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

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Showing 61 - 70 of 262 results

Status:
Investigational
Source:
INN:zimlovisertib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Voruciclib (also known as P1446A-05) is a flavone-based, potent and selective CDK 4/6 inhibitor with activity in multiple BRAF-mutant and wild type cell lines. It is currently in clinical trials in combination with BRAF inhibitor (PLX4032) to treat advanced BRAF-mutant melanoma. Voruciclib has significant inhibitory activity against cutaneous and uveal melanoma. Mechanistic studies revealed that P1446A-05 inhibits phosphorylation targets of CDK members, and induces cell cycle arrest and apoptosis irrespective of melanoma genotype or phenotype. Voruciclib Hydrochloride is in phase I clinical trials by Piramal Life Sciences for the treatment of chronic lymphocytic leukaemia and malignant melanoma.
Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Lucitanib (E-3810) is a novel multi-kinase inhibitor currently in clinical trials for its anti-angiogenic and anti-tumor activity. A Phase I/IIa clinical trial of lucitanib was initiated in 2010 and has demonstrated multiple objective responses in FGFR1 gene-amplified breast cancer patients, and objective responses were also observed in patients with tumors often sensitive to VEGFR inhibitors, such as renal cell and thyroid cancer. Lucitanib is an oral, potent inhibitor of the tyrosine kinase activity of fibroblast growth factor receptors 1 through 3 (FGFR1-3), vascular endothelial growth factor receptors 1 through 3 (VEGFR1-3) and platelet-derived growth factor receptors alpha and beta (PDGFR alpha-beta). The most common adverse events were hypertension, asthenia, and proteinuria.
Status:
Investigational
Source:
NCT02499497: Phase 2 Interventional Completed Prostate Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.
Status:
Investigational
Source:
INN:gluceptate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gluceptate sodium also known as sodium glucoheptonate (H-Quest A300) is a non-toxic, a non-hazardous chelating agent, which forms stable complexes with di- and trivalent metal ions such as Ca2+, Fe2+, Fe3+, Al3+, etc. This substance is highly compatible with strong alkaline mediums and can prevent the bacterial degradation of the solution. Gluceptate sodium has various applications in water treatment, agricultural, cosmetics, textile processing and in some others fields.
Status:
Investigational
Source:
INN:lanopepden [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LANOPEPDEN is an inhibitor of peptide deformylase, a bacterial enzyme required for protein maturation. It was in development for the treatment of complicated bacterial skin infection and hospitalized community-acquired pneumonia.
Status:
Investigational
Source:
INN:epetraborole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Epetraborole (AN3365 or GSK2251052) is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase. It is active against Gram-negative bacteria, including Enterobacteriaceae bearing NDM-1 and KPC carbapenemases, as well as P. aeruginosa. Epetraborole was under development for the treatment of Gram-negative bacterial infections.
Status:
Investigational
Source:
NCT03456804: Phase 2 Interventional Completed Castration Levels of Testosterone
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

CEP-11981 is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR) and Tie2 receptor tyrosine kinases with potential antiangiogenic and antineoplastic activities. Preclinical studies have shown that CEP-11981 exhibits promising permeability, metabolic stability, and pharmacokinetic properties across multiple species. Studies of pharmacologic activity across angiogenesis assays, animal tumor models, and human tumor models have shown sustained, dose-related antiangiogenic and antitumor inhibition. In clinical trals CEP-11981 administration leads to disease stabilization in patients with recurrent or refractory solid tumors. Despite acceptable tolerability of CEP-11981 at the MTD, further development by the sponsor has ceased.
Status:
Investigational
Source:
NCT01020799: Phase 2 Interventional Completed Major Depressive Disorder
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)