CIENCIASMEDICASNEWS: NCI Drug Dictionary - National Cancer Institute

NCI Drug Dictionary - National Cancer Institute

299 results found for: R

Revival: (Other name for: soy protein isolate)
Revlimid: (Other name for: lenalidomide)
RevM10 gene: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
REXIN-G: (Other name for: retrovector encoding mutant anti-cyclin G1)
rexinoid NRX194204: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rezulin: (Other name for: troglitazone)
RFT5-dgA immunotoxin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rhEndostatin: (Other name for: recombinant human endostatin)
rhenium Re 188 BMEDA-liposome: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rhenium Re 188 ethiodized oil: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rheumatrex: (Other name for: methotrexate)
rhizoxin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rhubarb/licorice herbal supplement: 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.
ribavirin: 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 trialsusing this agent. (NCI Thesaurus)
ribociclib: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
riboflavin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
ribonuclease QBI-139: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
ribosome-inactivating protein CY503: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Riboxamide: (Other name for: tiazofurin)
rice bran: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
R-ICE regimen: 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. (NCI Thesaurus)
ricolinostat: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
ridaforolimus: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Ridaura: (Other name for: auranofin)
rifabutin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rifaximin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
RIG-I selective ligand RGT100: 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.
rigosertib sodium: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rilimogene galvacirepvec: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rilimogene galvacirepvec/rilimogene glafolivec: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rilotumumab: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rilutek: (Other name for: riluzole)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
rimiducid: 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 trialsusing this agent. (NCI Thesaurus)
rindopepimut: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rintatolimod: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Riomet: (Other name for: metformin hydrochloride)
risedronate sodium: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
risperidone formulation in rumenic acid: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Ritalin: (Other name for: methylphenidate hydrochloride)
ritonavir: 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 trialsusing this agent. (NCI Thesaurus)
Rituxan: (Other name for: rituximab)
Rituxan Hycela: (Other name for: rituximab and hyaluronidase human)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
rituximab and hyaluronidase human: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rituximab conjugate CON-4619: 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.
rivaroxaban: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rivastigmine tartrate: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rizatriptan benzoate: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
RNA electroporated CD19CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
RNAdjuvant: (Other name for: ssRNA-based immunomodulator CV8102)
RNR inhibitor COH29: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
robatumumab: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Robimycin: (Other name for: erythromycin)
Robinul: (Other name for: glycopyrrolate)
Rocaltrol: (Other name for: calcitriol)
Rocephin: (Other name for: ceftriaxone sodium)
rociletinib: 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.
ROCK2 inhibitor KD025: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rocuronium bromide: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Roferon-A: (Other name for: recombinant interferon alpha-2a)
roflumilast: 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.
rolapitant hydrochloride: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rolontis: (Other name for: eflapegrastim)
romidepsin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
romiplostim: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Romozin: (Other name for: troglitazone)
roniciclib: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
ropidoxuridine: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
ropinirole hydrochloride: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ROR1 CAR-specific autologous T lymphocytes: 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 trialsusing this agent. (NCI Thesaurus)
RORgamma agonist LYC-55716: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rosiglitazone maleate: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rostaporfin: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rosuvastatin calcium: 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 trialsusing this agent. (NCI Thesaurus)
Rotarix: (Other name for: rotavirus vaccine)
rotavirus vaccine: A viral vaccine that prevents against rotavirus infection, the leading cause of severe acute gastroenteritis. Check for active clinical trials using this agent. (NCI Thesaurus)
Rou Cong Rong: 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 trialsusing this agent. (NCI Thesaurus)
rovalpituzumab tesirine: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rowasa: (Other name for: mesalamine)
roxadustat: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Roxanol: (Other name for: morphine sulfate)
Roxicodone: (Other name for: oxycodone hydrochloride)
Rozerem: (Other name for: ramelteon)
RP-Mycin: (Other name for: erythromycin)
RSV fusion inhibitor GS-5806: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
rubitecan: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rubraca: (Other name for: rucaparib camsylate)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
rucaparib phosphate: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
ruthenium-based photosensitizer TLD1411: 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.
ruthenium-based transferrin targeting agent NKP-1339: 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.
ruxolitinib phosphate: 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Rydapt: (Other name for: midostaurin)