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

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Showing 1791 - 1800 of 24423 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pramiconazole is a novel azole with potent antifungal activity against yeasts, dermatophytes and many other fungal species. It is a new addition to the family of triazole antifungal agents that act by inhibiting fungal cell membrane ergosterol synthesis, thereby leading to increased cell permeability and destruction. In preclinical studies, pramiconazole exhibited similar or superior antifungal activity to ketoconazole and itraconazole, and selectively inhibited ergosterol synthesis with a broad spectrum activity. Pramiconazole was absorbed rapidly and had a long half-life, allowing for once-daily dosing. In phase I and II clinical trials, pramiconazole reduced the growth of Candida albicans, Malassezia globosa, Microsporum canis, Trichophyton mentagrophytes and Trichophyton rubrum, and was generally well tolerated. Pramiconazole is a well-tolerated and effective treatment for pityriasis versicolor.
Status:
Investigational
Source:
INN:ioprocemic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ioprocemic Acid is hydrocinnamic acid derivative patented by Schering-Kahlbaum A.-G. as radiographic contrast medium for liver imaging
Status:
Investigational
Source:
NCT00296569: Phase 2 Interventional Completed Osteoarthritis
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MK-0686 is a bradykinin B1 receptor antagonist patented by American multinational pharmaceutical company Merck & Co for the treatment of neuropathic pain and inflammation. MK-0686 demonstrates significantly reduced susceptibility to human P-gp mediated efflux and shows good potential for human CNS penetration based on brain levels in CF-1 mice and monkeys. Additionally, MK-0686 also exhibited good CNS bradykinin B1 receptor occupancy in the transgenic rat expressing the human B1 receptor and showed oral efficacy in reducing CFA-induced hyperalgesia in a humanized mouse. Unfortunately, in phase II clinical trials MK-0686 failed to demonstrate efficacy in phase II clinical trials.
Status:
Investigational
Source:
INN:profexalone [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Profexalone is an oxazolidinone derivative patented by Delalande S. A. as anticonvulsive, muscle-relaxant, antidepressive, anti-inflammatory, and analgesic compound.
Status:
Investigational
Source:
INN:glenvastatin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Glenvastatin (HR780) is a synthetic HMG-CoA reductase (HMGCR) inhibitor. Like other statins, glenvastatin shows very low systemic bioavailability due to an extensive first pass effect at the intestinal and/or hepatic level. This is a positive trait, since the liver is the target organ for statins. Evidence has been found that glenvastatin protects the vascular endothelium from oxidant stress and inhibits the migration and proliferation of smooth muscle cells. In rabbits, long-term treatment with glenvastatin reduces the plasma cholesterol level, and decreases the liver cholesterol contents. There are no results of clinical trials for glenvastatin.
Status:
Investigational
Source:
NCT01033097: Phase 2 Interventional Completed Pruritus in Patients With Atopic Dermatitis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:indanidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Indanidine is a selective and effective α2-antagonist, α1-partial agonist patented by pharmaceutical company Siegfried A.-G as a low toxic compound with direct hypotensive action. Indanidine does not penetrate the blood-brain barrier, does not induce drug-metabolizing enzymes in the liver, does not cause behavioral changes.
Status:
Investigational
Source:
INN:phenomorphan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Phenomorphan is the μ-opioid receptor agonist. Phenomorphan is a synthetic narcotic analgesic structurally related to racemorphan and racemethorphan. It has no accepted medicinal value in the United States.
Status:
Investigational
Source:
NCT00743925: Phase 2 Interventional Completed Acute Coronary Syndrome
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.
Status:
Investigational
Source:
NCT00233909: Phase 1/Phase 2 Interventional Completed Leukemia, Myeloid
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zosuquidar (LY-335979) is an experimental antineoplastic drug. It is is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Zosuqidar was initially characterized by Syntex Corporation, which was acquired by Roche in 1990. Roche licensed the drug to Eli Lilly in 1997. It was granted orphan drug status by the FDA in 2006 for AML. Zosuquidar Trihydrochloride had been in phase III clinical trials by Kanisa Pharmaceuticals for the treatment of acute myeloid leukaemia. However, this research has been discontinued.

Showing 1791 - 1800 of 24423 results