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

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Showing 1441 - 1450 of 24164 results

Status:
Investigational
Source:
NCT00384423: Phase 2 Interventional Completed Alzheimer's Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PRX-03140 is a partial agonist of the 5-HT4 receptor that is being developed by EPIX Pharmaceuticals for Alzheimer's disease. In vitro shows potent binding to 5-HT4 receptor and increased cAMP production in human embryonic kidney-293 cells expressing recombinant rat 5-HT(4) receptors. In the clinical trial, PRX-03140 was associated with a statistically significant improvement in the Alzheimer’s Disease Assessment Scale.
Status:
Investigational
Source:
INN:sipagladenant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00401284: Phase 2 Interventional Completed Sleep Initiation and Maintenance Disorders
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:linarotene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Linarotene is arotinoid derivative. It is an antikeratolytic agent. Linarotene had been in preclinical phase by Ortho Pharmaceutical (Johnson & Johnson) and BASF Pharma for the treatment of skin disorders. However, this research was discontinued.
Status:
Investigational
Source:
NCT00436852: Phase 2 Interventional Completed Disseminated Neuroblastoma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


ABT-751 is an orally bioavailable antimitotic sulfonamide, which binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, leads to a block in the cell cycle at the G2M phase, resulting in cellular apoptosis. ABT-751 had been in phase Ⅱ clinical studies for the treatment of breast cancer; colorectal cancer; non-small cell lung cancer; renal cancer, prostate cancer, but these researches have been discontinued.
Luminespib (NVP-AUY922) is a highly potent isoxazole-based, nongeldanamycin HSP90 inhibitor that inhibits the adenosine triphosphatase activity of HSP90. Luminespib is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib potently inhibited in vitro growth in all 41 NSCLC cell lines evaluated with IC50 less than 100 nM. IC100 value less than 40 nM was seen in 36 of 41 lines. Luminespib (NVP-AUY922) has greater potency, reduced hepatotoxicity, and lower dependence on DT-diaphorase than the first-generation HSP90 inhibitors. Luminespib was discovered in a multiparameter lead optimization program based on a high-throughput screening hit methodology developed jointly by The Institute of Cancer Research, UK and the pharmaceutical company Vernalis. It has been licensed to Novartis. Luminespib activity is independent of NQO1/DT-diaphorase, maintained in drug-resistant cells and under hypoxic conditions. The molecular signature of HSP90 inhibition, comprising induced HSP72 and depleted client proteins, was readily demonstrable. Pre-clinical studies proved that Luminespib acts via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis. These results helped Luminespib to enter clinical trials for various cancers including breast cancers. From 2011 to 2014 it was in Phase II clinical trials.
Status:
Investigational
Source:
NCT02266745: Phase 2 Interventional Active, not recruiting Advanced Solid Tumors
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03212170: Phase 2 Interventional Active, not recruiting Invasive Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03863574: Phase 2 Interventional Completed Non Alcoholic Steatohepatitis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Saroglitazar, a dual peroxisome proliferator-activated receptor PPAR-α/γ agonist, was an emerging therapeutic option on glycemic and lipid parameters. The Zydus Group has launched LipaglynTM ((Saroglitazar) in India for diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In addition, saroglitazar participated in phase II clinical trials that completed enrolment in patients with primary biliary cholangitis and in patients with non-alcoholic steatohepatitis.
Status:
Investigational
Source:
NCT02457273: Phase 2 Interventional Completed Neuroendocrine Carcinomas
(2015)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Showing 1441 - 1450 of 24164 results