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

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Showing 331 - 340 of 4227 results

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.
SU-14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3). SU-14813 was developed as a next-generation TKI agent following sunitinib (SU-11248) designed to demonstrate optimized pharmacokinetic (PK) and tolerability profiles. SU14813 demonstrated broad and potent antitumor activity equivalent to that of sunitinib, which resulted in tumor regression, growth arrest, growth delay, and prolonged survival in established xenograft cancer models in mice. A phase II trial of SU-14813 in patients with breast cancer was completed. However, according to the Pfizer pipeline development has been discontinued.
Status:
Investigational
Source:
NCT00690287: Phase 1 Interventional Completed Type 2 Diabetes
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02483182: Phase 2 Interventional Completed Herpes Labialis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

SIS Shulov Innovative Science is developing ZEP 3, a short synthetic peptide. This drug was studied in phase II clinical trial for the treatment of cold sores (Herpes labialis). In addition, was shown that ZEP-3 exhibited analgesic activity in various indications such as osteoarthritis, herpes labialis and ocular pain. In parallel, the company is planning a phase II clinical study in atopic dermatitis.
Status:
Investigational
Source:
NCT02965885: Phase 1 Interventional Completed Advanced Solid Tumors
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



TAS-116 is a highly potent oral HSP90 inhibitor with unique tissue distribution properties. TAS-116 has the potential to demonstrate antitumor activity, while being designed to limit certain adverse events by unique tissue distribution. Phase-II clinical trials in gastrointestinal stromal tumours are ongoing in Japan.
Status:
Investigational
Source:
NCT02005991: Phase 1 Interventional Completed Healthy
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
USAN:GILDEURETINOL ACETATE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alkeus Pharma's lead compound, ALK-001, is an oral compound with a well-understood mechanism of action. ALK-001 was specifically designed to prevent the formation of these toxic vitamin A dimers in the eye. ALK-001 is a chemically-modified vitamin A, in which 3 hydrogen atoms have been replaced by 3 deuterium atoms at carbon number 20. Replacing the retina's vitamin A with ALK-001 slows the formation of toxic vitamin A dimers. ALK-001 is in phase II clinical trials for the treatment of Stargardt's disease. The compound was co-developed by Alkeus Pharmaceuticals and Columbia University.
Status:
Investigational
Source:
NCT00847197: Phase 2 Interventional Completed Dyslipidemia
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



MK-1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist. Exhibits no binding at the GRP109B receptor. This drug had been in phase II clinical trial for the treatment of atherosclerosis and Dyslipidemia. But then, according to Merck, elevation of HDL cholesterol relative to placebo did not meet the trial's pre-specified primary objective for efficacy; no safety signals were implicated as drivers of the decision to discontinue development.
Status:
Investigational
Source:
NCT00868790: Phase 2 Interventional Terminated Type 2 Diabetes Mellitus
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MK 3577 is an orally active glucagon receptor antagonist which was under development by Merck & Co for the treatment of type 2 diabetes mellitus. MK 3577 demonstrate activity in cellular models and preclinical trials. In phase II clinical trials MK 3577 shows good efficacy and acceptable level of adverse events, but no further development reports were published.
Status:
Investigational
Source:
NCT01006122: Phase 2 Interventional Completed Excessive Daytime Sleepiness
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PF-03654746 is a potent, selective antagonist of the human H3 receptor, developed by Pfizer. It was in the clinical trial phase II for the treatment of excessive daytime sleepiness (EDS) associated with narcolepsy, Tourette syndrome as well as potential anti-allergy applications and in phase I of clinical trial for the treatment of Schizophrenia and Alzheimer's disease, but these investigations were discontinued.