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

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Showing 51 - 60 of 735 results

Status:
Investigational
Source:
NCT04452435: Phase 2 Interventional Completed COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Compound M24 is a selective angiotensin II AT2 receptor agonist with a Ki value of 0.4 nM for the AT2 receptor. Compound enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. In a mouse model of atherosclerosis, plaque size and stability were improved in ApoE‐/‐ mice treated with M24. Treatment with M24 resulted in decrease in scar size and reduction in markers of inflammation in a rat model of myocardial infaction.
Status:
Investigational
Source:
NCT03976076: Phase 2 Interventional Terminated Refractory Infantile Spasms
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

BMS-690514 is a potent, reversible oral inhibitor of epidermal growth factor receptor (EGFR/HER-1), HER-2 and -4, and vascular endothelial growth factor receptors (VEGFRs)-1 to -3 offering targeted inhibition of tumour growth and vascularisation in a single agent. Bristol-Myers Squibb was developing BMS 690514, as an oral treatment for cancer. BMS-690514 had being in phase II for the treatment of breast cancer; non-small cell lung cancer, but later these studies were discontinued.
Status:
Investigational
Source:
NCT03110549: Phase 1 Interventional Terminated Human Immunodeficiency Virus
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MX-100 (also known as PL-100) is a benzenesulfonamide derivative patented by Pharmacor Inc as HIV aspartyl protease inhibitor. MX-100 retained excellent antiviral activity against almost all of these protease inhibitor-resistant viruses and that its performance in this regard was superior to those of atazanavir, amprenavir, indinavir, lopinavir, nelfinavir, and saquinavir. In almost every case, the increase in the EC50 for MX-100 observed with viruses containing multiple mutations in protease was far less than that obtained with the other drugs. Preclinical studies showed that MX-100 possessed suboptimal solubility and pharmacokinetic, (PK) properties, possibly hindering further development. MX-100 successfully completed preclinical and clinical development (phase I in healthy volunteers) and have been licensed to Merck in 2006
Status:
Investigational
Source:
NCT00838162: Phase 2 Interventional Completed Human Immunodeficiency Virus Type 1
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ASC-09 orTMC-310911, a HIV protease inhibitor, participated in phase II clinical for the treatment of Human Immunodeficiency Virus Type 1. However, no recent development has been reported.
Status:
Investigational
Source:
INN:lorbamate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lorbamate is a carbamate that has been studied for use as a skeletal muscle relaxer and tranquilizer. It is GABA-A receptors agonist.
Status:
Investigational
Source:
NCT02573870: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.
Status:
Investigational
Source:
NCT01859962: Phase 2 Interventional Completed Chronic Hepatitis C
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ravidasvir (RDV, ASC16) is a second‐generation, pan‐genotypic non‐structural (NS) 5A inhibitor, which inhibits viral replication and assembly. Ravidasvir exhibits high antiviral potency with EC50 0.04–1.14 nM for HCV GT1–GT6. The pharmacokinetics results indicated that steady status achieved quickly after the first dose. Metabolism studies utilizing human clinical samples showed that Ravidasvir was very stable, with only modest (~2%) metabolite formation. Biliary excretion of Ravidasvir appears to be the primary route of elimination of the absorbed dose, while renal excretion of the intact drug appears to be negligible. In clinical trans twelve-week Ravidasvir and ritonavir-boosted Danoprevir in combination with ribavirinfor 12 weeks achieve the sustained virologic response rate of 100% in treatment-naïve non-cirrhotic Asian patients with HCV GT1 infection. Ravidasvir for treatment‐naïve, non‐cirrhotic HCV GT1 patients was safe and well tolerated. There was no death, treatment‐related serious adverse events, and discontinued cases due to adverse events.
Status:
Investigational
Source:
NCT02082457: Phase 2 Interventional Completed Irritable Bowel Syndrome
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Relenopride (YKP-10811) is a serotonin 4 (5-HT4) receptor agonist that was developed for regulation of gastric motility. It improved antral contractions and accelerated gastric emptying in dogs and had no adverse effects. Phase II clinical trials have investigated the efficacy and safety of relenopride in patients with (chronic and functional) constipation and irritable bowel syndrome (IBD). Relenopride was reported to accelerate gastrointestinal motility and colonic transit and improve bowel functions in patients with functional constipation, compared with placebo.
Status:
Investigational
Source:
NCT01168817: Phase 2 Interventional Completed Erectile Dysfunction
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Nelociguat, a soluble guanylate cyclase (sGC) activator, has been in phase II clinical trials by Bayer for the treatment of erectile dysfunction and heart failure. However, no recent development has been reported. Nelociguat is a direct soluble guanylate cyclase (sGC) stimulator that acts independently of nitric oxide (NO); has an EC50 of 353 nM on P-VASP formation in rat aortic smooth muscle cells. BAY 60-4552 is pharmacologically active major metabolite of Riociguat.