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

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Showing 1271 - 1280 of 34955 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)



Y-700 (Niraxostat or 1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid) is an inhibitor of xanthine oxidoreductase. Y-700 demonstrated high oral bioavailability being predominantly eliminated via the liver. It potently reduces serum uric acid levels. Y-700 was in clinical trials for the treatment of gout.
Status:
Investigational
Source:
INN:alamifovir
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Alamifovir is a novel antiviral agent which was under development with Mitsubishi Pharma Corporation in Japan as a potential treatment for hepatitis B (HBV). Alamifovir and its hydrolyzed derivatives have shown preclinical efficacy activity against wild-type and lamivudine-resistant hepatitis B virus. The effective concentration of alamifovir required to reduce replication by 50% (EC50) for the wild-type was 0.027 uM, which is approximately 20 times less than lamivudine, and the EC50 for the lamivudine-resistant mutants was 2.6 to 3.3 uM. The mechanism of action of alamifovir appears to be via the inhibition of the protein priming reaction and the packaging reaction, thereby decreasing HBV replication. Alamifovir`s development has been discontinued.
Status:
Investigational
Source:
USAN:Actinoquinol Sodium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Actinoquinol is sunscreen agent that absorbs Ultraviolet B light. Actinoquinol in combination with hyaluronic acid drops might be helpful for the human eye in the defense against photooxidative and other oxidative processes.
Status:
Investigational
Source:
NCT00671580: Phase 2 Interventional Completed Skin Infections
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Razupenem (also known as PZ-601 or PTZ601) is an anti-MRSA carbapenem antibiotic. It is active against Enterobacteriaceae and Gram-positive bacteria including methicillin-resistant staphylococci and enterococci, and was investigated as potential alternative drug (replacing common antibiotics) against resistant bacteria. In healthy male volunteers, razupenem did not cause serious adverse events. The potential effect and safety of razupenem has been evaluated in a phase II clinical trial studying skin infection.
Status:
Investigational
Source:
INN:tibeglisene
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tibeglisene (also known as BM 13907) is a pentynoic acid derivative patented by Boehringer Mannheim G.m.b.H. as insulin sensitizer with hypoglycemic activity. Tibeglisene is also able to reduce serum triglyceride and cholesterol concentrations. Tibeglisene exerts favor influences on glucose-transport activity.
Status:
Investigational
Source:
NCT03694249: Phase 2 Interventional Active, not recruiting Malignant Solid Tumor
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ifetroban was developed as a thromboxane A2/prostaglandin H2 receptor antagonist by Bristol-Myers Squibb for cardiovascular indications. In spite of the positive preclinical results where the drug has shown the cardioprotective and antithrombotic activities and was effective. The development of this drug for coronary thrombosis, peripheral vascular disorders, and thrombosis was discontinued. Bristol-Myers Squibb donated the entire program to Vanderbilt University, which further identified ifetroban’s potential in treating patients for several niche indications. Cumberland acquired the ifetroban program from Vanderbilt through its majority-owned subsidiary, Cumberland Emerging Technologies taking responsibility for development and commercialization of the product. Ifetroban oral capsule is being developed by Cumberland for the treatment of systemic sclerosis (SSc) also called scleroderma. With pulmonary disease emerging as the major cause of death in SSc patients, preclinical work indicates that ifetroban is capable of preventing cardiac fibrosis in a model of pulmonary arterial hypertension. In addition, this drug successfully completed phase II clinical trials for the treatment of hepatorenal syndrome (HRS) in hospitalized adult patients, where were determined the safety and pharmacokinetics of 3 days of intravenous ifetroban. In addition, the recruitment is anticipated for Phase 2 study of daily, oral anti-fibrotic therapy to prevent heart muscle disease and improve heart muscle function in ambulatory and non-ambulatory Duchenne patients. In December 2018, Vanderbilt-Ingram Cancer Center and Cumberland Pharmaceuticals initiated a phase II trial to assess the safety and feasibility of ifetroban in treating patients with malignant solid tumors that are at high risk of coming back after treatment and spreading throughout the body.
Status:
Investigational
Source:
INN:lidadronic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lidadronic acid is the calcium metabolism regulator.
Status:
Investigational
Source:
NCT03658096: Not Applicable Interventional Enrolling by invitation Distal Radioulnar Joint Sprain
(2017)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Quiflapon Sodium (MK-0591; (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)- indol-2-yl]-2,2-dimethyl propanoic acid, previously L-686,708) had been in phase II clinical studies for the treatment of inflammatory bowel disease, but the study was discontinued later, because in spite of MK-591 markedly inhibited Leukotrienes (LT) biosynthesis, it did not differ significantly from placebo in clinical efficacy. Also was discovered, that MK-0591 may modify the airway changes associated with bronchial hyper responsiveness, as well as offer symptomatic relief in asthma. MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay. In additional, recently was discovered, that MK591 possesses all major attributes of a standard anti-metastatic agent with significant cancer-selective effect, and suggest that MK591 may turn out to be an effective agent for therapy of castration-resistant, bone-metastatic prostate cancer. Though details of the molecular underpinnings of the anti-metastatic action of MK591 are unknown at this time, this finding gives an opportunity for further exploration to better understand the signaling mechanisms involved by in vitro and in vivo experiments.
Pemaglitazar was developed as a dual peroxisome proliferator-activated receptors alpha and gamma (PPAR- α,γ) agonist. Information about the further development of this drug is not available.

Showing 1271 - 1280 of 34955 results