Disease & Drug Info

Drug Dictionary

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. Check for active clinical trials using this agent. (NCI Thesaurus)

R1 Cooling Gel Plus R2 Moisturizing/Sun Protecting Lotion

A skin care treatment system consisting of a cytokine-containing milk-based cooling gel and a cytokine-containing milk-based soothing lotion with hydrating and potential protective activity against radiation-induced dermatitis. Application of the R1 cooling gel immediately upon radiation treatment may hydrate the skin, provide cooling relief, and may protect the skin against radiation-induced dermatitis. The subsequent application of the R2 lotion moisturizes the skin while also protecting the skin against inflammation. In addition, R2 contains avobenzone, homosalate, octinoxate and octocrylene, which exert UVA and UVB skin protective activity. Check for active clinical trials using this agent.

rabeprazole sodium

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. Check for active clinical trials using this agent. (NCI Thesaurus)

rabusertib

An inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

racemic XK469

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. Check for active clinical trials using this agent. (NCI Thesaurus)

racotumomab

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. Check for active clinical trials using this agent. (NCI Thesaurus)

RadiaPlex Rx Gel

(Other name for: sodium hyaluronate topical hydrogel)

radiosensitizer RRx-001

A dinitroazetidine derivative with potential radiosensitizing activity. Upon administration, RRx-001 is able to dilate blood vessels, thereby increasing tumor blood flow and thus improving oxygenation to the tumor site. By increasing oxygen levels, these tumor cells may be more susceptible to radiation therapy. Tumor hypoxia is correlated with tumor aggressiveness, metastasis and resistance to radiotherapy. Check for active clinical trials using this agent. (NCI Thesaurus)

radium Ra 223 dichloride

A radiopharmaceutical composed of the dichloride salt of the alpha-emitting isotope radium Ra 223, with antineoplastic activity. Like calcium, radium targets bone tissue and preferentially accumulates in osteoblastic lesions, such as those seen in areas of bone metastases. Radium Ra 223 forms complexes with hydroxyapatite and becomes incorporated into the bone matrix. The radioisotope Ra 223 kills bone cancer cells through local emission of high energy alpha particles, causing DNA double-strand breaks and tumor regression in the skeleton. The short range effects of alpha emission allows for localized DNA damage with limited toxicity to nearby healthy bone tissue. Check for active clinical trials using this agent. (NCI Thesaurus)

Radix Angelicae sinensis/Radix Astragali herbal supplement

A traditional Chinese medicine comprising of Radix Angelicae Sinensis (RAS) and Radix Astragali (RA), with potential anti-inflammatory, immunostimulatory, neuroprotective, anti-hepatotoxic and antineoplastic activities. The main chemical constituents of RAS include ferulic acid, Z-ligustilide, butylidenephthalide and various polysaccharides. RA is the dried root of Astragalus membranaceus with primary constituents such polysaccharides, triterpenoids as well as isoflavones. Though their mechanisms of action remain largely elusive, Radix Angelicae Sinensis/Radix Astragali herbal supplements are commonly used for the treatment of various health conditions affecting women including premenstrual syndrome, dysmenorrhea, pelvic pain, recovery from childbirth and menopausal symptoms. These agents are also used for alleviating constipation, preventing and treating anemia and allergic attacks, and for the management of hypertension, joint pain and ulcers. Check for active clinical trials using this agent. (NCI Thesaurus)

radotinib hydrochloride

An orally available, hydrochloride salt form of radotinib, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. Check for active clinical trials using this agent.

rAD-p53

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Raf kinase inhibitor HM95573

An orally available inhibitor of members of the Raf family of serine/threonine protein kinases, with potential antineoplastic activity. Upon administration, Raf kinase inhibitor HM95573 binds to and inhibits the B-Raf mutant V600E and C-Raf. This inhibits B-Raf V600E- and C-Raf-mediated signal transduction pathways, thereby inhibiting tumor cell growth of susceptible tumor cells. In addition, HM95573 may also inhibit mutated Ras proteins. Raf protein kinases play a key role in the Raf/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. The Raf mutation B-Raf V600E, where the valine at residue 600 is substituted for glutamic acid, is frequently overexpressed in a variety of human tumors and results in the constitutive activation of the Raf/MEK/ERK signaling pathway. Check for active clinical trials using this agent. (NCI Thesaurus)

Raf kinase inhibitor LGX818

An orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

raloxifene hydrochloride

The hydrochloride salt form of raloxifene, a selective benzothiophene estrogen receptor modulator (SERM) with lipid lowering effects and activity against osteoporosis. Raloxifene hydrochloride specifically binds to estrogen receptors in responsive tissue, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it promotes or suppresses the transcription of estrogen-regulated genes, thereby exerting its agonistic or antagonistic effects. This agent functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In tissue like bone, it decreases bone resorption and bone turnover and increases bone mineral density. Raloxifene hydrochloride acts as an estrogen antagonist in uterine and breast tissue. This agent also exerts an anti-proliferative effect on estrogen-sensitive breast cancer. Check for active clinical trials using this agent. (NCI Thesaurus)

raltegravir potassium

The orally bioavailable potassium salt of a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. Check for active clinical trials using this agent. (NCI Thesaurus)

raltitrexed

A quinazoline folate analogue with antineoplastic activity. After transport into cells via the reduced folate carrier, raltitrexed undergoes intracellular polyglutamation and blocks the folate-binding site of thymidylate synthase, thereby inhibiting tetrahydrofolate activity and DNA replication and repair and resulting in cytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)

ramelteon

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ramipril

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ramosetron hydrochloride

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ramucirumab

A recombinant, fully human monoclonal antibody directed against human vascular endothelial growth factor receptor 2 (VEGFR-2) with antiangiogenesis activity. Ramucirumab specifically binds to and inhibits VEGFR-2, which may result in an inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells. Check for active clinical trials using this agent. (NCI Thesaurus)

Ranexa

(Other name for: ranolazine)

ranibizumab

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. Check for active clinical trials using this agent. (NCI Thesaurus)

ranimustine

A chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

ranitidine hydrochloride/bismuth potassium citrate/sucralfate hydrate formulation

A formulation containing the hydrochloride salt form of the non-imidazole histamine H2 receptor antagonist ranitidine, bismuth potassium citrate, and the hydrate form of sucralfate, a basic aluminum complex of sulfated sucrose, with potential antacid, radio- and cytoprotective activities. Upon oral administration of the ranitidine hydrochloride/bismuth potassium citrate/sucralfate hydrate formulation, ranitidine binds to and blocks the activity of the histamine H2 receptors in the parietal cells in the stomach and in the gastrointestinal (GI) tract, thereby decreasing acid secretion. Sucralfate physically binds to the surface of damaged mucosa, thereby forming a protective barrier that shields the GI tract from stomach acid. It also neutralizes stomach acid. Bismuth inhibits peptic activity, increases mucosal secretions and acts as a barrier to prevent damage by acid. Altogether, this protects against ulcer formation and may help to heal existing ulcers. Check for active clinical trials using this agent. (NCI Thesaurus)

ranolazine

An orally available, piperazine derivative with anti-anginal and potential antineoplastic activities. Ranolazines mechanism of action for its anti-ischemic effects has yet to be fully elucidated but may involve the alteration of the trans-cellular late sodium current in the ischemic myocyte. By preventing the rise of intracellular sodium levels, ranolazine may affect the transport activity of sodium-dependent calcium channels and prevent the calcium overload during myocardial ischemia, thereby preventing cellular injury. Ranolazines potential antineoplastic effect may depend on its inhibitory effect on fatty acid oxidation, which may sensitize tumor cells to apoptosis and decrease tumor cell proliferation; fatty acid oxidation provides energy and promotes tumor cell proliferation and survival. Check for active clinical trials using this agent.

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Rapaflo

(Other name for: silodosin)

Rapamune

(Other name for: sirolimus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Rayaldee

(Other name for: modified-release calcifediol capsule)

RayGel

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

Razadyne

(Other name for: galantamine hydrobromide)

razoxane

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. Check for active clinical trials using this agent. (NCI Thesaurus)

R-CHOP regimen

An immunochemotherapy regimen consisting of rituximab, cyclophosphamide, hydroxydaunorubicin hydrochloride (doxorubicin hydrochloride), vincristine (Oncovin) and prednisone used to treat both indolent and aggressive forms of non-Hodgkin lymphoma. (NCI Thesaurus)

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