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Dictionary of drugs: R
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
Drug dictionary R
The orally bioavailable solvate of the R-(-) enantiomer of gossypol and acetic acid with potential antineoplastic activity. As a BH3 mimetic, R-(-)-gossypol binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteins such as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Racemic gossypol is a polyphenolic compound isolated from cottonseed.
The R-isomer of a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent.
A skin care treatment system consisting of a cytokine-containing milk-based cooling gel and a cytokine-containing milk-based soothing lotion with hydrating and potential protective activity against radiation-induced dermatitis. Application of the R1 cooling gel immediately upon radiation treatment may hydrate the skin, provide cooling relief, and may protect the skin against radiation-induced dermatitis. The subsequent application of the R2 lotion moisturizes the skin while also protecting the skin against inflammation. In addition, R2 contains avobenzone, homosalate, octinoxate and octocrylene, which exert UVA and UVB skin protective activity.
A preparation of purified, pasteurized, gamma immune globulin obtained by the immunization of rabbits with human thymocytes, with T-cell depleting and immunosuppressive activities. Upon administration, rabbit anti-thymocyte globulin (rATG) specifically recognizes, modulates and destroys T lymphocytes. Although the exact mechanism of action by which rATG causes immunosuppression is not completely understood, it is likely caused by a combination of T-lymphocyte depletion and reduction in T-cell activation and their cytotoxic activities. Administering ATG with chemotherapy prior to stem cell transplantation may reduce the risk of graft-versus-host disease (GvHD).
The sodium salt of the prodrug rabeprazole, a substituted benzimidazole proton pump inhibitor, with potential anti-ulcer activity. After protonation, accumulation, and transformation to the active sulfenamide within the acidic environment of gastric parietal cells, rabeprazole selectively and irreversibly binds to and inhibits the H+, K+ATPase (hydrogen-potassium adenosine triphosphatase) enzyme system located on the parietal cell secretory surface, inhibiting gastric acid secretion.
An inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types.
The racemic form of a synthetic quinoxaline phenoxypropionic acid derivative with antineoplastic properties. XK469R selectively inhibits topoisomerase II by stabilizing the enzyme-DNA intermediates in which topoisomerase subunits are covalently linked to DNA through 5-phosphotyrosyl linkages, thereby interfering with DNA repair and replication, RNA and protein synthesis. This agent possesses unusual solid tumor selectivity and activity against multidrug-resistant cancer cells. XK469R is more water soluble and active than the pure isomers, R(+)XK469 and S(-)XK469.
An anti-idiotype murine monoclonal antibody (MoAb) specific to P3 MoAb with anti-metastatic effect. Racotumomab binds to the idiotype region of P3 MoAb and functionally mimics the three-dimensional structure of N-glycolyl ceramides of mono-sialyl lactose, the antigenic target of P3. As a result, this anti-idiotype antibody may stimulate the host immune system to elicit humoral and cellular immune responses against tumor cells expressing NeuGc-GM3 gangliosides, which are expressed in a wide variety of tumor cells.
Brand name for sodium hyaluronate topical hydrogel
A dinitroazetidine derivative with potential radiosensitizing activity. Upon administration, RRx-001 is able to dilate blood vessels, thereby increasing tumor blood flow and thus improving oxygenation to the tumor site. By increasing oxygen levels, these tumor cells may be more susceptible to radiation therapy. Tumor hypoxia is correlated with tumor aggressiveness, metastasis and resistance to radiotherapy. Check for '"active clinical trials using this agent.
A radiopharmaceutical composed of the dichloride salt of the alpha-emitting isotope radium Ra 223, with antineoplastic activity. Like calcium, radium targets bone tissue and preferentially accumulates in osteoblastic lesions, such as those seen in areas of bone metastases. Radium Ra 223 forms complexes with hydroxyapatite and becomes incorporated into the bone matrix. The radioisotope Ra 223 kills bone cancer cells through local emission of high energy alpha particles, causing DNA double-strand breaks and tumor regression in the skeleton. The short range effects of alpha emission allows for localized DNA damage with limited toxicity to nearby healthy bone tissue.
A traditional Chinese medicine comprising of Radix Angelicae Sinensis (RAS) and Radix Astragali (RA), with potential anti-inflammatory, immunostimulatory, neuroprotective, anti-hepatotoxic and antineoplastic activities. The main chemical constituents of RAS include ferulic acid, Z-ligustilide, butylidenephthalide and various polysaccharides. RA is the dried root of Astragalus membranaceus with primary constituents such polysaccharides, triterpenoids as well as isoflavones. Though their mechanisms of action remain largely elusive, Radix Angelicae Sinensis/Radix Astragali herbal supplements are commonly used for the treatment of various health conditions affecting women including premenstrual syndrome, dysmenorrhea, pelvic pain, recovery from childbirth and menopausal symptoms. These agents are also used for alleviating constipation, preventing and treating anemia and allergic attacks, and for the management of hypertension, joint pain and ulcers.
An orally available, hydrochloride salt form of radotinib, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature.
A replication-defective, recombinant adenoviral vector encoding the wild-type human tumor-suppressor protein p53 gene with potential antineoplastic activity. Upon intratumoral administration, rAD-p53 binds to the coxsakie-and-adenovirus receptor (CAR) on tumor cells and enters cells selectively via receptor-mediated endocytosis, which may result in the overexpression of wild-type p53 intracellularly and p53-mediated tumor regression. In addition, this agent may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against tumor cells, may activate natural killer (NK) cells to exert antitumor ‘bystander effects’ and may downregulate the expression of various oncogenes. The p53 protein blocks tumor cell cycle progression and directly initiates apoptosis; the p53 gene, a tumor suppressor gene, is deleted or mutated in a significant number of cancers.
An orally available inhibitor of members of the Raf family of serine/threonine protein kinases, with potential antineoplastic activity. Upon administration, Raf kinase inhibitor HM95573 binds to and inhibits the B-Raf mutant V600E and C-Raf. This inhibits B-Raf V600E- and C-Raf-mediated signal transduction pathways, thereby inhibiting tumor cell growth of susceptible tumor cells. In addition, HM95573 may also inhibit mutated Ras proteins. Raf protein kinases play a key role in the Raf/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. The Raf mutation B-Raf V600E, where the valine at residue 600 is substituted for glutamic acid, is frequently overexpressed in a variety of human tumors and results in the constitutive activation of the Raf/MEK/ERK signaling pathway. Check for '"active clinical trials using this agent.
An orally active, small molecule with potential antineoplastic activity. XL281 specifically inhibits RAF kinases, located downstream from RAS in the RAS/RAF/MEK/ERK kinase signaling pathway, which may result in reduced proliferation of tumor cells. RAS mutations may result in constitutive activation of the RAS/RAF/MEK/ERK kinase signaling pathway, and have been found to occur frequently in human tumors. Check for '"active clinical trials using this agent.
A protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity. Raf/MEK dual kinase Inhibitor RO5126766 specifically inhibits the kinase activities of Raf and MEK, resulting in the inhibition of of target gene transcription that promotes malignant transformation of cells. Both Raf and MEK are serine/threonine-specific kinases that respond to extracellular stimuli, such as mitogens, and are involved in the regulation of cellular processes, such as gene expression, mitosis, differentiation, and apoptosis.
The hydrochloride salt form of raloxifene, a selective benzothiophene estrogen receptor modulator (SERM) with lipid lowering effects and activity against osteoporosis. Raloxifene hydrochloride specifically binds to estrogen receptors in responsive tissue, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it promotes or suppresses the transcription of estrogen-regulated genes, thereby exerting its agonistic or antagonistic effects. This agent functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In tissue like bone, it decreases bone resorption and bone turnover and increases bone mineral density. Raloxifene hydrochloride acts as an estrogen antagonist in uterine and breast tissue. This agent also exerts an anti-proliferative effect on estrogen-sensitive breast cancer.
The orally bioavailable potassium salt of a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. Check for '"active clinical trials using this agent.
A quinazoline folate analogue with antineoplastic activity. After transport into cells via the reduced folate carrier, raltitrexed undergoes intracellular polyglutamation and blocks the folate-binding site of thymidylate synthase, thereby inhibiting tetrahydrofolate activity and DNA replication and repair and resulting in cytotoxicity.
A synthetic melatonin analogue with hypnotic and circadian rhythm-modulating activities. Ramelteon binds to and activates melatonin receptors 1 and 2 in the suprachiasmatic nucleus (SCN) of the brain, thereby promoting the onset of sleep. Unlike the nonbenzodiazepine sedative hypnotics zolpidem and zaleplon, this agent does not activate GABA receptors and, so, produces no GABA receptor-mediated anxiolytic, myorelaxant, and amnesic effects.
A prodrug and nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Ramipril is converted in the liver by de-esterification into its active form ramiprilat, which inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. This agent also causes an increase in bradykinin levels and a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis.
The hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. Upon administration, ramosetron selectively binds to and blocks the activity of 5-HT subtype 3 (5-HT3) receptors located in the vagus nerve terminal and in the vomiting center in the central nervous system (CNS), suppressing chemotherapy-induced nausea and vomiting.
A recombinant, fully human monoclonal antibody directed against human vascular endothelial growth factor receptor 2 (VEGFR-2) with antiangiogenesis activity. Ramucirumab specifically binds to and inhibits VEGFR-2, which may result in an inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells.
Brand name for ranolazine
A second-generation, recombinant humanized IgG1 kappa monoclonal antibody fragment directed against human vascular endothelial growth factor (VEGF) alpha. Ranibizumab binds to VEGF alpha and inhibits VEGF alpha binding to its receptors, VEGFR1 and VEGFR2, thereby preventing the growth and maintenance of tumor blood vessels. The molecular weight of this agent (48 kD) is much smaller than the molecular weight of bevacizumab (MW ~149 kD), allowing complete penetration of the retina and the subretinal space following intravitreal injection. In contrast to other anti-VEGF aptamers such as pegaptanib, ranibizumab has a high specificity and affinity for all soluble human isoforms of VEGF.
A chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells. Check for '"active clinical trials using this agent.
A member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.
A formulation containing the hydrochloride salt form of the non-imidazole histamine H2 receptor antagonist ranitidine, bismuth potassium citrate, and the hydrate form of sucralfate, a basic aluminum complex of sulfated sucrose, with potential antacid, radio- and cytoprotective activities. Upon oral administration of the ranitidine hydrochloride/bismuth potassium citrate/sucralfate hydrate formulation, ranitidine binds to and blocks the activity of the histamine H2 receptors in the parietal cells in the stomach and in the gastrointestinal (GI) tract, thereby decreasing acid secretion. Sucralfate physically binds to the surface of damaged mucosa, thereby forming a protective barrier that shields the GI tract from stomach acid. It also neutralizes stomach acid. Bismuth inhibits peptic activity, increases mucosal secretions and acts as a barrier to prevent damage by acid. Altogether, this protects against ulcer formation and may help to heal existing ulcers.
An orally available, piperazine derivative with anti-anginal and potential antineoplastic activities. Ranolazine’s mechanism of action for its anti-ischemic effects has yet to be fully elucidated but may involve the alteration of the trans-cellular late sodium current in the ischemic myocyte. By preventing the rise of intracellular sodium levels, ranolazine may affect the transport activity of sodium-dependent calcium channels and prevent the calcium overload during myocardial ischemia, thereby preventing cellular injury. Ranolazine’s potential antineoplastic effect may depend on its inhibitory effect on fatty acid oxidation, which may sensitize tumor cells to apoptosis and decrease tumor cell proliferation; fatty acid oxidation provides energy and promotes tumor cell proliferation and survival.
A natural homologue of ribonuclease A isolated from the eggs of the frog Rana pipiens. Ranpirnase primarily degrades cellular transfer RNA with a substrate specificity for uridine-guanidine base-pair sequences, resulting in inhibition of protein synthesis and cytotoxicity. This agent also activates caspase-9 in mitochondria, resulting in tumor cell apoptosis.
Brand name for silodosin
Brand name for sirolimus
A population of T lymphocytes polarized by rapamycin with potential immunomodulating activity. The autologous T cells collected from the patient were co-stimulated with antibodies to the T-cell cell surface proteins CD3 and CD28 and expanded ex vivo in the presence of rapamycin, an immunosuppressive drug, and then infused back into the same patient. Both CD3 and CD28 are required for full T cell activation. These lymphocytes expressed anti-apoptotic bcl-2 family member proteins (reduced Bax, Bak; increased phospho-Bad); maintained mitochondrial membrane potentials; and displayed reduced apoptosis. Adoptive transfer of this type of T cell potentially induces an anti-apoptotic Th1/Tc1 effector phenotype by promoting autophagy.
An orally bioavailable retinoid acid receptor alpha (RARalpha) agonist and vitamin A derivative, with potential antineoplastic activity. Upon administration, RARalpha agonist IRX5183 binds to and activates RARalpha, which promotes RARalpha-mediated signaling. This results in the transcription of RARalpha-responsive genes, which are responsible for cellular differentiation and proliferation. This results in the induction of cellular differentiation and apoptosis, and leads to the inhibition of cellular proliferation and tumorigenesis. RARalpha is a nuclear receptor and a member of the steroid receptor superfamily; reduced RARalpha signaling is correlated with cancer development in a variety of cancer cell types.
A cancer vaccine containing a RAS oncogene-encoded peptide with potential antineoplastic activity. RAS peptide cancer vaccine may stimulate a RAS peptide-specific antitumoral T-cell cytotoxic immune response, resulting in an inhibition of tumor cell proliferation and tumor cell death.
A recombinant urate oxidase enzyme isolated from a genetically-modified strain of Saccharomyces cerevisae. Urate oxidase catalyzes the oxidation of uric acid to the excretable mebolite allantoin, a molecule that is 5-10 times more water-soluble than uric acid. An enzyme that occurs endogenously in most mammals, urate oxidase is not found in humans.
A triazole with antifungal activity. Ravuconazole inhibits 14a demethylase, an enzyme involved in sterol synthesis, resulting in lysis of the fungal cell wall and fungal cell death.
A longer-acting antibody directed against terminal complement protein C5, with potential anti-inflammatory activity. Upon administration, ravulizumab-cwvz binds to terminal complement protein C5, thereby blocking C5 cleavage into pro-inflammatory components and preventing the complement-mediated destruction of red blood cells (RBCs) as seen in paroxysmal nocturnal hemoglobinuria (PNH). Compared to other anti-C5 antibodies, ALXN1210 is longer-acting and allows for monthly dosing. C5, a complement pathway protein, is expressed at high levels by the liver.
Brand name for modified-release calcifediol capsule
Brand name for reduced glutathione-L-cysteine-anthocyanins gel
Brand name for galantamine hydrobromide
An orally bioavailable bis-dioxopiperazine and a derivative of the chelating agent ethylenediaminetetraacetic acid (EDTA) with antineoplastic, antiangiogenic, and antimetastatic activities. Razoxane specifically inhibits the enzyme topoisomerase II without inducing DNA strand breaks, which may result in the inhibition of DNA synthesis and cell division in the premitotic and early mitotic phases of the cell cycle. This agent may also exhibit antiangiogenic and antimetastatic activities although the precise molecular mechanisms of these actions are unknown.
An immunochemotherapy regimen consisting of rituximab, cyclophosphamide, hydroxydaunorubicin hydrochloride (doxorubicin hydrochloride), vincristine (Oncovin) and prednisone used to treat both indolent and aggressive forms of non-Hodgkin lymphoma.
A regimen consisting of rituximab, cyclophosphamide, vincristine, and prednisone used to treat indolent non-Hodgkin lymphoma.
An synthetic compound containing the organic phosphonate hydroxyethylidene diphosphonate (HEDP) labeled with the radioisotope rhenium Re 186. Re-186 hydroxyethylidene diphosphonate binds to hydroxyapatitie in bone, delivering a cytotoxic dose of beta radiation to primary and metastatic bone tumors. Re-186 is a beta emitter with a short half-life, a radioisotope profile that provides localized antitumor radiocytotoxicity while sparing extramedullary bone marrow tissues.
An orally bioavailable, traditional Chinese medicine (TCM)-based formulation composed of Realgar-Indigo naturalis formula (RIF) with potential antineoplastic activity. The main constituents in RIF are realgar, Indigo naturalis, and Salvia miltiorrhiza, with tetraarsenic tetrasulfide (As4S4), indirubin and tanshinone IIA as the main active ingredients, respectively, which appear to exert synergistic effects on cancer cells. Tetraarsenic tetrasulfide specifically induces the ubiquitination and degradation of the oncoprotein promyelocytic leukemia retinoic acid receptor alpha (PML-RARalpha). In addition, the active ingredients in the Realgar-Indigo naturalis formulation enhance the expression of myeloid differentiation genes, and induce G(1)/G(0) cell cycle arrest. PML-RARalpha, an acute promyelocytic leukemia (APL)-specific fusion gene, inhibits differentiation and promotes survival of myeloid precursor cells.
A quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.
An orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. Rebastinib binds to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation; in addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and the receptor tyrosine kinases TIE-2 and VEGFR-2. Rebastinib may exhibit more potent activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis, respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety of cellular responses including differentiation, division, adhesion, and the stress response.
Brand name for ribavirin
A sulfhydryl-based second-generation matrix metalloproteinase (MMP) inhibitor with potential antineoplastic activity. Rebimastat selectively inhibits several MMPs (MMP 1, 2, 8, 9, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
Brand name for cediranib maleate
A recombinant peptide that is chemically identical to or similar to the endogenous 70-kD heat shock protein (HSP70). HSP70 is a molecular chaperone that prevents physiologic stress-induced cell death by inhibiting both caspase-dependent and caspase-independent apoptosis. Because this peptide is often overexpressed in tumor cells, autologous vaccination with HSP70 derived from tumor cells may stimulate the host immune system to mount a tumoricidal cytotoxic T lymphocyte (CTL) response. Check for '"active clinical trials using this agent.
A recombinant replication-defective adenovirus which encodes the gene for the cytokine human interferon-beta (IFN-beta). Once inserted into and replicating in host tumor cells, recombinant adenovirus-hIFN-beta expresses human IFN-beta, which may stimulate an antiproliferative natural killer (NK) cell response against tumor cells and induce caspase-mediated tumor cell apoptosis.
A replication-deficient recombinant adenovirus encoding human interferon alpha-2b with potential antineoplastic activity. Upon intravesical administration, recombinant adenovirus-interferon SCH 721015 infects nearby tumor cells and expresses INF alpha-2b intracellularly which activates the transcription and translation of genes whose products mediate antiviral, antiproliferative, antitumor, and immune-modulating effects.
A non-replicating recombinant adenovirus type 5 (Ad5)-vector encoding the gene for interferon alpha-2b (IFNα2b) and the gene transfer enhancement agent Syn 3, with potential antineoplastic activity. Upon intravesical administration, recombinant adenovirus-interferon with Syn3 transfects both cancerous and normal bladder cells, and the adenovirus secretes interferon (IFNα2b) into the bladder. IFN exerts a direct antitumor killing effect and a bystander effect, thereby killing adjacent, non-transfected cancerous bladder cells. Syn 3 enhances the ability of the adenoviral vector to transfect cells.
A replication-defective adenovirus containing a gene that encodes the human protein L523S with potential antineoplastic activity. Upon administration, recombinant adenovirus-L523S vaccine expresses L523S, which may stimulate antibody and cytotoxic T lymphocyte (CTL) responses against tumor cells expressing L523S. L523S is an RNA-binding protein that belongs to the KOC (K homology domain containing protein over-expressed in cancer) family of proteins. As an oncofetal protein, L523S is normally expressed in early embryonic tissues and certain normal adult tissues such as colon, fallopian tube, gall bladder, and ovary tissues but may be overexpressed in squamous cell cancers of the lung.
A genetically-engineered adenovirus that contains the gene that encodes the human tumor-suppressor protein p53 with potential antineoplastic activity. Recombinant adenovirus-p53 SCH-58500 delivers p53 into tumor cells, which may result in p53-mediated cell cycle arrest and apoptosis.
An orally available, genetically engineered Salmonella typhimurium strain expressing a truncated form of the human cytokine interleukin-2 (IL-2) gene, with antitumor activity. Upon administration of recombinant attenuated S. typhimurium expressing IL-2 (SalpIL2), this Salmonella strain may selectively accumulate and divide in a variety of tumor types, and express IL-2. In turn, IL-2 may induce natural killer (NK) cell proliferation thereby enhancing their activity. This may inhibit the growth of tumor cells.
A recombinant vaccine containing a genetically detoxified adenylate cyclase toxin (CyaA) of Bordetella pertussis coupled, through its catalytic site, to the melanoma tyrosinase A2 epitope YMDGTMSQV, with potential antineoplastic activity. Via the toxin moiety, the recombinant B. pertussis adenylate cyclase toxin-tyrosinase A2 epitope specifically binds to the alphaMbeta2 integrin (CD11b/CD18) located on CD11b-positive antigen-presenting cells (APC). Upon processing and presentation of the melanoma-specific epitope by MHC class I molecules to the surface of these APCs, a specific cytotoxic T-cell (CTL) response against tumor cells expressing tyrosinase may be initiated, resulting in decreased tumor growth and cell lysis.
A recombinant, bispecific, single chain antibody directed against both the T-cell surface-associated costimulatory molecule CD28 and a melanoma-associated proteoglycan (MAPG) with potential antitumor activity. By targeting both CD28 and MAPG, recombinant bispecific single-chain antibody rM28 enhances cytotoxic T-cell recognition of melanoma cells, which may result in immune effector cell-mediated tumor cell death and a decrease in distant metastases. This agent appears to have a long serum half-life secondary to the formation of dimers. When activated, CD28 facilitates interactions between T-cells and other immune effector cells resulting in cytotoxic T-lymphocyte responses; MAPG is a surface antigen expressed on the majority of melanomas, including primary cutaneous, ocular and metastatic melanomas.
A recombinant therapeutic agent which is chemically identical to or similar to CD40-ligand. CD40-ligand, also known as CD40L/TRAP and CD154, is a type II membrane protein which binds to CD40, a cell surface receptor that belongs to the tumor necrosis factor receptor family; CD40 is expressed on B lymphocytes, monocytes, dendritic cells (DC), hematopoietic progenitors, endothelial cells and epithelial cells. Recombinant CD40-ligand may be used to activate DC ex vivo via CD40 binding; CD40-ligand-activated DC may provide or augment a protective antitumor immunity when administered in dendritic cell cancer vaccines.
A recombinant sialidase fusion protein composed of a sialidase catalytic domain derived from Actinomyces viscosus, a constituent of the normal oral and gastrointestinal flora in humans, fused to a cell surface-anchoring domain, with potential anti-viral activity. Following administration by oral inhalation, DAS181 proteolytically removes sialic acid from the airway epithelium, which inhibits viral binding to and internalization by cells of the respiratory epithelium and prevents viral replication. The cell surface anchoring-domain of this agent may increase retention time and drug potency. Sialic acids in the respiratory tract are used by influenza and parainfluenza viruses to invade airway epithelial cells.
A cancer vaccine consisting of a truncated recombinant HER2 peptide (dHER2) with potential antineoplastic activity. Upon administration, recombinant dHER2 vaccine may stimulate the host immune response to mount a cytotoxic T-lymphocyte response against tumor cells that overexpress the HER2 protein, resulting in tumor cell lysis. The HER2 protein is a tumor-associated antigen (TAA) that is overexpressed in a variety of cancers. dHER2 includes the extracellular domain (ECD) and a part of the intracellular domain (ICD) of the HER2 protein.
A plasmid DNA encoding human L523S, an RNA-binding protein that belongs to the KOC (K homology domain containing protein overexpressed in cancer) family, with potential antineoplastic activity. Vaccination with L523S DNA may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express the L523S protein. As an oncofetal protein, L523S is normally expressed in early embryonic tissue, but is overexpressed in certain cancer cell types.
A recombinant fusion protein composed of the full-length extracellular domain (soluble) of human receptor tyrosine kinase ephrin type-B receptor 4 (sEphB4) and fused, at its C-terminus, to full-length human serum albumin (HSA), with potential antineoplastic and anti-angiogenic activities. sEphB4-HSA functions as a decoy receptor for the membrane-bound ligand Ephrin-B2 (Efnb2) and interferes with the binding of Efnb2 to its native receptors, including EphB4 and EphA3. This may result in a reduction of angiogenesis and a reduction in cell growth of Efnb2 and/or EphB4 over-expressing tumor cells. In addition, this agent also prevents the angiogenic effects of numerous growth factors due to interactions between Efnb2 and EphB4. Efnb2 and EphB4 are overexpressed in a variety of tumor cell types; the bi-directional signaling of Efnb2-EphB4 plays an important role in angiogenesis and tumor cell migration, invasion, and proliferation. Albumin reduces this agent’s degradation, improves circulation time and may thus improve efficacy.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine Flt3. Flt3 ligand binds to the Flt3 tyrosine kinase receptor and, synergistically with other growth factors, stimulates the proliferation and mobilization of certain bone marrow precursor cells, including CD34+ cells, and dendritic cells. When proteolytically cleaved, the transmembrane isoform of Flt3 ligand generates the soluble form soluble Flt3 ligand , which is also biologically active. Check for '"active clinical trials using this agent.
A cancer vaccine adjuvant consisting of a recombinant fowlpox virus encoding human granulocyte-macrophage colony-stimulating factor (GM-CSF). GM-CSF binds to specific cell surface receptors on various immuno-hematopoietic cell types, enhancing their proliferation and differentiation and stimulating macrophage and dendritic cell functions in antigen presentation and antitumor cell-mediated immunity. Administration of recombinant fowlpox GM-CSF vaccine adjuvant may induce an immune response against tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the stimulatory molecule transgene B7-1. Recombinant fowlpox-B7.1 (rF-B7.1) vaccine may enhance antigen presentation and activate antitumoral cytotoxic T-cells.
A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM). This agent may enhance CEA presentation to antigen presenting cells (APC) and activate cytotoxic T-cells against CEA-expressing tumors.
A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA). Administration of this agent may stimulate a cytotoxic T cell response against PSA-expressing tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
A cancer vaccine comprised of a recombinant fowlpox virus vector encoding TRICOM. TRICOM is comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3) that may enhance antigen presentation and activate cytotoxic T-cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
A recombinant fowlpox virus vaccine with potential antineoplastic activity. Binding to the melanoma antigen tyrosinase, recombinant fowlpox-tyrosinase vaccine generates cellular immune responses against melanoma cells expressing the tyrosinase antigen; this effect is enhanced by the co-administration of interleukin 2 (IL-2). Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
A long-acting recombinant fusion protein composed of human serum albumin (HSA) fused to granulocyte colony stimulating factor (G-CSF), with potential granulopoietic activity. Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, thereby stimulating the proliferation, differentiation, function, and survival of neutrophil precursors and mature neutrophils. This may prevent granulocytopenia. HSA fusion increases the molecular weight of G-CSF, prolongs its half-life and masks G-CSF, thereby preventing G-CSF degradation which further increases the half-life and bioavailability of G-CSF. Check for '"active clinical trials using this agent.
A recombinant chaperone-peptide complex-based vaccine composed of a complex between heat shock protein hsp110 and the human melanoma-associated antigen gp100, with potential antineoplastic activity. Upon vaccination, recombinant hsp110-gp100 chaperone complex activates the immune system to exert a cytotoxic T cell immune response and antigen-specific interferon-gamma production against gp100-overexpressing cancer cells. Gp100, is overexpressed in a variety of cancer cell types. Hsp110, binds to and chaperones full-length proteins during heat shock; as an immunoadjuvant it is able to enhance an immune response against antigen(s) and stimulate T-lymphocyte activation.
A therapeutic recombinant analogue of a member of the endogenous CC chemokines with potential antineoplastic activity. Expressed by various lymphoid tissues, endogenous 6Ckine is chemotactic for B and T lymphocytes and dendritic cells.
A replication selective, recombinant, E1B and partial E3 gene deleted form of human adenovirus type 5, with potential antineoplastic activity. Upon intratumoral injection of recombinant human adenovirus type 5, the adenovirus selectively replicates in cancer cells while preventing viral replication in normal, healthy cells. This induces a selective adenovirus-mediated cytotoxicity in cancer cells, which leads to cancer cell lysis. In addition, viral spread to adjacent cells, following lysis of infected cells, may activate the immune system to kill the infected tumor cells. The E1B protein causes p53 inactivation, which promotes viral replication; deletion of E1B allows for p53 activation in normal cells, which prevents viral replication in normal, healthy cells. The mutation and subsequent inactivation of p53 in cancer cells enables the E1B-deleted adenovirus to selectively replicate in cancer cells. Partial deletion of E3, encoding the adenovirus death protein, enhances the safety profile of the administered adenovirus. Check for '"active clinical trials using this agent.
A long-acting recombinant fusion protein incorporating human serum albumin (HSA)-derived and human granulocyte colony stimulating factor (G-CSF)-derived moieties with potential granulopoietic activity. G-CSF, a naturally occurring cytokine, stimulates the production of granulocytes and stem cells in the bone marrow and their release into the blood; it also stimulates the differentiation, function, and survival of neutrophil precursors and mature neutrophils. Albumin fusion may promote an increased serum half-life and bioavailability of the G-CSF moiety of this fusion protein. Check for '"active clinical trials using this agent.
A recombinant, soluble glycosylated form of human angiotensin converting enzyme 2 (rhACE2) with antihypertensive and potential antineoplastic activities. Recombinant human angiotensin converting enzyme 2 APN01 may normalize ACE2 levels, cleaving angiotensin II to create angiotensin-(1-7) and restoring the function of the renin-angiotensin system (RAS). ACE2, a homolog of ACE1, appears to function as a negative regulator of the RAS system by converting angiotensin II to angiotensin-(1-7), a peptide with actions that counteract the cardiovascular actions of angiotensin II. In addition, angiotensin-(1-7) may inhibit cyclooxygenase 2 (COX-2) and the production of proinflammatory prostaglandins and may activate the angiotensin-(1-7) G protein-coupled receptor Mas, resulting in diminished tumor cell proliferation. ACE2 levels may be reduced in malignancy and diabetes and in liver, cardiovascular and lung diseases.
A recombinant form of human bone morphogenetic protein 2 (rhBMP-2), with potential bone remodeling and osteoinductive activities. Following administration, rhBMP-2 induces BMP-2 signaling cascades, which leads to osteoblast differentiation, enhancement of bone repair and formation, and improvement of re-vascularization. This promotes bone healing. BMP-2, a protein belonging to the transforming growth factor beta (TGFb) superfamily of proteins, plays a key role in bone and cartilage formation. Check for '"active clinical trials using this agent.
A recombinant form of human bone morphogenetic protein 4 (rhBMP4; rhBMP-4), with potential antineoplastic activity. Upon administration, rhBMP4 binds to BMP receptors (BMPRs) and activates BMP-mediated signal transduction pathways. This may lead to the transcription of BMP4-target genes and to inhibition of the proliferation of certain tumor cell types. Additionally, rhBMP4 binding promotes the differentiation of normal stem cells and decreases both differentiation and renewal of cancer stem cells (CSCs). BMP4, an extracellular signaling molecule belonging to the transforming growth factor beta (TGFb) superfamily, plays a key role in bone formation. It also plays a role in the pathogenesis of certain cancers; BMP4 suppresses growth of certain types of cancer cells, and is also able to induce migration, invasion, and epithelial-mesenchymal transition (EMT), which may promote cancer metastasis and progression.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous glycoprotein hormone human chorionic gonadotropin (HCG). HCG binds to cells of the corpus luteum, thereby stimulating progesterone production and helping to maintain a secretory endometrium.
A peptide vaccine preparation, containing recombinant human epidermal growth factor (rEGF) linked to the Neisseria meningitidis-derived recombinant immunogenic carrier protein P64k (rP64k) and mixed with the immunoadjuvant Montanide ISA 51, with potential active immunotherapy activity. Recombinant human EGF-rP64K/Montanide ISA 51 vaccine may trigger a humoral immune response against vaccine rEGF and rP64K and, so, against endogenous EGF. Antibody-mediated inhibition of endogenous EGF binding to its receptor, epithelial growth factor receptor (EGFR), may result in the inhibition of tumor cell proliferation.
A recombinant human proteolytic fragment of the C-terminal end of type XVIII collagen. Endostatin induces microvascular endothelial cell apoptosis and inhibits endothelial proliferation and angiogenesis, which may result in a reduction in tumor burden. This agent also may decrease hepatic metastasis by inhibiting proinflammatory cytokines and vascular cell adhesion molecule (VCAM)-dependent cell attachment to the hepatic microvasculature.
A recombinant form of the naturally-occurring polypeptide human epidermal growth factor with potential epithelial regenerative and cytoprotective activities. Upon topical application, recombinant human epidermal growth factor (rhEGF) may stimulate epithelial proliferation, differentiation and migration, which may result in the acceleration of epithelial regeneration and wound healing. In addition, rhEGF may attenuate epithelial cytotoxicities related to chemotherapy and/or radiotherapy. Check for '"active clinical trials using this agent.
An immunocytokine consisting of human pro-inflammatory cytokine tumor necrosis factor alpha (TNFalpha) fused to a human single-chain variable fragment (scFv) directed against the extra-domain B (ED-B) of fibronectin (L19), with potential immunopotentiating and antineoplastic activities. The L19 moiety of recombinant human fusion protein L19TNFalpha binds to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. In turn, the TNFalpha moiety may locally induce an immune response against ED-B fibronectin-expressing tumor cells and may specifically decrease the proliferation of ED-B-expressing tumor cells. ED-B is predominantly expressed during angiogenesis and tumor growth.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine granulocyte colony-stimulating factor (G-CSF). Secreted by monocytes, macrophages and neutrophils and other cells after activation, G-CSF stimulates the proliferation and differentiation of hematopoietic progenitor cells committed to the neutrophil/ granulocyte lineage.
A human recombinant form of the naturally occurring human enzyme hyaluronidase with potential chemoadjuvant activity. Upon local administration, recombinant human hyaluronidase hydrolyzes hyaluronic acid, a glucosaminoglycan responsible for the viscosity of the interstitial barrier. The digestion of hyaluronic acid lowers the viscosity in the interstitial space, thereby increasing permeability and facilitating local penetration of chemotherapeutic agents into cancer cells.
A long-acting immunoglobulin (Ig) fusion protein composed of a recombinant form of the endogenous human protein interleukin-7 (rhIL-7) and fused to a hybrid Fc (hyFc) region of a human antibody, with hematopoietic and immunopotentiating activities. Upon administration of recombinant human IL-7-hyFc NT-I7, IL-7 stimulates the proliferation, differentiation, trafficking and survival of a variety of T-cell subsets, including naive, central memory (CM), effector memory (EM), terminally differentiated effector memory (TEMRA) and natural killer (NK) T cells, and enhances T-cell-mediated anti-tumor immune responses. Compared to rhIL-7 alone, fusion to the hyFc region enhances the half-life of IL-7. The hyFc region is composed of the hinge and N-terminal portion of heavy chain constant (CH) region 2 (hinge-CH2) of human IgD, which is fused to the C-terminal region of CH2 and the entire CH3 region of human IgG4.
A recombinant agent that is chemically identical or similar to the endogenous cytokine interleukin-15 (IL-15) with immunomodulating activity. IL-15, secreted by mononuclear phagocytes (and some other cell types) following viral infection, regulates T and natural killer cell activation and proliferation. This cytokine induces activation of transcription activators STAT3, STAT5, and STAT6 via JAK kinase signal transduction pathways in mast cells, T cells, and dendritic epidermal T cells. IL-15 and interleukin-2 (IL-2) are structurally similar and share many biological activities; both may bind to common hematopoietin receptor subunits, negatively regulating each other's activity. CD8+ memory T cell number has been shown to be regulated by a balance between IL-15 and IL-2.
A recombinant fusion protein consisting of human cytokine interleukin 22 (IL-22) fused to a human immunoglobulin G2 (IgG2)-Fc, with potential cell protective activity. Upon intravenous administration of recombinant human IL-22 IgG2-Fc, IL-22 binds to its cognate receptor IL-22R, which is highly expressed in parenchymal tissues and epithelial cells at mucosal surfaces. This leads to the activation of IL-22/IL-22R-mediated signal transduction pathways, and results in the activation of signal transducer and activator of transcription 3 (STAT3). STAT3 activation may have a protective and regenerative effect and may protect against the development of various inflammatory and immunological diseases. Specifically, recombinant human IL-22 IgG2-Fc may protect intestinal stem cells from dying due to acute graft-versus-host disease (aGvHD). IL-22, produced by various immune cells and upregulated during inflammation, plays a key role in controlling immune responses and bacterial infection, and in the enhancement of intestinal barrier function, gut immunity, and tissue repair.
A recombinant protein similar or identical to human mannan-binding lectin (MBL) with opsonin activity. MBL, a soluble pattern recognition receptor (PRR) collectin in the C-type lectin superfamily, is a plasma protein that plays an important role in innate immunity; MBL contains a carbohydrate recognition domain at one end and a collagen-like stalk domain at the other. Upon MBL binding to mannose residues on mannose-containing polysaccharides (mannans) on the surfaces of a microorganisms, activation of the complement system results in the deposition of complement components (opsonization) and the clearance of the opsonized microorganisms by phagocytic cells. MBL is part of the mannan-binding lectin pathway (also known as the Ali/Krueger pathway), which has similarities to the classical complement pathway in that activation of C4 and C2 produce activated complement proteins further down the complement cascade. However, unlike the classical complement pathway, activation of this pathway is not antibody dependent.
A recombinant, bivalent, human papillomavirus (HPV) vaccine, containing virus-like particles for HPV types 16 and 18 linked to the adjuvant ASO4, with potential immunoprotective and antineoplastic properties. Upon administration, recombinant human papillomavirus bivalent vaccine may generate humoral and cellular immunity against HPV types-16 and -18 antigens, thereby preventing cervical infection upon exposure to HPV types 16 and 18. In addition, this agent may stimulate an antitumoral cellular immune response against cervical cancer associated with HPV infection.
A non-infectious, recombinant, nonavalent vaccine prepared from highly purified virus-like particles (VLPs) comprised of the major capsid (L1) proteins from human papillomavirus (HPV) types 6, 11, 16, 18, 31, 33, 45, 52, and 58, with active immunizing activity. Upon administration, the recombinant HPV nonavalent vaccine activates the immune system to produce antibodies against the 9 HPV types. This protects against HPV infection and HPV-related cancers. Altogether, HPV types 6, 11, 16, 18, 31, 33, 45, 52, and 58 account for the majority of the HPV types that cause cervical, vulvar, vaginal and anal cancers.
A non-infectious recombinant, quadrivalent vaccine prepared from the highly purified virus-like particles (VLPs) of the major capsid (L1) protein of human papillomavirus (HPV) Types 6, 11, 16, and 18 with immunoprophylactic activity. The immunoprohylactic efficacy of L1 VLP vaccines, such as recombinant human papillomavirus quadrivalent vaccine, appear to be mediated by the development of humoral immune responses. HPV Types 16 and 18 account for approximately 70% of cervical cancers and HPV Types 6 and 11 account for approximately 90% of genital warts.
A fully recombinant form of the human pentraxin 2 (PTX2) protein with potential antifibrotic activity. Upon intravenous administration, recombinant human serum amyloid P/pentraxin 2 (PRM-151) may inhibit myofibroblast generation by preventing the differentiation of circulating monocytes into fibrocytes and profibrotic macrophages. PTX2 is a circulating plasma protein that belongs to the class of pattern recognition receptors (PRR) of the innate immune system.
A therapeutic glycoprotein cytokine chemically identical to or similar to endogenous human stem cell factor with hematopoietic activity. Recombinant human stem cell factor (rhSCF) binds to the receptor tyrosine kinase c-kit, which may stimulate the growth of peripheral blood progenitor cells (PBPCs). This agent works synergistically with other hematopoietic growth factors. rhSCF may promote bone marrow recovery after myeloablative therapies and procedures.
One of a group of recombinant therapeutic glycoprotein cytokines with antiviral, anti-proliferative, and immunomodulating activities. Interferons bind to specific cell-surface receptors, leading to the transcription and translation of genes with interferon-specific response elements (ISREs). The resultant proteins mediate many complex effects, ultimately leading to inhibition of viral protein synthesis and cellular growth, alteration of cellular differentiation, interference with oncogene expression, activation of natural killer cells, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity. The production of endogenous interferons is induced in response to foreign agents such as bacteria, viruses and parasites and to tumor cells.
A class of naturally-isolated or recombinant therapeutic peptides used as antiviral and anti-tumor agents. Alpha interferons are cytokines produced by nucleated cells (predominantly natural killer (NK) leukocytes) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes containing an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral effects (viral protein synthesis); antiproliferative effects (cellular growth inhibition and alteration of cellular differentiation); anticancer effects (interference with oncogene expression); and immune-modulating effects (natural killer cell activation, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity).
A non-glycosylated recombinant interferon with antiviral and antineoplastic activities. Alfa interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects.
A proprietary recombinant protein highly resembling human interferon alpha 2b (IFN-a2b), with potential anti-tumor, anti-inflammatory, immunomodulating and antiviral activities. Upon injection, recombinant IFN alpha 2b-like protein binds to specific IFN alpha cell surface receptors. This activates interferon-mediated signal transduction pathways and induces the transcription and translation of genes with interferon-specific response elements (ISREs). This may activate the immune system, including the activation of natural killer cells (NKs) and may result in an inhibition of tumor cell proliferation, tumor angiogenesis, metastasis and an induction of apoptosis. Compared to human IFN-a2b (HuINF-a2b), this agent exhibits enhanced antiviral and antiproliferative activities. In addition, this agent exhibits antiviral activity against a variety of viruses, including hepatitis B and C viruses, human immunodeficiency virus (HIV) and Avian Influenza.
The non-glycosylated recombinant interferon alpha, subtype 1b, with immunostimulatory and antineoplastic activities. Alpha interferon-1b binds to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects.
A non-glycosylated recombinant human alpha interferon, subtype 2a, produced in the bacterium E. coli. Interferon alpha-2a binds to its specific cell-surface receptor, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune modulating effects. Check for '"active clinical trials using this agent.
A recombinant protein which is chemically identical to or similar to endogenous interferon beta with antiviral and anti-tumor activities. Endogenous interferons beta are cytokines produced by nucleated cells (predominantly natural killer cells) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes with an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral (the most important being inhibition of viral protein synthesis), antiproliferative and immune modulating effects. The recombinant therapeutic forms of interferon beta are interferon beta 1-a and interferon beta 1-b.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous lymphokine interferon gamma (IFN-gamma) with antineoplastic, immunoregulatory, and antiviral activities. Therapeutic IFN-gamma binds to and activates the cell-surface IFN-gamma receptor, stimulating antibody-dependent cytotoxicity and enhances natural killer cell attachment to tumor cells. This agent also activates caspases, thereby inducing apoptosis in malignant cells.
A recombinant form of the endogenous heterodimeric cytokine interleukin-12 with potential antineoplastic activity. Recombinant interleukin-12 binds to and activates its cell-surface receptor, stimulating the production of interferon-gamma (IFN) which, in turn, induces IFN-gamma-inducible protein-10 (IP-10) and so inhibits tumor angiogenesis.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-18 (IL-18). Produced primarily by macrophages, IL-18 induces the production of interferon-gamma (IFN-gamma), and enhances the activity of natural killer (NK) and cytotoxic T lymphocytes (CTL). As a potential immunotherapeutic agent, IL-18 displays antitumor effects in vitro and in animal models.
A recombinant agent which is chemically identical to or similar to the endogenous protein cytokine interleukin-1 (IL-1). The IL-1 precursor is produced by monocytes, activated macrophages, and other cell types; mature IL-1 is generated by proteolytic cleavage by proteases such as IL-1-beta converting enzyme (ICE). This agent enhances T cell proliferation and B cell growth and differentiation and induces the expression of proinflammatory cytokines.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous protein cytokine interleukin 1 (IL-1)-beta. Produced by monocytes and activated macrophages, endogenous mature IL-1 is generated through proteolytic cleavage by proteases such as IL-1-beta converting enzyme (ICE). This agent promotes angiogenesis, fibroblast proliferation, and neutrophil chemotaxis; it also regulates the functions of lymphocytes and epithelial cells and is involved in the 'acute phase response' to infection.
A recombinant form of interleukin-3, a cytokine produced by activated T-cells and mast cells involved in intercellular communication, hematopoiesis, and inflammation. IL-3 binds and activates specific receptors on hematopoietic cells and in the nervous system, triggering expression of specific genes via the Ras signaling pathway and through Jak2 activation. This agent stimulates the proliferation of pluripotent hematopoietic progenitor cells.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-4 (IL-4). Produced primarily by activated T-cells, IL-4 binds to and activates its cell-surface receptor, stimulating the proliferation and differentiation of activated B-cells and enhancing their ability to present antigens to T-cells. As a potential immunotherapeutic agent, recombinant IL-4 also augments the effects of other cytokines on dendritic cells (DC), cytotoxic T lymphocytes (CTL), and tumor-infiltrating lymphocytes (TIL).
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-6 (IL-6) with antiapoptotic, proinflammatory, antiinflammatory, proproliferative and proangiogenic activities. IL-6 binds to its receptor (IL-6R), activating a receptor-CD130 receptor complex; the CD130 portion of the complex is a signal transduction protein that activates JAK kinases and ras-mediated signaling pathways, which in turn activate downstream signaling pathways, resulting in the activation of various transcription factors (STAT, ELK-1, NF-IL-6, etc.) and gene transcription. The physiological effects of IL-6 are complex and varied and include hematopoietic, pyrogenic and thermogenic, proinflammatory, antiinflammatory, proproliferative (anti-apoptotic), and angiogenic effects. Check for '"active clinical trials using this agent.
A recombinant protein which is chemically identical to or similar to endogenous interleukin-7 (IL-7) with hematopoietic and immunopotentiating properties. Produced by bone marrow, thymic stromal, and spleen cells, the cytokine interleukin-7 is a hematopoietic growth factor for progenitor B cells and T cells and stimulates proliferation and differentiation of mature T-cells and natural killer cells. Check for '"active clinical trials using this agent.
A cocktail preparation of synthetic interleukin (IL) -1, IL-2, IL-6 , tumor necrosis factor (TNF)-alpha, interferon gamma and other cytokines that are chemically identical to or similar to signaling molecules secreted by leukocyte cells. Leukocyte interleukins are essential in many immune responses, such as antibodies production, modulating secretion of other cytokines, and activation of bone marrow stem cells. Check for '"active clinical trials using this agent.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous protein cytokine macrophage colony-stimulating factor (M-CSF). Synthesized endogenously by mesenchymal cells, M-CSF stimulates the survival, proliferation, and differentiation of hematopoietic cells of the monocyte-macrophage series and can reverse treatment-related neutropenias. Recombinant M-CSF may also enhance antigen presentation and activate antitumoral cytotoxic T-cells.
A recombinant tumor-specific melanoma antigen. Vaccination with recombinant MAGE-3.1 antigen may induce a host immune response against MAGE-expressing cells, resulting in antitumoral T cell-mediated cytotoxicity. MAGE-expressing cells are found in melanoma, non-small-cell lung carcinoma (NSCLC), head and neck squamous cell carcinoma, transitional cell carcinoma of the bladder, and esophageal carcinoma.
A recombinant form of a human macrophage inflammatory protein-1 alpha (MIP1-alpha) with a substitution of aspartate to alanine at position 26, with potential immunomodulating and radiotherapy potentiating activity. Intravenous administration of recombinant MIP1-alpha variant ECI301 after local tumor irradiation enhances the anti-tumor effect of ionizing radiation at the irradiated site as well as the antitumor effect at non-irradiated tumor sites (known as the abscopal effect). The abscopal effect appears to be attributed to this agent’s ability to recruit and activate leukocytes, such as monocytes, dendritic cells, natural killer cells and T lymphocytes, thereby initiating an anti-tumor immune response against cancer cells. MIP1-alpha, also known as chemokine (C-C motif) ligand 3, is a ligand for the chemokine receptors CCR1, CCR4 and CCR5 that are involved in immune and inflammatory responses.
A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the 5T4 fetal oncoprotein (MVA-h5T4). Vaccination with recombinant modified vaccinia Ankara-5T4 vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing 5T4 fetal oncoprotein antigen, resulting in tumor cell lysis. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attentuated, replication-defective vaccinia strain incapable of virion assembly.
An 85-amino acid recombinant peptide derived from protein c2 of the hemophagocytic hookworm Ancylostoma caninum (a common canine parasite) with anticoagulant activity. Recombinant nematode anticoagulant protein c2 (rNAPc2) binds to circulating activated factor X (FXa) or zymogen factor X (FX) to form a binary complex which subsequently binds to and inhibits membrane-bound activated factor VII/tissue factor complex (FVIIa/TF). When administered prophylactically, this agent may reduce the incidence of deep venous thrombosis without hemostatic compromise. Because rNAPc2 inhibits the formation of the FVIIa/TF protease complex, which may play a role in the cellular signaling of both metastatic and angiogenic processes, it may impede tumor progression.
A recombinant, live attenuated, nonpathogenic oncolytic virus containing the oral poliovirus Sabin type 1 in which the internal ribosomal entry site (IRES) is replaced with the IRES from human rhinovirus type 2 (HRV2), with potential antineoplastic activity. Upon intratumoral administration of recombinant oncolytic poliovirus PVS-RIPO, the poliovirus is selectively taken up by and replicates in tumor cells expressing CD155 (poliovirus receptor, PVR or NECL5) eventually causing tumor cell lysis. CD155, an oncofetal cell adhesion molecule and tumor antigen, is ectopically expressed in certain cancers, such as glioblastoma multiforme (GMB), and plays an important role in tumor cell migration, invasion, and metastasis. Due to the heterologous HRV2 IRES in this recombinant virus, PVS-RIPO only propagates in susceptible, nonneuronal cells (e.g., GBM).
A recombinant small peptide inhibitor of the terminal complement pathway protein C5 originally derived from a protein in the saliva of the Ornithodoros moubata tick, with potential anti-inflammatory and cytoprotective activities. Upon administration, recombinant Ornithodoros moubata saliva-derived small protein complement C5 inhibitor targets and binds to a unique site on the terminal complement protein C5, which blocks C5 cleavage into the pro-inflammatory components C5a and C5b, and prevents the C5b-dependent assembly of the membrane-attack complex (MAC; C5b-9). This prevents MAC-mediated lysis and destruction of red blood cells (RBCs) in paroxysmal nocturnal hemoglobinuria (PNH) and prevents tissue destruction in various other complement-mediated inflammatory and autoimmune diseases. In addition, this C5 inhibitor targets, binds to and inhibits the activity of leukotriene B4 (LTB4), thereby further preventing inflammatory-mediated cell destruction.
A synthetic cyclic peptide form of the naturally occurring posterior pituitary hormone oxytocin. Oxytocin binds to oxytocin receptors in the uterine myometrium, which triggers the G-protein coupled receptor signal transduction cascade that causes increased intracellular calcium concentrations. Increased calcium concentration levels activate myosin light chain kinase which, in turn, induces the formation of the contractile protein actomyosin. This stimulates uterine smooth muscle contractions. This agent also stimulates smooth muscles in the mammary glands, thereby causing lactation.
A recombinant therapeutic agent that is identical or similar to an 84-amino-acid polypeptide produced by the parathryoid gland which functions to maintain a constant concentration of calcium ions (Ca2+) in the extracellular fluid. In target tissues, parathyroid hormone (PTH) binds to and activates the parathryorid hormone receptor (PTHR), a cell surface G protein-coupled receptor; there are two types of receptors, parathyroid hormone receptor 1 (PTH1R) found in bone and the kidney and parathyroid hormone receptor 2 (PTH2R) found primarily in the central nervous system (CNS), pancreas, testis, and placenta. Activation of PTHRs results in the activation of adenylyl cyclase and phospholipase C in target tissue cells, which, depending upon the specific target tissue, results in the enhancement of intestinal Ca2+ absorption, mobilization of bone Ca2+, and renal Ca2+ reabsorption.
A recombinant form of the endogenous chemokine platelet factor 4 with potential antiangiogenesis and antineoplastic activities. As a heparin-binding tetramer, recombinant platelet factor 4 inhibits growth factor-stimulated endothelial cell proliferation, migration, and angiogenesis; it has been shown that this agent inhibits fibroblast growth factor 2 (FGF2) angiogenic activity downstream from the FGF2 receptor. Its activity is antagonized by heparin. Recombinant platelet factor 4 may also directly inhibit the proliferation of some tumor cell types.
A recombinant form of the human PRAME (Preferentially Expressed Antigen of Melanoma) protein combined with the AS15 adjuvant, with potential immunostimulatory and antineoplastic activities. Upon intramuscular administration, GSK2302025A may stimulate the host immune response to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that overexpress the PRAME protein, resulting in tumor cell lysis. The tumor-associated antigen PRAME is often overexpressed by a variety of tumor cell types. AS15 is an potent adjuvant liposomal formulation that contains CpG 7909, monophosphoryl lipid, and QS-21.
A whole, heat-killed, recombinant Saccharomyces cerevisiae yeast-based vaccine genetically altered to express the carcinoembryonic antigen (CEA) peptide 610D with potential immunostimulating and antineoplastic activities. Upon administration, recombinant Saccharomyces cerevisia-CEA(610D) vaccine GI-6207 may stimulate a host cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells, which may result in tumor cell lysis. CEA, a tumor associated antigen, is overexpressed on a wide variety of human cancer cells including colorectal, gastric, lung, breast and pancreatic cancer cells. CEA 610D encodes for 9 amino acids (605-613) in which aspartate is substituted for asparagine at position 610 (610D) in order to strengthen the induction of the CTL response against CEA-expressing tumor cells.
A recombinant human soluble CD4 with antiviral activity. Recombinant human soluble CD4 has the amino terminus but not the T-cell binding domain of the endogenous CD4 antigen. This soluble CD4 protein competitively binds to envelope glycoprotein (gp120) of human immunodeficiency virus (HIV) resulting in inhibition of interaction between gp120 and the endogenous CD4 antigen, thereby blocking viral recognition of CD4 and subsequent entry of HIV into CD4 bearing cells.
A recombinant form of the naturally-occurring cytokine interferon-alpha (IFN-a) that has a modified spatial configuration, with immunomodulating, antiviral and antineoplastic activities. Upon administration of recombinant super-compound interferon (rSIFN-co), this agent binds to IFN-specific cell surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects. The 3-dimensional conformational change improves efficacy and causes fewer side effects compared to IFN-a. Check for '"active clinical trials using this agent.
A recombinant form of a polypeptide chemically identical to or similar to the hormone secreted by the thymus gland. Thymosin is generally known to have functions in the preprocessing of T cells and the development of B cells to plasma cells to produce antibodies. In particular, the predominant form of thymosin, beta 4 thymosin, is the principal actin-sequestering protein that plays an important role in functions that involve actin molecules, such as maintenance of cell shape, cytoplasmic organization, cell movement, and cell division.
A peptide hormone secreted by the anterior pituitary. It promotes the growth of the thyroid gland and stimulates the synthesis of thyroid hormones and the release of thyroxine by the thyroid gland.
A recombinant form of the human anterior pituitary glycoprotein thyroid stimulating hormone (TSH) with use in the diagnostic setting. With an amino acid sequence identical to that of human TSH, thyrotropin alfa binds to TSH receptors on normal thyroid epithelial cells or well-differentiated thyroid cancer cells, stimulating iodine uptake and organification, synthesis and secretion of thyroglobulin (Tg), triiodothyronine (T3), and thyroxine (T4).
A recombinant polypeptide chemically identical to or similar to the endogenous cytokine transforming growth factor-beta-2 (TGF-beta-2). TGF-beta-2 modulates cell growth and immune function and may promote or inhibit tumor growth, depending on the tumor cell type. TGF-beta-2 may also suppress host immune system recognition of and/or response to tumor cells.
A recombinant therapeutic agent which is chemically identical to or similar to one of a number of endogenous tumor necrosis factor (TNF) proteins. TNF family cytokines bind to and activate specific cell-surface receptors, thereby mediating inflammatory processes, cell proliferation, immunity, angiogenesis, and tumor cell cytotoxicity. One primary antitumor effect of TNFs involves stimulation of T cell-mediated antitumor cytotoxicity.
A recombinant therapeutic agent which is chemically identical to or similar to an endogenous non-mutated melanocyte differentiation antigen expressed by both normal and malignant melanocytes. Vaccinations with recombinant tyrosinase-related protein-2 may elicit an antitumoral cytotoxic T-cell response against tumor cells and some normal cells that express tyrosinase-related protein-2.
A vaccine consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA). Vaccination with recombinant vaccinia prostate-specific antigen vaccine stimulates the host immune system to mount a cytotoxic T-cell response against tumor cells expressing PSA.
A recombinant vaccinia virus encoding the T-cell co-stimulatory molecule B7-1. Co-administration of recombinant vaccinia-B7.1 and a tumor-associated antigen in a cancer vaccine may enhance tumor-associated antigen-specific T-cell responses.
A vaccine consisting of recombinant vaccinia virus encoding the tumor-associated antigen carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-CEA(6D)-TRICOM vaccine stimulates the host immune system to mount a T-cell response against tumor cells expressing the CEA antigen. The use of TRICOM in the vaccine may elicit a greater antitumor cytotoxic T lymphocyte (CTL) immune response compared to the use of vaccinia-CEA alone.
A vaccine containing a recombinant vaccinia virus that encodes the gene for human mucin-1, a tumor-associated antigen. Upon administration, recombinant vaccinia-MUC-1 vaccine may elicit a MUC-1-specific cytotoxic T cell response against tumor cells bearing MUC-1.
A cancer vaccine consisting of an inactivated recombinant vaccinia virus encoding epitope peptides derived from melanoma-related HLA-A2-restricted tumor-associated antigens (TAAs), including Melan-A(27-35), gp100(280-288) and tyrosinase(1-9), and two co-stimulatory B7 proteins, B7.1 (CD80) and B7.2 (CD86). Upon administration, recombinant vaccinia-multiepitope melanoma peptides-B7.1-B7.2 vaccine may stimulate a cytotoxic T-lymphocyte response against melanoma cells that express TAAs which share epitopes with the epitope peptides expressed by the vaccine viral vector, resulting in tumor cell lysis; vaccine viral vector-expressed co-stimulatory proteins B7.1 and B7.2 may enhance the cytotoxic T-lymphocyte immune response to the TAAs.
A cancer vaccine consisting of a recombinant vaccinia viral vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with recombinant vaccinia- NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis.
A vaccine consisting of recombinant vaccinia virus encoding a triad of costimulatory molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-TRICOM vaccine stimulates the host immune system to mount a non-specific T-cell response. With the addition of a tumor-associated antigen peptide, this vaccine may enhance a tumor-specific immune response.
A recombinant, replicating oncolytic vesicular stomatitis virus (VSV) carrying the human interferon-beta (IFN-b) gene, with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, recombinant VSV expressing IFN-b replicates in the tumor environment specifically, partially due to defective innate antiviral host defense mechanisms in tumor cells, involving type I IFNs, and exerts its cytolytic activity towards the tumor cells. By expressing human IFN-b, an INF-b-mediated antiviral immune response in surrounding normal cells is activated which protects normal cells against virus replication and VSV-mediated cell lysis. However, tumor cells have a defective IFN-b-mediated innate antiviral immune response allowing for VSV to replicate in these cells without interference. In addition, the IFN-b produced by VSV may activate an immune response in surrounding normal cells and may activate T-lymphocytes, dendritic cells and natural killer cells; thus, inducing an anti-tumor immune response against the tumor cells. VSV, a single-stranded RNA virus belonging to the genus Vesiculovirus of the family Rhabdoviridae, is relatively nonpathogenic to healthy humans.
A recombinant, replicating oncolytic vesicular stomatitis virus (VSV) carrying the human interferon-beta (IFN-b) gene and the tyrosinase related protein 1 (TYRP1) gene, with potential immunomodulating and antineoplastic activities. Upon intratumoral and intravenous administration, recombinant VSV-expressing IFN-b/TYRP1 preferentially replicates in tumor cells. Due to defective IFN-b-mediated innate antiviral host defense mechanisms in tumor cells, VSV is able to replicate in these cells without interference. This induces VSV-mediated cytolytic activity towards the tumor cells. By expressing human IFN-b, an IFN-b-mediated antiviral immune response in surrounding normal cells is activated which protects normal cells against virus replication and the associated VSV-mediated cell lysis. Also, the IFN-b produced by VSV may activate an immune response in surrounding normal cells, involving the activation of cytotoxic T lymphocytes (CTL), dendritic cells (DCs) and natural killer (NK) cells. This induces an anti-tumor immune response against the tumor cells. In addition, the expression of TYRP1 further activates the immune system to induce a CTL-mediated immune response against the TYRP1-expressing tumor cells, thereby further killing TYRP1-expressing tumor cells. VSV, a single-stranded RNA virus belonging to the genus Vesiculovirus of the family Rhabdoviridae, is relatively nonpathogenic to healthy humans but is able to rapidly replicate in and induce apoptosis of tumor cells. TYRP1, a tumor-associated antigen (TAA), is primarily expressed in melanocytes and melanomas.
Brand name for hepatitis B vaccine (recombinant)
Brand name for levoketoconazole
Brand name for epoetin beta
Brand name for therapeutic hydrocortisone
Tomato juice derived from red tomatoes, with potential antioxidant and chemopreventive activities. Red tomato juice contains higher levels of the trans-isomer of lycopene (trans-LYC) compared to the cis-isomer (cis-LYC). Lycopene, a linear, unsaturated hydrocarbon carotenoid, is the major red pigment in certain fruits such as tomatoes, pink grapefruit, apricots, red oranges, watermelon, rosehips, and guava. As an antioxidant, lycopene scavenges free radicals which may both inhibit cellular oxidation and prevent free radical damage to cells. cis-LYC is better absorbed than its trans form.
A gel formulation containing reduced glutathione, L-cysteine, and anthocyanins with potential antioxifdant, immunostimulating, and chemoprotective activities. Reduced glutathione is the primary cellular antioxidant and plays important roles in the antioxidation of reactive oxygen species and free radicals and, as a thiol-containing co-enzyme, in the detoxification of xenobiotic compounds. In addition, glutathione affects DNA synthesis and repair and exerts immunostimulating activity by increasing the production of interleukin-2 (IL-2), promoting antigen presentation, and stimulating T-suppressor/cytotoxic (CD8 cells) cells. The flavonoid anthocyanins, derived from various blue and purple flowering plants, are potent scavengers of reactive oxygen species.
An orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Refametinib specifically inhibits mitogen-activated protein kinase kinase 1 (MAP2K1 or MAPK/ERK kinase 1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers.
Brand name for lepirudin
An adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors. Check for '"active clinical trials using this agent.
Brand name for collagen/aloe vera/vitamin E/lidocaine topical hydrogel
Brand name for phentolamine mesylate
Brand name for metoclopramide hydrochloride
An orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling.
Brand name for insulin, regular
An orally available antagonist of the glucocorticoid receptor (GR), with potential antineoplastic activity. Upon administration, relacorilant competitively binds to and blocks GRs. This inhibits the activity of GRs, and prevents both the translocation of the ligand-GR complexes to the nucleus and gene expression of GR-associated genes. This decreases the negative effects that result from excess levels of endogenous glucocorticoids, like those seen when tumors overproduce glucocorticoids. In addition, by binding to GRs and preventing their activity, inhibition with relacorilant also inhibits the proliferation of GR-overexpressing cancer cells. GRs are overexpressed in certain tumor cell types and promote tumor cell proliferation.
A population of allogeneic related donor cytotoxic T lymphocytes (CTLs) specifically reactive to human adenovirus (Ad) with potential immunomodulating and anti-adenoviral activities. Upon infusion of related donor Ad-specific CTLs, these cells help reconstitute Ad-specific CTL responses in patients at risk of developing Ad infections after allogeneic stem cell transplant or in Ad-infected immunocompromised hosts. These related donor Ad-specific CTLs are manufactured with the CliniMACS Prodigy Cytokine Capture System which facilitates production of the Ad-specific CTLs.
A monoclonal antibody directed against the inhibitor receptor lymphocyte activation gene-3 (LAG-3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, relatlimab binds to LAG-3 on tumor infiltrating lymphocytes (TILs). This may activate antigen-specific T lymphocytes and enhance cytotoxic T cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG-3 is a member of the immunoglobulin superfamily (IgSF) and binds to major histocompatibility complex (MHC) class II. LAG-3 expression on TILs is associated with tumor-mediated immune suppression.
Brand name for zanamivir
Brand name for methylnaltrexone bromide
An orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.
Brand name for mirtazapine
Human mesenchymal stem cells (MSCs) harvested from bone marrow of healthy adult donors and expanded ex vivo, with potential immunosuppressive activity. Remestemcel-L cells are hypo-immunogenic due to lack of major histocompatibility II (MHC II) molecule expression, eliciting little, if any, host immune response upon intravenous infusion. Infusion of allogeneic MSCs may result in: a) increased production of anti-inflammatory cytokines, such as interleukin-10, prostaglandin E, and hepatocyte growth factor; b) decreased mononuclear phagocyte expression of indoleamine 2,3,-dioxygenase, which catabolizes L-tryptophan into its pro-inflammatory metabolites; and c) modulated dendritic cell (DC)maturation and disrupted activities of natural killer (NK) cells and CD8+ and CD4+ T cells. In addition, pluripotent MSCs, upon administration, may be recruited to damaged tissue sites, differentiating along specific lineages when stimulated.
Brand name for infliximab
Brand name for black cohosh
The hydrochloride salt form of remifentanil, a synthetic anilidopiperidine derivative and short-acting opiate agonist with analgesic and anesthetic properties. Remifentanil selectively binds to and activates the mu-opioid receptor, thereby producing analgesia, respiratory depression, miosis, reduced gastrointestinal motility, and euphoria.
Brand name for galantamine hydrobromide
Brand name for apolizumab
A multipeptide cancer vaccine targeting renal cell carcinoma with potential immunopotentiating activity. Renal cell carcinoma peptides vaccine IMA901 consists of 10 different synthetic tumor-associated peptide (TUMAP) antigens (9 HLA-class I-binding and 1 HLA class II-binding); endogenously, these TUMAPs are expressed by the majority of renal cell carcinomas. Vaccination with this agent may significantly increase host cytotoxic T-lymphocyte (CTL) immune responses against tumor cells expressing these peptide antigens.
A cancer vaccine in which autologous dendritic cells are transfected with patient-specific renal cell carcinoma (RCC) RNA and a synthetic, truncated human CD40 ligand (CD40L) RNA with potential immunostimulatory and antineoplastic activities. Individual RCC-specific RNA, encoding a unique repertoire of tumor-associated antigens (TAAs) (including telomerase reverse transcriptase, G250, and oncofetal antigen) is electroporated into autologous dencritic cells (DCs), transfected with synthetic RNA that encodes a truncated version of the T-cell protein CD40L; the transfected autlogous DCs express and process both patient-specific RCC TAAs and the truncated CD40L protein. When reintroduced back to the patient, renal cell carcinoma/CD40L RNA-transfected autologous dendritic cell vaccine AGS-003 may elicit a highly specific cytotoxic T-cell (CTL) response against RCC cells expressing the patient-specific RCC TAA repertoire. The signal cascade initiated by stimulation of the truncated, ectopically expressed co-stimulatory molecule CD40L results in the secretion of the inflammatory cytokine IL-12 downstream.
Brand name for girentuximab
Brand name for tretinoin
Brand name for pelareorep
A nonsulfonylurea insulin secretagogue belonging to the melgitinide class with hypoglycemic activity. Repaglinide is rapidly absorbed and has a rapid onset and short duration of action. This agent is metabolized in the liver by CYP2C8 and CYP3A4 and its metabolites are excreted in the bile. Repaglinide has a half-life of one hour.
An orally available inhibitor of CXC chemokine receptor types 1 (CXCR1) and 2 (CXCR2), with potential antineoplastic activity. Upon administration, reparixin allosterically binds to CXCR1 and prevents CXCR1 activation by its ligand interleukin 8 (IL-8 or CXCL8). This may cause cancer stem cell (CSC) apoptosis and may inhibit tumor cell progression and metastasis. CXCR1, overexpressed on CSCs, plays a key role in CSC survival and the ability of CSC to self-renew; it is also linked to tumor resistance to chemotherapy. Inhibition of the IL-8/CXCR1 interaction also potentiates the cytotoxic effect of chemotherapeutic agents. In addition, reparixin inhibits CXCR2 activation and may reduce both neutrophil recruitment and vascular permeability during inflammation or injury.
A regimen consisting of rituximab, followed by a continuous infusion of etoposide, vincristine and doxorubicin, given with prednisone and a bolus dose of cyclophosphamide, used for the treatment of aggressive forms of non-Hodgkin's lymphoma, including mantle cell lymphoma.
Brand name for ropinirole hydrochloride
Brand name for mannitol
Brand name for anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1)
A naturally occurring capsaicin analog found in the latex of the cactus Euphorbia resinifera with analgesic activity. Resiniferatoxin (RTX) binds to and activates the transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel in the plasma membrane of primary afferent sensory neurons. This increases the permeability to cations, and leads to an influx of calcium and sodium ions. This results in membrane depolarization, causing an irritant effect, followed by desensitization of the sensory neurons thereby inhibiting signal conduction in afferent pain pathways and causing analgesia. TRPV1, a member of the transient receptor potential channel (TRP) superfamily, is a heat- and chemo-sensitive calcium/sodium ion channel that is selectively expressed in a subpopulation of pain-sensing primary afferent neurons.
An imidazoquinolinamine Toll-like receptor (TLR) agonist with potential immunostimulatory activity. Resiquimod binds to and activates TLRs 7 and 8, mainly on dendritic cells (DCs), macrophages, and B-lymphocytes, which results in the activation of the TLR signaling pathway and nuclear translocation of the transcription activator NF-kB another transcription factors; subsequently, the production of cytokines, especially interferon-alpha (INF-a), increases, enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans cells, which may result in enhanced activation of T-lymphocytes. Due to its immunostimulatory activity, this agent may potentially be useful as a vaccine adjuvant.
A topical gel containing the Toll-like receptor (TLR) agonist resiquimod, an imidazoquinolinamine, with potential immunomodulating activity. Upon topical application, the resiquimod gel CD11301 binds to TLR7 and 8, which are found mainly on dendritic cells (DCs), macrophages, and B lymphocytes, and activates the TLR signaling pathway, which results in the induction of the nuclear translocation of transcription activator nuclear factor kappa-B (NF-kB) and activation of other transcription factors. Subsequently, NF-kB-dependent gene expression is induced and cytokine production increases, especially interferon-alpha (INF-a), which results in the enhancement of T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate epidermal Langerhans cells, leading to enhanced activation of T lymphocytes.
A topical gel containing the Toll-like receptor (TLR) agonist resiquimod, an imidazoquinolinamine and with potential immunomodulating activity. Resiquimod binds toTLR7 and 8, mainly on dendritic cells, macrophages, and B-lymphocytes, and activates the TLR signaling pathway, resulting in the induction of the nuclear translocation of transcription activator NF-kB and activation of other transcription factors; subsequently, gene expression increases and the production of cytokines increases, especially interferon-alpha (INF-a), resulting in the enhancement of T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate epidermal Langerhans cells, leading to an enhanced activation of T-lymphocytes.
A form of dietary fiber that resists degradation in the small intestine by gastrointestinal (GI) enzymes with potential chemopreventive and prebiotic activity. Upon consumption of resistant starch, the fiber is not metabolized or absorbed in the small intestine and enters the colon unaltered. Once in the colon, the starch is fermented by anaerobic colonic bacteria and produces short-chain fatty acids (SCFA), including butyrate, which has anti-inflammatory and immunoregulatory activities. In addition, butyrate appears to exert antitumor effects by inhibiting tumor cell proliferation, inducing tumor cell differentiation and apoptosis in colorectal cancer cells.
An orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, inhibition of the transcription of tumor suppressor genes, inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.
Brand name for theophylline
Brand name for cyclosporine ophthalmic emulsion
A phytoalexin derived from grapes and other food products with antioxidant and potential chemopreventive activities. Resveratrol induces phase II drug-metabolizing enzymes (anti-initiation activity); mediates anti-inflammatory effects and inhibits cyclooxygenase and hydroperoxidase functions (anti-promotion activity); and induces promyelocytic leukemia cell differentiation (anti-progression activity), thereby exhibiting activities in three major steps of carcinogenesis. This agent may inhibit TNF-induced activation of NF-kappaB in a dose- and time-dependent manner.
A proprietary formulation of resveratrol, a polyphenolic phytoalexin derived from grapes and other food products with potential antioxidant, anti-obesity, antidiabetic and chemopreventive activities. Resveratrol may activate sirtuin subtype 1 (SIRT-1). SIRT1 activation has been reported to inhibit tumorigenesis and tumor cell proliferation. SIRT-1 is a member of the silent information regulator 2 (SIR2) (or sirtuin) family of enzymes that plays an important role in mitochondrial activity and acts as a protein deacetylase. SIRT1 appears to be involved in the regulation of numerous transcription factors such as Nf-kB and p53.
An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.
An orally bioavailable selective inhibitor of mutant forms of and fusion products involving the proto-oncogene receptor tyrosine kinase RET, with potential antineoplastic activity. Upon administration, BLU-667 binds to and targets various RET mutants and RET-containing fusion product. RET gene mutations and translocations result in the upregulation and/or activation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and regression of these cancers.
An orally bioavailable selective multikinase inhibitor of mutant forms, fusions and rearrangements involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET) as well as the serine/threonine-protein kinase B-raf (BRAF), with potential antineoplastic activity. Upon oral administration, RET/BRAF multikinase inhibitor RXDX-105 selectively and potently binds to and targets various RET- and BRAF-containing mutants, fusions and rearrangements. This results in inhibition of cell growth in tumors cells that exhibit increased RET and BRAF activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers. BRAF, a member of the raf family of serine/threonine protein kinases, plays a role in the regulation of MAP kinase/ERK signaling pathways, which may be constitutively activated in certain cancer cells with activating BRAF gene mutations.
Brand name for epoetin alfa
The hydrochloride salt of a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.
Brand name for tretinoin
Brand name for tretinoin
A synthetic analogue of 9-cis retinoic acid with potential antineoplastic and chemopreventive activities. Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.
retinoid X receptor agonist IRX4204]] A second generation rexinoid and agonist of retinoid X receptor (RXR), with potential antineoplastic, neuroprotective, immunoregulatory, and disease-modifying activities. Upon administration, IRX4204 specifically binds to and activates RXRs, thereby activating RXR-mediated signaling pathways and inducing changes in gene expression that lead to cell differentiation. In responsive cancer cells, IRX4204 induces cell differentiation, decreases cell proliferation, and induces apoptosis, which leads to cancer regression. IRX4204 enhances the differentiation of CD4-positive T lymphocytes into inducible regulatory T cells (iTreg) and suppresses the development of inflammatory T helper 17 (Th17) cells. In addition, IRX4204 is able to cross the blood-brain barrier (BBB) and induces the differentiation of oligodendrocyte precursor cells (OPCs) into oligodendrocytes, promotes repair of myelin, and enhances the survival of dopaminergic neurons.
The fat soluble vitamin retinol. Vitamin A binds to and activates retinoid receptors (RARs), thereby inducing cell differentiation and apoptosis of some cancer cell types and inhibiting carcinogenesis. Vitamin A plays an essential role in many physiologic processes, including proper functioning of the retina, growth and differentiation of target tissues, proper functioning of the reproductive organs, and modulation of immune function.
A naturally-occurring fatty acid ester form of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Retinyl acetate binds to and activates retinoid receptors, inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation in some cancer cell types and exhibits immunomodulatory properties.
A replication-incompetent, pathotropic, tumor matrix (collagen)-targeted, retroviral vector encoding an N-terminal deletion mutant form of the cyclin G1 gene with potential antineoplastic activity. Under the control of a hybrid long-terminal repeat/cytomegalovirus (CMV) promoter, retrovector encoding mutant anti-cyclin G expresses the mutant cyclin G1 construct, resulting in disruption of tumor cell cyclin G1 activity and decreased cellular proliferation and angiogenesis. This agent preferentially targets collagen of the tumor matrix because of the incorporation of the collagen-binding domain of von Willebrand factor (vWF) on the retrovector surface. Exploiting the collagen-targeting mechanism of vWF permits delivery of the retrovector to tumor sites where angiogenesis and collagen matrix exposure occur.
Brand name for zidovudine
Brand name for naltrexone hydrochloride
Brand name for soy protein isolate
Brand name for lenalidomide
RevM10 is a dominant-negative mutant of HIV-1 Rev gene, which encodes a RNA-binding protein involving in nuclear trafficking of unspliced viral mRNAs. Due to the fact that Rev is essential for HIV-1 replication makes it an attractive target for antiviral approaches. Based on the notion of intracellular immunization, in vitro studies that introducing RevM10 gene into stem cells have demonstrated its ability to combat HIV-1 infection in human hematopoietic cells.
Brand name for retrovector encoding mutant anti-cyclin G1
An orally bioavailable synthetic retinoid X receptor (RXR) agonist with potential antineoplastic and anti-inflammatory activities. Rexinoid NRX 194204 selectively binds to and activates RXRs. Because RXRs can form heterodimers with several nuclear receptors (NRs), RXR activation by this agent may result in a broad range of gene expression depending on the effector DNA response elements activated. Rexinoid NRX 194204 may inhibit the tumor-necrosis factor (TNF)-mediated release of nitric oxide (NO) and interleukin 6 (IL6) and may inhibit tumor cell proliferation. This agent appears to be less toxic than RAR-selective ligands.
Brand name for troglitazone
A recombinant immunotoxin consisting of the anti-CD25 monoclonal antibody RFT5 fused to the deglycosylated ricin A-chain (dgA) with potential antitumor activity. The monoclonal antibody moiety of RFT5-dgA immunotoxin attaches to CD25 (the alpha chain of the IL-2 receptor complex) on the cell membrane; after internalization, the dgA moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. CD25 is expressed on activated normal T and B cells and macrophages and is frequently upregulated in many hematologic malignancies.
Brand name for arginine hydrochloride
Brand name for recombinant human endostatin
A liposome-based preparation consisting of the beta- and gamma-emitting radionuclide rhenium Re 188 (Re 188) linked to the chelator N,N-bis (2-mercaptoethyl)-N',N'-diethylethylenediamine (BMEDA) and encapsulated in liposomes, with potential tumor imaging and antineoplastic activities. Upon intravenous infusion of rhenium Re 188 BMEDA-labeled liposomes, the liposomes selectively target tumor cells, facilitate the retention of the radioisotope by those cells, and cause localized antitumor radiocytotoxicity while sparing surrounding normal, healthy cells. In addition, Re 188 BMEDA-labeled liposomes can be used for imaging purposes. Re 188 has a short half-life and a short path length, which further contribute to limiting the radiotoxicity to the tumor cells.
A rhenium (Re) 188 conjugate of ethiodized oil (lipiodol), an iodinated ethyl ester derived from poppy seed oil, with potential antineoplastic activity. Upon hepatic intra-arterial injection rhenium Re 188 ethiodized oil accumulates in hepatocellular carcinoma (HCC) tumor cells, thereby delivering a cytotoxic dose of radiation through Re 188 directly to the tumor cells. This may kill tumor cells while sparing surrounding normal cells and tissues. Compared to iodine I 131, Re 188 has a shorter half-life.
A synthetic compound containing the bisphosphonate etidronate (hydroxyethylidene diphosphonate, HEDP) labeled with rhenium Re188, a beta-emitting radioisotope with potential antineoplastic activity. Upon administration, Re-188 etidronate binds to hydroxyapatite in bone, delivering a cytotoxic dose of beta radiation to primary and metastatic bone tumors. The beta-radiation may provide localized anti-tumor radiotoxicity while sparing extramedullary bone marrow tissues.
Brand name for methotrexate
A macrocyclic lactone. Rhizoxin binds to tubulin and inhibits microtubule assembly, thereby inducing cytotoxicity. This agent also may inhibit endothelial cell-induced angiogenic activity, which may result in decreased tumor cell proliferation.
A cancer vaccine composed of an immunogenic peptide derived from the Ras homolog family member C (RhoC; Rho-related GTP-binding protein RhoC) that is emulsified in the immunoadjuvant montanide ISA-51, with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration, RhoC peptide vaccine RV001V may stimulate the host immune system to mount a humoral and cytotoxic T-lymphocyte (CTL) response against tumor cells expressing RhoC, which results in tumor cell lysis. RhoC, a tumor-associated antigen (TAA) that is overexpressed in a variety of tumor cell types, is associated with increased metastatic potential.
A decoction of rhubarb root (Da Huang) and licorice root (Gan Cao) used in Chinese Herbal Medicine. Upon ingestion, the rhubarb/licorice herbal supplement may help improve appetite.
A synthetic nucleoside analogue of ribofuranosyl with antiviral activity. Ribavirin incorporates into viral nucleic acid, inhibits viral ribonucleic acid (RNA) synthesis, induces viral genome mutations, and inhibits normal viral replication. Ribavirin shows activity against a variety of RNA viruses, especially hepatitis C virus. Check for '"active clinical trials using this agent.
An orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Ribociclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
An essential human nutrient that is a heat-stable and water-soluble flavin belonging to the vitamin B family. Riboflavin is a precursor of the coenzymes flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD). These coenzymes are of vital importance in normal tissue respiration, pyridoxine activation, tryptophan to niacin conversion, fat, carbohydrate, and protein metabolism, and glutathione reductase mediated detoxification. Riboflavin may also be involved in maintaining erythrocyte integrity. This vitamin is essential for healthy skin, nails, and hair.
A nuclease of mammalian origin that cleaves the phosphodiester bond between nucleotides of ribonucleic acids with potential antineoplastic activity. Ribonuclease QBI-139 catalyzes the hydrolysis and degradation of RNA leading to the inhibition of protein synthesis and cell death.
A recombinant protein that inactivates the ribosome with potential antineoplastic and immunomodulating activities. Ribosome-inactivating protein CY503 binds to the cell surface sialyltransferase CD75 and is internalized; intracellularly, CY503 cleaves an adenine-specific N-glycosidic bond on the 28S ribosomal subunit, which may result in tumor cell apoptosis. This agent has also been shown to activate natural killer (NK) cells, induce cytokine receptor expression, and stimulate the release of cytokines. CD75 is expressed on mature B-cells and subsets of T-cells and erythrocytes.
Brand name for tiazofurin
The nutrient-rich hard outer layer of the rice cereal grain, with potential chemopreventive, antioxidant, iron chelating, anticholesterol and anti-inflammatory activities. Rice bran is rich in fiber, such as beta-glucan, pectin and gum; it also comprises vitamins and minerals, such as iron, magnesium and phosphorus, and essential fatty acids. In addition, Rice bran contains various bioactive components, including ferulic acid, tricin, beta-sitosterol, gamma-oryzanol, phytic acid, and inositol hexaphosphate (IP6). The potential anticancer activity of rice bran may be due to the synergistic effects of these phytochemicals on their ability to induce apoptosis, inhibit cell proliferation, and alter cell cycle progression in cancer cells. Rice bran's bioactive components also protect against tissue damage by scavenging free radicals and blocking chronic inflammatory responses. In addition, they are able to modulate the gut microflora and carcinogen-metabolizing enzymes, thereby further exerting a chemopreventive effect.
A chemoimmunotherapy regimen consisting of rituximab, ifosfamide, carboplatin and etoposide used to treat indolent and aggressive forms of non-Hodgkin lymphoma; also used to treat relapsed and refractory non-Hodgkin lymphoma.
An orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. Ricolinostat selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. This leads to an accumulation of unfolded and misfolded ubiquitinated proteins and may eventually induce cancer cell apoptosis, and inhibition of cancer cell growth. HDAC6, a class II HDAC deacetylase located in the cytoplasm, appears to play a key role in the formation and activation of the aggresomes needed for degradation of misfolded proteins. Compared to non-selective HDAC inhibitor, ricolinostat is able to reduce the toxic effects on normal, healthy cells.
A small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and,consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
Brand name for auranofin
A semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription.
An orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity. Rifaximin binds to the beta-subunit of bacterial DNA-dependent RNA polymerase, inhibiting bacterial RNA synthesis and bacterial cell growth. As rifaximin is not well absorbed, its antibacterial activity is largely localized to the gastrointestinal tract.
A synthetic RNA oligonucleotide and agonist of the retinoic acid-inducible gene I protein (RIG-I; DDX58), with potential antineoplastic activity. Upon intratumoral/intralesional administration, the RIG-I selective ligand RGT100 targets and binds to the cytosolic RNA receptor RIG-I. This induces RIG-I-mediated signaling, upregulates interferon (IFN)-alfa (IFN-a) and beta (IFN-b), and induces a potent IFN-mediated innate immune response against the tumor cells. This induces the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTL) and induces apoptosis in cancer cells. Check for '"active clinical trials using this agent.
A synthetic benzyl styryl sulfone analogue with potential antineoplastic activity. Rigosertib sodium inhibits polo-like kinase1 (Plk1), inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.
A vaccine formulation consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA) and recombinant vaccinia virus encoding three co-stimulatory molecule transgenes B7.1, ICAM-1, and LFA-3 (TRICOM). Vaccination with PSA in combination with TRICOM may enhance antigen presentation, resulting in the augmentation of a cytotoxic T cell (CTL) immune response against tumor cells expressing PSA.
A vaccine formulation consisting of rilimogene galvacirepvec (V-PSA-TRICOM; PROSTVAC-V), a recombinant vaccinia virus, and rilimogene glafolivec (F-PSA-TRICOM; PROSTVAC-F), a recombinant fowlpox virus, with potential immunostimulating and antineoplastic activities. Both viruses encode modified forms of human prostate specific antigen (PSA) and the three co-stimulatory molecule transgenes (TRIad of COstimulatory Molecules; TRICOM), B7.1 (CD80), intercellular adhesion molecule-1 (ICAM-1), and lymphocyte function-associated antigen-3 (LFA-3). Using a prime-boost vaccine regimen, with a primary vaccination of rilimogene galvacirepvec followed by multiple booster vaccinations of rilimogene glafolivec, the PSA-TRICOM vaccines infect antigen-presenting cells (APCs), such as dendritic cells (DCs). Upon processing and expression of the PSA and TRICOM proteins on their surfaces, the DCs are able to initiate cytotoxic T-lymphocyte (CTL) responses against PSA-expressing cancer cells. The combination of PSA and TRICOM greatly enhances T-cell activation and T-cell-mediated tumor cell killing.
A cancer vaccine consisting of a recombinant fowlpox virus encoding fragment of human prostate-specific antigen (PSA), PSA:154-163 (155L), and a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM). Administration of this agent may induce a cytotoxic T cell response against PSA-expressing tumor cells. Dendritic cells infected with TRICOM vectors greatly enhance naive T-cell activation and peptide-specific T-cell stimulation. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
A fully human IgG2 monoclonal antibody directed against the human hepatocyte growth factor (HGF) with potential antineoplastic activity. Rilotumumab binds to and neutralizes HGF, preventing the binding of HGF to its receptor c-Met and so c-Met activation; inhibition of c-Met-mediated signal transduction may result in the induction of apoptosis in cells expressing c-Met. c-Met (HGF receptor or HGFR), a receptor tyrosine kinase overexpressed or mutated in a variety of epithelial cancer cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.
Brand name for riluzole
A benzothiazole derivative with neuroprotective and potential anti-depressant and anxiolytic activities. While the mechanism of action of riluzole is unknown, its pharmacological activities in motor neurons include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. In animal models, this agent has been shown to exhibit myorelaxant and sedative activities, apparently due to the blockade of glutamatergic neurotransmission.
A lipid-permeable tacrolimus analogue with homodimerizing activity. Rimiducid homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity. This agent is used to homodimerize the Fv-containing drug-binding domains of genetically engineered receptors such as the iCD40 receptor of the autologous dendritic cell vaccine BP-GMAX-CD1, resulting in receptor activation. Check for '"active clinical trials using this agent.
A cancer vaccine consisting of a human epidermal growth factor receptor variant III (EGFRvIIi)-specific peptide conjugated to the non-specific immunomodulator keyhole limpet hemocyanin (KLH) with potential antineoplastic activity. Vaccination with rindopepimut may elicit a cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing EGFRvIII. EGFRvIII, a functional variant of EGFR that is not expressed in normal tissues, was originally discovered in glioblastoma multiforme (GBM) and has also been found in various other cancers such as breast, ovarian, metastatic prostate, colorectal, and head and neck cancers. EGFRvIII contains an 83 amino acid deletion in its extracellular domain and has been shown to transform NIH/3T3 mouse embryonic fibroblast cells in vitro.
A synthetic derivative of inosinic acid with antiretroviral and immunomodulatory activities. Rintatolimod acts through a number of pathways to stimulate the antiviral activity of the immune system. This agent stimulates interferon production; activates the oligoadenylate synthase-RNase L pathway; stimulates natural killer cell activity; and acts as a non-mitogenic stimulator of the immune system. Rintatolimod also inhibits replication of the human immunodeficiency virus (HIV) in vitro.
Brand name for metformin hydrochloride
An orally available, small-molecule inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1; receptor-interacting protein 1; RIP1) with potential antineoplastic and immunomodulatory activities. Upon administration, GSK3145095 disrupts RIPK1-mediated signaling, which may reduce C-X-C motif chemokine ligand 1 (CXCL1)-driven recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME). This allows effector cells, such as natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), to kill and eliminate cancer cells. RIPK1, a serine-threonine kinase that normally plays a key role in inflammation and cell death in response to tissue damage and pathogen recognition, is overexpressed in certain cancer types and may be associated with oncogenesis and promotion of the immunosuppressive nature of the TME.
The hemipentahydrate monosodium salt of risedronic acid, a synthetic pyridinyl bisphosphonate. Risedronic acid binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption.
An orally bioavailable capsule formulation containing the antipsychotic agent risperidone suspended in the lipid rumenic acid, with potential antineoplastic activity. Upon administration of VAL401, risperidone may, through an as of yet not elucidated mechanism of action, reduce cellular activity and tumor cell proliferation in multiple cancers.
Brand name for methylphenidate hydrochloride
A synthetic aromatic derivative with antiviral properties. Ritonavir is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases, thereby preventing the cleavage of Gag-Pol polyproteins and resulting in the production of noninfectious viral particles. This agent is more active against HIV-1. Because ritonavir targets the HIV replication cycle after translation and before assembly, it is active in chronically infected cells that generally are not affected by nucleoside reverse transcriptase inhibitors. Check for '"active clinical trials using this agent.
Brand name for rituximab
Brand name for rituximab and hyaluronidase human
A recombinant chimeric murine/human antibody directed against the CD20 antigen, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes. Following binding, rituximab triggers a host cytotoxic immune response against CD20-positive cells.
A combination preparation of rituximab, a genetically engineered chimeric murine/human immunoglobulin (Ig) G1 kappa monoclonal antibody directed against the CD20 antigen, and the recombinant form of the human enzyme hyaluronidase, with antineoplastic activity. Upon subcutaneous administration of rituximab and hyaluronidase human, the hyaluronidase reversibly depolymerizes the polysaccharide hyaluronan in the subcutaneous tissue. This increases the permeability of the subcutaneous tissue and enhances the absorption of rituximab into the systemic circulation. In turn, rituximab targets and binds to CD20 expressed on tumor cells, and induces tumor cell lysis primarily through the induction of complement dependent cytotoxicity (CDC) and antibody-dependent cell mediated cytotoxicity (ADCC). When administered subcutaneously, hyaluronidase, an endoglycosidase, increases the dispersion and absorption of co-administered drugs. CD20 is expressed on the surface of pre-B and mature Blymphocytes, and is overexpressed in a variety of B-cell malignancies.
A proprietary conjugate of rituximab, a recombinant chimeric murine/human antibody directed against the CD20 antigen, with potential antineoplastic activity. Upon administration of the rituximab conjugate CON-4619, the rituximab moiety targets and binds to CD20, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes. Following binding, rituximab triggers a host cytotoxic immune response against CD20-positive cells.
A regimen consisting of rituximab, ifosfamide, cytarabine and etoposide that can be used in the treatment of non-Hodgkin lymphoma (NHL).
An orally bioavailable oxazolidinone derivative and direct inhibitor of the coagulation factor Xa with anticoagulant activity. Upon oral administration, rivaroxaban selectively binds to both free factor Xa and factor Xa bound in the prothrombinase complex. This interferes with the conversion of prothrombin (factor II) to thrombin and eventually prevents the formation of cross-linked fibrin clots. Rivaroxaban does not affect existing thrombin levels.
The tartrate salt form of rivastigmine, a phenylcarbamate derivative exhibiting cognitive stimulating property. Although the mechanism of action has not been fully elucidated, rivastigmine tartrate may bind reversibly to cholinesterase, thereby decreasing the breakdown of acetylcholine and enhancing cholinergic function.
The benzoate salt form of rizatriptan, a member of the triptan class agents with anti-migraine property. Rizatriptan benzoate selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries, and to 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. Receptor binding results in constriction of cranial vessels and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Rizatriptan benzoate may also relief migraine headaches by inhibition of pro-inflammatory neuropeptide release.
An oral polymer matrix-based rinse formulation that contains N-acetylcysteine, an antioxidant amino acid derivative with antiinflammatory properties. RK-0202 may alleviate symptoms of radiation-induced oral mucositis.
Autologous, genetically engineered T lymphocytes that have been electroporated with an mRNA encoding for an anti-CD19 chimeric antigen receptor (CAR) consisting of an anti-CD19 single chain variable fragment (scFv) coupled to the co-stimulatory signaling domain of 4-1BB (CD137) and the zeta chain of the T-cell receptor CD3 complex (CD3-zeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, the RNA electroporated CD19CAR-CD3zeta-4-1BB-expressing autologous T-lymphocytes attach to cancer cells expressing CD19. This induces selective toxicity against CD19-expressing tumor cells and causes tumor cell lysis. The 4-1BB co-stimulatory molecule signaling domain enhances T-cell activation and signaling after recognition of CD19. CD19 antigen is a B-cell specific cell surface antigen, which is expressed in all B-cell lineage malignancies.
Brand name for ssRNA-based immunomodulator CV8102
An orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. This blocks the interaction between the hRRM1 and hRRM2 subunits and interferes with the assembly of the active hRRM1/hRRM2 complex of RNR. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA, and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis. RNR, an enzyme that catalyzes the conversion of ribonucleoside diphosphate to deoxyribonucleoside diphosphate, is essential for de novo DNA synthesis and plays an important role in cell growth; it is overexpressed in many cancer cell types and is associated with increased drug resistance, cancer cell growth and metastasis.
A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Robatumumab binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; downregulation of this survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.
Brand name for erythromycin
Brand name for glycopyrrolate
Brand name for calcitriol
Brand name for ceftriaxone sodium
An orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Rociletinib binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, CO-1686 inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors. This agent shows minimal activity against wild-type EGFR, hence does not cause certain dose-limiting toxicities.
An orally administered inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II), with potential immunomodulating activity. Upon administration, ROCK2 inhibitor KD025 binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signal transduction pathways and modulates various pro- and anti-inflammatory immune cell responses. ROCK2 is upregulated in various diseases, including various fibrotic, neurodegenerative and autoimmune diseases.
The bromide salt form of rocuronium, an intermediate-acting quaternary aminosteroid with muscle relaxant property. Rocuronium bromide competitively binds to the nicotinic receptor at the motor end plate, and antagonizes acetylcholine binding, which results in skeletal muscle relaxation and paralysis.
A synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.
Brand name for recombinant interferon alpha-2a
An orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3′,5′-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis. PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3′5′-cyclic guanosine monophosphate (cGMP) to their inactive 5′ monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases.
The hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.
Brand name for eflapegrastim
A bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins.
A recombinant protein with megakaryopoiesis stimulating activity. Romiplostim mimics endogenous thrombopoietin (TPO), directly binding to and activating the platelet thrombopoietin receptor (TpoR, Mpl, or CD110 antigen), a cytokine receptor belonging to the hematopoietin receptor superfamily. Activation of TpoR stimulates the proliferation and differentiation of megakaryocytes, resulting in an increase in the production of blood platelets.
Brand name for troglitazone
An orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. Roniciclib selectively binds to and inhibits the activity of CDK1/Cyclin B, CDK2/Cyclin E, CDK4/Cyclin D1, and CDK9/Cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle progression and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are often dysregulated in cancerous cells.
An orally available 5-substituted 2-pyrimidinone-2'-deoxyribonucleoside analogue and prodrug of 5-iododeoxyuridine (IUdR), an iodinated analogue of deoxyuridine, with radiosensitizing activity. Upon oral administration, ropidoxuridine (IPdR) is efficiently converted to idoxuridine (IUdR) by a hepatic aldehyde oxidase. In turn, IUdR is incorporated into DNA during replication, thereby sensitizing cells to ionizing radiation by increasing DNA strand breaks. Compared to IUdR, ropidoxuridine is associated with a lower toxicity profile and improved anti-tumor activity.
The hydrochloride salt form of ropinirole, a non-ergot dopamine agonist with antiparkinsonian property. Acting as a substitute for dopamine, ropinirole hydrochloride binds to and activates dopamine D2 and D3 receptors within the caudate putamen in the brain, thereby improving motor function.
The hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity. Ropivacaine binds to voltage-gated sodium ion channels in the neuronal membrane, thereby preventing the permeability of sodium ions and resulting in. a stabilization of the neuronal membrane and inhibition of depolarization; nerve impulse generation and propagation are blocked, resulting in a reversible loss of sensation.
A quinoline-3-carboxamide with potential antineoplastic activity. Roquinimex inhibits endothelial cell proliferation, migration, and basement membrane invasion; reduces the secretion of the angiogenic factor tumor necrosis factor alpha by tumor-associated macrophages (TAMs); and inhibits angiogenesis. This agent is also an immune modulator that appears to alter cytokine profiles and enhance the activity of T cells, natural killer cells, and macrophages.
A mixture of two T-lymphocyte preparations expressing a chimeric antigen receptor (CAR) consisting of an anti-receptor tyrosine kinase-like orphan receptor 1 (ROR1) single chain variable fragment (scFv) fused to either the co-stimulatory signaling domain cluster of differentiation 28 (CD28), and the zeta chain of the T-cell receptor (TCR)/CD3 complex (CD3-zeta) (ROR1CD28zeta), or the co-stimulatory signaling domain cluster of differentiation 137 (CD137; 4-1BB), and the zeta chain of the T-cell receptor (TCR)/CD3 complex (CD3-zeta) (ROR1CD137zeta), with potential immunomodulating and antineoplastic activities. Upon simultaneous administration of the two T lymphocyte populations ROR1CD28zeta and ROR1CD137zeta , the ROR1 CAR-specific autologous T-lymphocytes are directed to tumor cells expressing ROR1, which may result in a selective toxicity against, and lysis of ROR1-expressing tumor cells. CD28, a T-cell surface-associated co-stimulatory molecule, is required for full T-cell activation, proliferation, and survival. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of ROR1. ROR1, also known as neurotrophic tyrosine kinase, receptor-related 1, is expressed during embryogenesis and by certain leukemias. Check for '"active clinical trials using this agent.
An orally bioavailable agonist of retinoic acid-related orphan receptor gamma (RORg), with potential immunomodulatory and antineoplastic activities. Upon oral administration of RORg agonist LYC-55716, this agent selectively binds to the nuclear receptor transcription factor RORg, forming a receptor complex that translocates to the nucleus, and binds to ROR response elements (ROREs), enhancing the function, proliferation and survival of type 17 T cells, including Th17 (helper T cells) and Tc17 (cytotoxic T cells). This may increase the expression of co-stimulatory molecules and decrease the expression of co-inhibitory molecules on T cells leading to increased production of cytokines and chemokines by T cells, decreased proliferation of regulatory T cells (Tregs), and abrogation of tumor-induced immunosuppression. This ultimately induces a T-cell-mediated immune response against cancer cells and leads to a reduction in tumor cell growth. RORg, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation, plays a key role in immune activation.
The maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Rosiglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation.
A synthetic purpurin with photosensitizing activity. Rostaporfin preferentially accumulates in tumor cells due to an increased rate of metabolism. Upon exposure to a light source, this agent absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen with local cytotoxic effects.
The calcium salt form of rosuvastatin, a statin with antilipidemic activity. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. Check for '"active clinical trials using this agent.
Brand name for rotavirus vaccine
A viral vaccine that prevents against rotavirus infection, the leading cause of severe acute gastroenteritis.
A Chinese herbal medicine (CHM) derived from the stems of the herbaceous plant Cistanche deserticola Y. C. Ma (Ginseng of the desert) belonging to the Orobanchaceae family. Rou Cong Rong may have antioxidative and neuroprotective activities. This traditional Chinese medicine (TCM) is used to help with pain, deficiency of kidney yang and may relieve constipation by moistening and smoothing stool. Check for '"active clinical trials using this agent.
An antibody-drug conjugate (ADC) containing an antibody (SC16) directed against an as of yet undisclosed protein and conjugated to the cytotoxic agent D6.5, with potential antineoplastic activity. Upon administration, the antibody moiety of rovalpituzumab tesirine selectively binds to the target on tumor cell surfaces. Upon internalization, the D6.5 moiety is released and causes DNA damage, which may result in the inhibition of proliferation of tumor cells that overexpress this target.
Brand name for mesalamine
An orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity. Upon administration, roxadustat binds to and inhibits HIF-PHI, an enzyme responsible for the degradation of transcription factors in the HIF family under normal oxygen conditions. This prevents HIF breakdown and promotes HIF activity. Increased HIF activity leads to an increase in endogenous erythropoietin production, thereby enhancing erythropoiesis. It also reduces the expression of the peptide hormone hepcidin, improves iron availability, and boosts hemoglobin (Hb) levels. HIF regulates the expression of genes in response to reduced oxygen levels, including genes required for erythropoiesis and iron metabolism.
Brand name for morphine sulfate
Brand name for oxycodone hydrochloride
Brand name for ramelteon
Brand name for erythromycin
An orally available inhibitor of human respiratory syncytial virus (RSV) fusion protein (F protein), with potential antiviral activity. Upon oral administration of GS-5806, this agent specifically binds to F protein on the viral surface, which inhibits RSV F protein-mediated fusion with the host cell membrane and prevents viral entry. This blocks RSV replication, reduces viral load, and decreases the severity of the disease. RSV F protein, a viral surface glycoprotein, plays a key role in RSV fusion with and entry into target cells.
A semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
Brand name for rucaparib camsylate
The camsylate salt form of rucaparib, an inhibitor of the nuclear enzyme polyadenosine 5’-diphosphoribose (poly-ADP-ribose) polymerase (PARP), with chemosensitizing, radiosensitizing, and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP-1, PARP-2 and PARP-3, and inhibits PARP1-mediated repair of single-strand DNA (ssDNA) breaks via the base-excision repair pathway; this enhances the accumulation of DNA strand breaks and promotes genomic instability and apoptosis. Rucaparib may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by ssDNA breaks.
A tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARP1 catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks.
A radioactive isotope of the rare element ruthenium, a member of the light platinum group. A radioactive plaque containing ruthenium 106 may be inserted into the eye to irradiate ophthalmic tumors.
A ruthenium-based photosensitizer (PS), that can potentially be used for photodynamic therapy (PDT). Upon intratumoral administration, the ruthenium-based PS TLD1411 targets mitochondria in tumor cells. Upon PDT, TLD1411 produces singlet molecular oxygen (O2), and induces a reactive oxygen species (ROS)-mediated tumor cell apoptosis.
A ruthenium-containing cancer agent targeting transferrin with potential antineoplastic activity. Upon intravenous administration, NKP-1339 (Ru3+) binds to transferrin (Tf) and is taken up via Tf receptors (TfR), which are overexpressed on cancer cells. Once inside the cell, NKP-1339 is released from Tf and is reduced, within the acidic environment of the endosomes, to its active form NKP-119 (Ru2+). In turn, the active form induces a redox reaction, thereby leading to the formation of reactive oxygen species (ROS) which inhibits GRP78 and SOD, endoplasmic reticulum-stress modulating molecules as well as BAG4 and ERK, program cell death regulating molecules. This eventually induces caspase-dependent apoptosis.
The phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.