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.
R-(-)-gossypol acetic acid
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 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.
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.
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.
RadiaPlex Rx Gel
(Other 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.
The chloride salt of the radioisotope radium-223 with bone-targeting, radioisotopic and potential antineoplastic activities. Upon administration, short-lived alpha-particle-emitting radium-223 localizes to bone metastases and kills tumor cells, with minimal effects on the surrounding population of normal cells.
Raf kinase inhibitor XL281
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.
Raf/MEK dual kinase inhibitor RO5126766
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 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.
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 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.
rapamycin-polarized Th1/Tc1 autologous T lymphocytes
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.
ras peptide cancer vaccine
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.
(Other name for: reduced glutathione-L-cysteine-anthocyanins gel)
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.
Re-186 hydroxyethylidene diphosphonate
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.
(Other name for: ribavirin)
(Other name for: recombinant interferon beta)
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.
recombinant 70-kD heat-shock protein
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.
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.
recombinant adenovirus-interferon SCH 721015
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.
recombinant adenovirus-L523S vaccine
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.
recombinant adenovirus-p53 SCH-58500
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.
recombinant attenuated Salmonella typhimurium expressing IL-2
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.
recombinant B. pertussis adenylate cyclase toxin-tyrosinase A2 epitope vaccine
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.
recombinant bispecific single-chain antibody rM28
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.
recombinant dHER2 vaccine
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.
recombinant DNA-L523S vaccine
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.
recombinant flt3 ligand
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.
recombinant fowlpox GM-CSF vaccine adjuvant
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.
recombinant fowlpox-B7.1 vaccine
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.
recombinant fowlpox-CEA(6D)/TRICOM vaccine
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.
recombinant fowlpox-prostate specific antigen vaccine
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.
recombinant fowlpox-tyrosinase vaccine
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.
recombinant human 6Ckine
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.
recombinant human albumin-human granulocyte colony-stimulating factor
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.
recombinant human angiotensin converting enzyme 2 APN01
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.
recombinant human chorionic gonadotropin
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.
recombinant human EGF-rP64K/Montanide ISA 51 vaccine
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.
recombinant human endostatin
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.
recombinant human epidermal growth factor
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.
recombinant human fusion protein L19TNFalpha
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.
recombinant human granulocyte colony-stimulating factor
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.
recombinant human hyaluronidase
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.
recombinant human mannan-binding lectin
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.
recombinant human mannose-binding lectin
A recombinant protein similar or identical to human mannose-binding lectin (MBL) with antimicrobial activity. MBL is a plasma protein containing a carbohydrate recognition domain at one end and a collagen-like stalk domain at the other. The presence of multiple carbohydrate binding sites in a single molecule of MBL (also called mannose-binding protein, mannan-binding protein or or MBP) allows strong binding to mannose residues on the phospholipid bilayer of microbial pathogens. Upon binding, activation of the complement system leads to the deposition of complement components on the surface of the microorganisms (opsonisation), followed by their clearance by phagocytic cells. Administration of the agent to deficient individuals may restore lectin function in vivo.
recombinant human stem cell factor
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.
recombinant interferon alfa
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).
recombinant interferon alpha-1b
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.
recombinant interferon alpha-2a
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.
recombinant interferon beta
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.
recombinant interferon gamma
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 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 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 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 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 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.
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.
recombinant leukocyte interleukin
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.
recombinant macrophage colony-stimulating factor
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.
recombinant MAGE-3.1 antigen
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.
recombinant modified vaccinia Ankara-5T4 vaccine
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.
recombinant nematode anticoagulant protein c2
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.
recombinant parathyroid hormone
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.
recombinant platelet factor 4
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.
recombinant PRAME protein plus AS15 adjuvant GSK2302025A
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.
recombinant Saccharomyces cerevisia-CEA(610D) vaccine GI-6207
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.
recombinant soluble human CD4 protein
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 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.
recombinant thyroid-stimulating hormone
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.
recombinant thyrotropin alfa
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).
recombinant transforming growth factor-beta-2
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.
recombinant tumor necrosis factor family protein
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.
recombinant tyrosinase-related protein-2
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.
recombinant vaccinia prostate-specific antigen vaccine
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.
recombinant vaccinia viral vector RO5217790
A vaccine consisting of recombinant modified vaccinia Ankara (MVA) viral vector encoding mutated forms of the genes for the viral oncoproteins E6 and E7 derived from the human papillomavirus (HPV) type 16 and the human cytokine interleukin-2 (hIL2), with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration, recombinant vaccinia viral vector RO5217790 may stimulate the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against cells expressing HPV E6 and E7, resulting in tumor cell lysis. Oncoproteins E6 and E7 have been implicated in the tumorigenesis of cervical carcinoma.
recombinant vaccinia-B7.1 vaccine
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.
recombinant vaccinia-CEA(6D)-TRICOM vaccine
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.
recombinant vaccinia-MUC-1 vaccine
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.
recombinant vaccinia-multiepitope melanoma peptides-B7.1-B7.2 vaccine
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.
recombinant vaccinia-NY-ESO-1 vaccine
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.
(Other name for: hepatitis B vaccine (recombinant))
(Other name for: therapeutic hydrocortisone)
reduced glutathione-L-cysteine-anthocyanins gel
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.
(Other name for: lepirudin)
(Other name for: phentolamine mesylate)
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.
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.