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• Cancer Drugs

- R -

• R(+)XK469

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.



• raloxifene

A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects.



• ranimustine

A chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells.



• ranpirnase

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.



• Rapamune

(Other name for: sirolimus)



• 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.



• rasburicase

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.



• ravuconazole

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.



• RayGel

(Other name for: reduced glutathione-L-cysteine-anthocyanins gel)



• RC-1291 ghrelin mimetic

A synthetic, orally bioavailable, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. RC-1291 ghrelin mimetic binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite.



• rebeccamycin analogue

A synthetic diethylaminoethyl analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. The rebeccamycin analogue intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis.



• Rebif

(Other name for: recombinant interferon beta)



• 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.



• recombinant adenovirus-hIFN-beta

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 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.



• 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 fowlpox GM-CSF vaccine

A cancer vaccine 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 fowlpox-sargramostim 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-CEA-MUC-1-TRICOM vaccine

A cancer vaccine comprised of a recombinant fowlpox viral vector encoding the carcinoembryonic antigen (CEA), MUC-1, a transmembrane glycoprotein secreted by glandular epithelial tissues, and TRICOM, comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3). This agent may enhance CEA and MUC-1 presentation to antigen-presenting cells (APC) and activate a cytotoxic T-cell response against CEA- and MUC-1-expressing tumor 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 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 growth hormone

A recombinant form of endogenous human growth hormone (GH), a polypeptide produced by the anterior lobe of the human pituitary gland. GH exhibits growth-promoting effects and metabolic effects on carbohydrate, fat, protein and bone metabolism. GH stimulates protein synthesis and the uptake of amino acids into cells, and induces lipolysis in adipose tissues. The secretion of GH increases with sexual maturation and then declines steadily.



• recombinant interferon alfa-2b

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.



• 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. (NCI04)



• 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 interleukin-7

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 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 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 tissue plasminogen activator

A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, recombinant tPA increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism.



• recombinant tumor necrosis factor

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 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.



• Rectoid

(Other name for: hydrocortisone)



• reduced glutathione-L-cysteine-anthocyanins gel

A gel formulation containing reduced glutathione, L-cysteine, and anthocyanins with potential antioxifdant, immunostimulating, and chemoprotective properties. 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.



• Regitine

(Other name for: phentolamine mesylate)



• Remicade

(Other name for: infliximab)



• Remifemin

(Other name for: black cohosh)



• Remitogen

(Other name for: apolizumab)



• Rencarex

(Other name for: monoclonal antibody G250)



• Renova

(Other name for: tretinoin)



• resveratrol

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.



• Retin-A MICRO

(Other name for: tretinoin)



• retrovector encoding mutant anti-cyclin G1

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.



• Retrovir

(Other name for: zidovudine)



• Revival

(Other name for: soy protein isolate)



• Revlimid

(Other name for: lenalidomide)



• REXIN-G

(Other name for: retrovector encoding mutant anti-cyclin G1)



• rF-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.



• R-flurbiprofen

An orally active synthetic enantiomer of flurbiprofen. R-flurbiprofen activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in arrest of tumor cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumor cells. R-flurbiprofen does not inhibit the enzyme cyclo-oxygenase.



• rhEndostatin

(Other name for: recombinant human endostatin)



• Rheumatrex

(Other name for: methotrexate)



• risedronate

A synthetic pyridinyl bisphosphonate agent. Risedronate binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption



• Ritalin

(Other name for: methylphenidate hydrochloride)



• rituximab

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.



• RK-0202

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.



• Ro 50-3821

A pegylated form of recombinant human erythropoietin, a glycosylated protein naturally produced in the kidney that stimulates erythrocyte production in the bone marrow. Methoxypolyethylene glycol epoetin beta may reverse anemias induced by cancer therapy.



• Rocaltrol

(Other name for: calcitriol)



• Rodex

(Other name for: warfarin)



• rofecoxib

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.



• Roferon-A

(Other name for: recombinant interferon alpha-2a)



• romidepsin

A bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), thereby affecting the regulation of gene expression and inducing cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several HSP90-dependent oncoproteins.



• ropivacaine hydrochloride

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.



• roquinimex

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.



• 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.



• Roxicodone

(Other name for: oxycodone hydrochloride)



• Rubidomycin

(Other name for: daunorubicin hydrochloride)



• ruthenium Ru 106

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.



• rV-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.