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

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Showing 1421 - 1430 of 24164 results

Status:
Investigational
Source:
NCT02350426: Phase 1 Interventional Terminated Arthritis, Rheumatoid
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Flutriciclamide F18 (18F-GE-180), a translocator protein (TSPO)-PET radiotracer was used using in different pathologies. This agent was studied in phase I clinical trial to assess inflammation in rheumatoid arthritis. However, this study was terminated because of the pre-defined stopping criteria in the protocol.
Status:
Investigational
Source:
NCT00356434: Not Applicable Interventional Terminated Thrombophilia
(2008)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Spiroxamine is a spirodecane derivative patented by German multinational pharmaceutical and life sciences company Bayer A.-G. as agrochemical fungicide. Spiroxamine acts as a sterol biosynthesis inhibitor with systemic activity. This active ingredient provides control of powdery mildew caused by the ascomycetous fungus, Uncinula necator (syn. Erysiphe necator) in grapes. In laboratory animals, the technical grade Spiroxamine was moderate to highly acutely toxic by the oral route and slightly acutely toxic by the dermal and inhalation routes of exposure. Spiroxamine was non-irritating to the eyes but moderately irritating to the skin. Spiroxamine caused an allergic skin reaction. Health effects in animals given repeated doses of Spiroxamine included effects on the liver, lining of the gastrointestinal and urogenital tracts, the eye and body weight. Spiroxamine did not cause cancer in animals and did not damage genetic material.
Status:
Investigational
Source:
NCT01927666: Not Applicable Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04669067: Phase 1/Phase 2 Interventional Active, not recruiting Acute Myeloid Leukemia
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials. Based on X-ray cocrystal structures a model of AMG 232 bound to MDM2 was developed. The model shows that the m-chlorophenyl, the p-chlorophenyl, and C-linked isopropyl fragments of AMG 232 bind to the Leu 26(p53), Trp 23(p53), and Phe 19(p53) pockets of MDM2, respectively. The carboxylic acid forms a salt bridge with His 96 and the isopropyl sulfone forms a novel interaction with the glycine shelf region of MDM2. AMG 232 in phase II in combination with trametinib and dabrafenib in subjects with metastatic melanoma; in phase I for the treatment of solid tumors, multiple myeloma and Acute Myeloid Leukemia.
Status:
Investigational
Source:
NCT03078322: Phase 2 Interventional Completed Major Depressive Disorder
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

4‐Chlorokynurenine (AV-101) is a neuropharmaceutical drug candidate in development for the treatment of major depressive disorder. Pharmacology studies conducted in rodent models have demonstrated AV-101’s antihyperalgesic activity in models of facilitated pain processing was seen at serum concentrations ranging from 150–300 M. In addition, AV-101 has been shown to be neuroprotective activity against an intrahippocampal injection of quinolinic acid, reductions in seizures, and antidepressive activity. An oral prodrug, AV-101, which, in the brain, is converted into one of the most potent and selective GlyB site antagonists of the NMDAR, has been demonstrated to be active in animal models of neuropathic pain. The two Phase 1 studies were designed to assess the safety and pharmacokinetics of AV-101, over a wide dose range, after daily dosing for 14-days. AV-101 has excellent safety and PK characteristics providing support for advancing AV-101 into Phase 2 studies in neuropathic pain.
Status:
Investigational
Source:
NCT03045861: Phase 2 Interventional Completed Infection, Human Immunodeficiency Virus
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT01081275: Phase 2 Interventional Unknown status Multiple Sclerosis
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03547115: Phase 1 Interventional Recruiting Follicular Lymphoma (FL)
(2018)
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.
Status:
Investigational
Source:
NCT03011320: Phase 1 Interventional Completed Ovary Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03255096: Phase 1 Interventional Completed Diffuse Large B-cell Lymphoma
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 1421 - 1430 of 24164 results