U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 281 - 290 of 402 results

Status:
Possibly Marketed Outside US
Source:
AGELOC TRANSFORMATION by Liebig, J.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Creatinine is a product of metabolism of creatine phosphate, a molecule that serves as a rapidly mobilizable reserve of a brain and skeletal muscle. Creatinine is excreted by kidneys with little or no reabsorption. Serum creatinine is the most commonly used indicator of renal function.
Broxuridine (5-Bromo-2-deoxyuridine, BrdU) is a thymidine analogue that is incorporated into replicating DNA. BrdU taken up by cells is phosphorylated and incorporated into DNA in place of dT. Although originally designed as a chemotherapeutic agent, sublethal concentrations of BrdU have long been known to alter the growth and phenotype of a wide range of cell types. The most popular use of BrdU is as a tracer of DNA synthesis. The other well-known use of BrdU is as a DNA photosensitizer. BrdU substitution of dT in DNA sensitizes it to near-UV light, and cells with BrdU-substituted DNA cannot survive after exposure to near-UV light. BUdR has side effects on cell functions. Cell growth can be inhibited, normal development of differentiating systems be perturbed, activities of specific enzymes be reduced. Mutagenic effects of BUdR are interpreted as reflections of a mispairing of BUdR in its rare enol form. Effects of BUdR which can be reversed by addition of thymidine are not likely to be mutagenic. As another mechanism of action of BUdR has been suggested that incorporation of BUdR into DNA alters the pattern of transcription.
Status:
Possibly Marketed Outside US
Source:
NCT04668118: Phase 4 Interventional Unknown status Dry Eye Syndromes
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Diquafosol, a dinucleotide Up4U, is an agonist for purinergic P2Y2 receptor. Diquafosol stimulated water and mucin secretion by acting on P2Y2 receptors on the conjunctival epithelial and goblet cell membrane and elevating intracellular calcium ion concentrations. The Japanese Ministry of Health, Labour and Welfare granted approval for DIQUAS Ophthalmic Solution 3% (diquafosol tetrasodium) for the treatment of dry eye.
Status:
Possibly Marketed Outside US
Source:
NCT03391440: Phase 4 Interventional Unknown status Pelvic Inflammatory Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Morinidazole is a novel third generation 5-nitroimidazole-class antimicrobial agent indicated for the treatment of anaerobic bacterial infections including appendicitis and pelvic inflammatory disease. Morinidazole is administered as a racemate. Morinidazole was approved by China Food and Drug Administration (CFDA) on February, 2014. The bactericidal activity of morinidazole, depends on the formation of a redox intermediate metabolite in the bacterium that causes DNA strand breakage, inhibits repair, and, ultimately leads to cell death. The main adverse effects (all are mild) relate to the drug are dizziness, drowsiness and nausea. Recent in vitro assays have demonstrated that higher antiparasitic potency is observed in S- morinidazole than in R-morinidazole.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Cediranib (AZD-2171) is a VEGFR-2 kinase inhibitor which was developed by AstraZeneca for the treatment of cancer. The drug reached the final stage of approval by European Medicines Agency in 2008 under the name Zemfirza (it was recommended to be taken in combination with platinum-based chemotherapy), however on 19 September 2016 AstraZeneca decided to withdraw the Marketing Authorisation Application.
Status:
Possibly Marketed Outside US
Source:
KALGUT by Tanabe Seiyaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Denopamine is a selective agonist of beta-1 adrenergic receptor. The drug was approved in Japan under the name Kalgut for the treatment of chronic heart failure.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Epacadostat (INCB024360) is an orally available hydroxyamidine and inhibitor of indoleamine 2,3- dioxygenase (IDO1). It shows little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat displays potential immune modulating and antineoplastic activities. Epacadostat has been tested in phase II and III studies for the treatment of malignant melanoma, fallopian tube cancer, non-small cell lung cancer, ovarian cancer, peritoneal cancer, solid tumors, pancreatic cancer. The most common detected adverse events were fatigue, nausea, decreased appetite, vomiting, constipation, abdominal pain, diarrhea, dyspnea, back pain, and cough.
Status:
Possibly Marketed Outside US
Source:
NCT03376958: Phase 4 Interventional Completed Relapsed and Refractory
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Apatinib is an orally bioavailable, small molecule tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 and used for the treatment of metastatic gastric cancer or gastroesophageal junction cancer that has progressed or relapsed after chemotherapy. To date, second-line ramucirumab and third-line Apatinib are the only anti-angiogenic approaches that have significantly improved the survival of patients with metastatic gastric cancer. Apatinib exhibited potent, highly-selective inhibition of VEGFR-2, c-kit, c-src, and RET tyrosine kinases. The efficacy of Apatinib monotherapy in patients with metastatic gastric cancer or gastroesophageal junction cancer for whom at least two prior chemotherapy regimens had failed was demonstrated in randomized open-label or double-blind phase II trials and a pivotal placebo-controlled phase III trial, all of which were conducted in China. Further clinical experience and long-term pharmacovigilance are required to definitively establish the efficacy and safety profile of Apatinib, including its use in combination with other chemotherapeutic agents.
Status:
Possibly Marketed Outside US
Source:
NCT02294396: Phase 4 Interventional Completed Overactive Bladder (OAB)
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Imidafenacin (KRP-197/ONO-8025) is the latest antimuscarinic (AM) developed for the treatment of overactive bladder syndrome (OAB) and, at the moment, it is marketed only in Japan. It has high affinities for the M3 and M1 muscarinic receptor subtypes, a low affinity for M2 receptors, and a potent inhibitory activity against rhythmic bladder contractions. Imidafenacin has excellent efficacy, tolerability, and safety. It is indicated for patients with nocturia, nocturnal polyuria, and benign prostatic hyperplasia.

Showing 281 - 290 of 402 results