBM-associated antigens, which activates a specific cytotoxic T-lymphocyte (CTL) response against GBM cells. This leads to GBM cell lysis. The six peptides are derived from tumor associated antigens (TAA) expressed on GBM cells and cancer stem cells (CSCs). GBM stem-like cells contain a specific range of antigens that are essential for the neoplastic growth and survival of GBM cells.
Brand name for gadobenate dimeglumine
Brand name for gadopentetate dimeglumine
A multikinase inhibitor with potential antineoplastic activity. Multikinase inhibitor 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs). This may result in the inhibition of angiogenesis and cell proliferation in tumor cells in which these kinases are upregulated. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias (AML). VEGFRs, tyrosine kinase receptors, are overexpressed in a variety of tumor cell types and play key roles in angiogenesis.
A small-molecule inhibitor of several kinases with potential antineoplastic activity. Multikinase inhibitor AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis; JAK2 is a kinase that transduces signals from the single chain and IL-3 cytokine receptor families, and from the IFN-gamma receptors; BCR-ABL is a fusion protein with tyrosine kinase activity that is commonly found in CML.
A multikinase inhibitor with potential antineoplastic activity. Upon intravenous infusion, multikinase inhibitor SAR103168 may, through the inhibition of multiple kinases, inhibit the phosphorylation and activation of signal transducer and activator of transcription 5 (STAT5). STAT5, a protein often upregulated in cancer cells, plays a key role in signal transduction pathways and the suppression of apoptosis.
Brand name for recombinant leukocyte interleukin
A vaccine consisting of an inactivated, Modified Vaccinia Ankara (MVA) viral vector encoding three herpes virus cytomegalovirus (CMV) tumor-associated antigens (TAAs), including UL83 (pp65), UL123 (IE1) and UL122 (IE2), with potential immunostimulating activity. The viral peptides expressed after administration of the multi-peptide CMV-MVA vaccine, may stimulate the immune system to mount both cytotoxic T-lymphocyte (CTL) and helper T-cell responses against CMV-infected cells. This results in cell lysis and prevents viral replication and the development of CMV disease. This vaccine also provides active immunization and protective immunity against CMV infection in CMV-negative patients. CMV infection can cause serious complications in patients receiving either allogeneic hematopoietic cell transplants (HCT) or solid organ transplants.
A cancer vaccine composed of a combination of the injectable formulations S-488210, which contains the three HLA-A*02:01-restricted peptides up-regulated lung cancer 10 (lymphocyte antigen 6K; LY6K; URLC10), cell division cycle-associated protein 1 (kinetochore protein Nuf2; NUF2; CDCA1) and insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3; KOC1) and S-488211, which contains the two HLA-A*02:01-restricted peptides DEP domain-containing protein 1A (DEPDC1) and M-phase phosphoprotein 1 (kinesin-like protein KIF20B; MPHOSPH1), with potential immunostimulatory and antitumor activities. Upon administration, multipeptide vaccine S-588210 may stimulate a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing KOC1, CDCA1, URLC10, DEPDC1 or MPHOSPH1 peptides, resulting in tumor cell lysis and decreased tumor growth.
A dendritic cell (DC) vaccine in which autologous DCs are loaded with multiple tumor-associated antigens (TAAs), with potential immunostimulating and antineoplastic activities. Upon re-infusion into the patient, the antigen-pulsed DCs stimulate the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against the TAA-expressing tumor cells.
Brand name for allogeneic multipotent adult progenitor cells
A preparation containing a mixture of multiple naturally occurring, active subtypes 1, 2, 8, 10, 14 and 21 of interferon alpha (IFN-alpha) with immunomodulating, anti-viral and anti-cancer activities. Multi-subtype natural human leukocyte IFN-alpha is purified from the leukocyte fraction of human blood challenged with Sendai virus. Upon administration, IFN-alpha subtypes bind to cell surface IFN-alpha receptors (IFNARs), resulting in an upregulation of interferon stimulated genes and related protein products. This ultimately leads to the proliferation of human B cells, activation of natural killer (NK) cells and dendritic cells (DCs), an increase in HLA-I and HLA-II expression and activation of CD8-lymphocytes. Compared to single-subtype IFN, multi-subtypes act synergistically.
An orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB).
A dietary supplement containing all or most of the vitamins that may not be readily available in the diet. Vitamins may be classified according to their solubility either in lipids (vitamins A, D, E, K, F) or in water (vitamins C, B-complex). Present in minute amounts in various foods, vitamins are essential to maintaining normal metabolism and biochemical functions.
A water-soluble prodrug, consisting of camptothecin covalently linked to polymeric backbone methacryloylglycynamide, with potential antineoplastic activity. After entering tumor cells, the active moiety camptothecin is slowly released from mureletecan via hydrolysis of the ester linkage. Camptothecin, an alkaloid isolated from the Chinese tree Camptotheca acuminata, binds to and stabilizes the topoisomerase I-DNA covalent complex. This inhibits the religation of topoisomerase I-mediated single-stranded DNA breaks and produces potentially lethal double-stranded DNA breaks when encountered by the DNA replication machinery, resulting in the inhibition of DNA replication and apoptosis. Compared to camtpothecin, this prodrug formulation increases camptothecin drug delivery to the tumor site while reducing systemic toxicity.
A plasmid DNA vaccine encoding the mouse tumor associated antigen tyrosinase-related protein-2 (TYRP2) with potential immunostimulating and antineoplastic activities. Upon administration, murine TYRP2 plasmid DNA vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing TYRP2; this vaccine may also induce an immune response against tyrosinase-related protein-1 (TYRP1). TYRP2 and TYRP1, melanosomal membrane glycoproteins upregulated in melanoma cells, are involved in melanin synthesis.
A murine IgG2a monoclonal antibody with immunosuppressive activity. Muromonab-CD3 binds to and inhibits CD3 on the surface of circulating T-lymphocytes; binding of muromonab-CD3 to CD3-positive T cells results in an early activation of this T cell subset, followed by cytokine release, and subsequently inhibition of T cell functions. This agent may cause the opsonization and elimination of CD3-positive T cells from the circulation by mononuclear phagocytes in the liver and spleen. CD3 is part of the functional T cell receptor (TCR) complex, which is necessary for antigen recognition by T cells, and is required for signal transduction.
A nutritional supplement containing an extract of the skin of muscadine grape (Vitis rotundifolia), with anti-inflammatory, antioxidant and potential chemopreventive activities. The skin extract of the muscadine grape contains numerous phytochemicals including hydrolyzable tannins and flavonoids, such as anthocyanin 3,5-diglucosides, quercetin, myricetin, and kaempferol glycosides. Upon administration, muscadine grape skin extract (MSKE) appears to inhibit PI3K/Akt and MAPK signaling, eventually leading to apoptosis and a reduction in tumor cell proliferation.
Brand name for muscadine grape skin extract
A liquid, oromucosal formulation containing a muscarinic agonist with potential anti-xerostomia activity. Upon application to the inside lining of the mouth, muscarinic agonist APD515 may locally act on muscarinic receptors on the salivary glands and may stimulate the production of saliva thereby relieving dryness of the mouth.
Brand name for alprostadil
Brand name for mechlorethamine hydrochloride
An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) mutant forms, including substitution mutations at the arginine in position 132, IDH1(R132) (IDH1-R132), with potential antineoplastic activity. Upon administration, mutant IDH-1 inhibitor DS-1001 specifically inhibits certain mutant forms of IDH1, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH1 mutations. IDH1(R132) mutations are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG. DS-1001 minimally targets and affects wild-type IDH1, which is expressed in normal, healthy cells.
An orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity. Upon oral administration, mutant p53 activator COTI-2 targets and binds to the misfolded mutant forms of the p53 protein, which induces a conformational change that normalizes p53 and restores its activity. This induces apoptosis in tumor cells in which the p53 protein is mutated. In addition, COTI-2 inhibits the activation of Akt2 and prevents the activation of the PI3K/AKT/mTOR pathway, thereby inducing apoptosis in cancer cells in which this pathway is overexpressed. p53, a tumor suppressor protein, plays a key role in controlling cellular proliferation and survival. High levels of mutant p53 are seen in many cancers and are associated with uncontrolled cellular growth.
A cancer vaccine consisting of autologous dendritic cells which have been pulsed with a mutant p53 peptide. Vaccination with mutant p53 peptide pulsed dendritic cells may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing mutant p53, resulting in tumor cell lysis. Many tumor cells overexpress mutant p53 proteins, resulting in the loss of apoptosis regulation and abnormal cell proliferation.
An orally available, small molecule, third-generation, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms with potential antineoplastic activity. EGFR inhibitor PF-06459988 specifically binds to and inhibits mutant forms of EGFR, including the secondary acquired resistance mutation T790M, which prevents EGFR-mediated signaling and leads to cell death in EGFRm-expressing tumor cells. Compared to some other EGFR inhibitors, PF-06459988 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause dose-limiting toxicities that are seen with the use of non-selective EGFR inhibitors, which also inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
A cancer priming vaccine consisting of a proprietary version of the recombinant vaccinia viral vector, modified vaccinia Ankara-Bavarian Nordic (MVA-BN), encoding the human transcription factor and tumor-associated antigen (TAA) brachyury, and a triad of T-cell co-stimulatory molecules (TRICOM), which is comprised of the three human immune-enhancing co-stimulatory molecules B7-1, ICAM-1 and LFA-3, with potential immunostimulatory and antineoplastic activities. Upon subcutaneous administration of MVA-BN-brachyury vaccine, the vector expresses the brachyury protein. The expressed brachyury protein may induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells expressing brachyury. The MVA-BN-brachyury vaccine, which is a priming vaccine, is followed by multiple boosting doses of the fowlpox virus (FPV)-brachyury vaccine. The expression of brachyury, a member of the T-box family of transcription factors that is overexpressed in numerous cancer cell types, is correlated with increased epithelial-mesenchymal transition (EMT), cancer resistance, cancer progression and metastasis. TRICOM enhances antigen-specific T-cell activation.
A regimen consisting of methotrexate, vinblastine, doxorubicin, and cisplatin used for the treatment of advanced-stage urothelial carcinoma, including bladder cancer. (NCI Thesaurus]]
A cancer vaccine consisting of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the gene for the CD4 epitope-rich C-terminal domain of the Epstein Barr Virus (EBV) antigen EBNA1 and fused to the full-length of the EBV-associated antigen latent membrane protein 2 (LMP2), with potential immunostimulatory and antineoplastic activities. Upon administration, MVA EBNA1/LMP2 vaccine may elicit a cytotoxic T-cell immune response against cancer cells expressing EBNA1 and LMP2. Multi-antigen vaccine therapy may be more efficacious than single-antigen vaccine therapy. EBNA1, a sequence-specific DNA binding protein, plays an important role in EBV episomal genome maintenance and gene transactivation.
A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the suicide gene FCU1with potential antineoplastic activity. FCU1 is a bifunctional yeast cytosine deaminase (CD) / uracil phosphoribosyltransferase (UPRT) fusion gene. Upon intratumoral administration, MVA-FCU1 TG4023 enters tumor cells where FCU1 is expressed. Subsequently, the noncytotoxic prodrug 5-fluorocytosine (5-FC) is administered systemically and is deaminated by CD in FCU1- transduced tumor cells into 5-fluorouracil (5-FU), which is then directly metabolized to 5-fluoro-uridine monophosphate (5-FUMP) by UPRT; 5-FUMP may then be further transformed to 5-fluoro-deoxyuridine monophosphate (5-FdUMP), an irreversible inhibitor of thymidylate synthase and, so, DNA synthesis through deprivation of deoxythymidine triphosphate (dTTP). 5-FU and its active metabolites may then selectively kill tumor cells, avoiding toxicity in nonmalignant cells. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attenuated, replication-defective vaccinia strain incapable of virion assembly.
A cancer vaccine comprised of a modified, replication-defective, vaccinia virus Ankara (MVA) strain encoding the tumor-associated antigens (TAAs) human papillomavirus type 16 (HPV16) subtypes E6 and E7, and human interleukin-2 (IL-2), with potential immunostimulating and antineoplastic activities. Vaccination with MVA-HPV16E6/E7-IL2 vaccine TG4001 stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing HPV16 E6 and E7, resulting in tumor cell lysis. Expression of IL-2 augments the specific CTL response against HPV16 E6- and E7-expressing tumor cells.
A bivalent cancer vaccine comprised of a modified vaccinia virus Ankara (MVA) strain encoding human mucin 1 (MUC1) and interleukin-2 (IL-2) with potential immunostimulating and antineoplastic activities. Originally developed for the eradication of smallpox, MVA is a highly attenuated and replication-defective strain incapable of virion assembly and exerts potent immunostimulatory activity against antigens. Vaccination with MVA-MUC1-IL2 vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) responses against tumor cells expressing MUC1, a tumor associated antigen, resulting in tumor cell lysis. Expression of IL-2 augments the specific CTL response against MUC1 expressing cells.
A cancer vaccine consisting of a recombinant modified vaccinia Ankara (MVA) viral vector encoding genes for prostate specific antigen (PSA) and prostate acid phosphatase (PAP) with potential immunostimulatory and antineoplastic activities. Upon administration, MVA-PSA-PAP prostate cancer vaccine expresses PSA and PAP peptides, which may elicit humoral and cellular immune responses against prostate cancer cells expressing PSA and PAP. Multi-antigen vaccine therapy may be more efficacious than single-antigen therapy vaccine therapy.
Brand name for bevacizumab
A combination peptide vaccine of 2 chimeric peptides of the promiscuous T cell epitope derived from measles virus fusion protein (MVF; amino acid residues 288-302) co-synthesized with B-cell epitopes derived from the HER-2/neu a.a. 597-626 and HER-2/neu a.a. 266-296, with potential antineoplastic activity. Vaccination with MVF-HER-2(597-626)/MVF-HER-2(266-296) peptide vaccine may induce an active specific immune response, mounting a cytotoxic T-lymphocyte (CTL) response and an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress the HER-2 protein. The oncogenic protein HER-2, a member of the human epidermal growth factor receptor (EGFR) family of tyrosine kinases, is overexpressed in a variety of cancers and is correlated with increased tumor growth, progression and a poor prognosis. HER-2(597-626) corresponds to the binding site of trastuzumab on the extracellular domain IV of HER-2; HER-2 (266-296) corresponds to the binding site of pertuzumab on the dimerization loop of domain II of HER-2.
A two-component, anti-cancer vaccine containing irradiated tumor cells from a patient, and a capsule implanted with a genetically modified allogeneic cell line that continuously releases granulocyte-macrophage colony stimulating factor (GM-CSF), with potential immune-protective and -boosting activities. Upon subcutaneous injection of MVX-1-loaded macrocapsule/autologous tumor cell vaccine MVX-ONCO-1, the GM-CSF-secreting allogeneic cell capsules and the autologous irradiated cells isolated from the patient's tumor are co-localized in the patient's tissue. This permits the production of GM-CSF and exposes the immune system to the tumor-associated antigens (TAA) expressed by the autologous tumor cells at the injection site. Local expression of GM-CSF recruits and activates antigen-presenting cells (APC), which induces both antibody-dependent cell-mediated cytotoxicity (ADCC) and cytotoxic T-lymphocyte responses at the site of the injection and systemically. This may lead to tumor regression. By using the patient’s own irradiated cancer cells as vaccine antigens, the patient's immune system is exposed to the entire repertoire of this individual's TAAs. The encapsulated cell technology (ECT) of GM-CSF-secreting allogeneic cell capsules ensures the continuous release of GM-CSF. GM-CSF, a monomeric glycoprotein that functions as a cytokine, is a strong immune booster and plays an important role in the activation of immune system.
Brand name for clotrimazole
Brand name for clotrimazole
A proprietary preparation of mycobacterial DNA oligonucleotides embedded in mycobacterial cell wall fragments derived from cultures of Mycobacterium phlei, with potential immunomodulatory and antineoplastic activities. DNA oligonucleotides in the mycobacterial cell wall-DNA complex (MCC) induce apoptosis by increasing BAX protein levels, releasing cytochrome C from mitochondria, and activating caspase-3 and -7, which results in the cleavage of poly (ADP-ribose) polymerase and the release of nuclear matrix proteins. In addition to its pro-apoptotic effect, MCC activates monocytes and macrophages to produce various cytokines, including interleukin 6 (IL-6), IL-8, IL-12, IL-18, and tumor necrosis factor alpha (TNF-a). This results in the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTLs) and interferon gamma (IFN-gamma) synthesis.
An extract from Mycobacterium tuberculosis (M. tuberculosis) containing the polysaccharide arabinomannan, with potential immunostimulating activity. Upon administration of M. tuberculosis arabinomannan Z-100, this agent may activate the immune system by increasing the expression of various cytokines, such as interferon-gamma (IFNg) and interleukin-12. This inhibits the activity of suppressor T-cells, increases T helper 1 cell (Th1) activity and may restore the balance between Th1/Th2 cells. Additionally, Z-100 may inhibit metastasis and tumor cell proliferation.
An attenuated strain of Mycobacterium w, a non-pathogenic, rapidly growing, atypical mycobacterium, with non-specific immunopotentiating properties. In addition to sharing a number of common B and T cell determinants with Mycobacterium leprae and Mycobacterium tuberculosis, Mycobacterium w (Mw) also shares an immunogenic determinant with prostate specific antigen (PSA). In vitro and in vivo studies have shown that heat-killed Mw can induce significant T-cell responses. This agent may induce host T-cell responses against tumor cells expressing PSA. PSA is a glycoprotein secreted by prostatic epithelial and ductal cells and may be overexpressed in prostate cancer cells.
Brand name for rifabutin
The morpholinoethyl ester of mycophenolic acid (MPA) with potent immunosuppressive properties. Mycophenolate stops T-cell and B-cell proliferation through selective inhibition of the de novo pathway of purine biosynthesis. In vivo, the active metabolite, MPA, reversibly inhibits inosine 5'-monophosphate dehydrogenase, an enzyme involved in the de novo synthesis of guanine nucleotides. MPA displays high lymphocyte specificity and cytotoxicity due to the higher dependence of activated lymphocytes on both salvage and de novo synthesis of guanine nucleotides relative to other cell types.
An antineoplastic antibiotic derived from various Penicillium fungal species. Mycophenolic acid is an active metabolite of the prodrug mycophenolate mofetil. Mycophenolic acid inhibits inosine monophosphate dehydrogenase (IMPDH), preventing the formation of guanosine monophosphate and synthesis of lymphocyte DNA that results in inhibition of lymphocyte proliferation, antibody production, cellular adhesion, and migration of T and B lymphocytes. Mycophenolic acid also has antibacterial, antifungal, and antiviral activities.
A lipid nanoparticle-based formulation consisting of small-interfering RNAs (siRNAs) directed against the oncogene c-Myc encapsulated in lipids with potential antineoplastic activity. Upon intravenous administration of MYC-targeting siRNA DCR-MYC, the lipid formulation promotes the uptake by tumor cells where the siRNAs moieties are subsequently released. The siRNAs bind to c-Myc mRNAs, which may result in the inhibition of translation and expression of the c-Myc protein and leads to growth inhibition for tumor cells that are overexpressing c-Myc. c-Myc, a proto-oncogene overexpressed in a variety of cancers, is involved in cellular proliferation, differentiation, and apoptosis.
Brand name for mycophenolic acid
Brand name for magnesium hydroxide/aluminum hydroxide
Brand name for busulfan
Brand name for gemtuzumab ozogamicin
Brand name for idiotype-pulsed autologous dendritic cell vaccine APC8020
Brand name for gold sodium thiomalate
Brand name for mirabegron