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

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Showing 901 - 910 of 13268 results

Status:
Investigational
Source:
NCT00987337: Phase 2 Interventional Completed Hepatitis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Filibuvir (PF-868554), being developed by Pfizer, is an orally administered, non-nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase for the potential treatment of chronic hepatitis C (HCV) infection. Filibuvir is a potent and specific inhibitor of the virally encoded NS5B polymerase, and inhibited genotype 1 sub genomic HCV replication in the cell-based replicon system. In phase I and a IIa clinical trial in treatment-naïve patients infected with genotype 1 HCV, filibuvir monotherapy or in combination with pegylated IFNα2a/ribavirin (the standard of care [SoC] for HCV infection) for up to 4 weeks significantly reduced HCV RNA levels compared with placebo or SoC alone. However, company stopped development of the drug and the decision to halt development of the non-nucleoside polymerase inhibitor, which was in mid-stage testing, was not related to any safety issues.
Status:
Investigational
Source:
INN:teloxantrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Teloxantrone (also known as DuP 937) was developed as an anthrapyrazole intercalator that inhibits DNA synthesis. Teloxantrone interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis. The drug participated in phase II clinical trials in colorectal carcinoma, in non-small cell lung cancer, in metastatic malignant melanoma. However, these studied apparently were discontinued.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.
Status:
Investigational
Source:
INN:ioseric acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ioseric Acid is triiodoisophthalamic acid derivative patented by Schering A.-G. as x-ray contrast media
Status:
Investigational
Source:
INN:ontazolast
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ontazolast (also known as BIRM 270) inhibits arachidonate release that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils. This drug was studied for the treatment of asthma. In addition, was shown that ontazolast possessed potent class-III antiarrhythmic properties and induces prolongation of QTc in a dose-dependent fashion.
Status:
Investigational
Source:
INN:cinnamaverine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cinnamaverine is an aminodiphenylacrylate, a smooth muscle relaxant and antispasmodic with some local anesthetic activity.
Status:
Investigational
Source:
INN:difebarbamate
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Difebarbamate is a barbituric acid derivative. It is a hypnotic drug. Difebarbamate is a component of Tetrabamate complex, which was introduced for clinical use in the treatment of alcoholism and various types of drug dependence. After oral administration of difebarbamate, the compound was completely metabolized and three metabolic pathways were observed: oxidation of Cl of the n-butyl chain which leads to the oxygen dealkylation; hydrolysis of the carbamoyloxy group; oxidation of the benzene ring in position 4. Tetrabamate can induce hepatotoxicity, probably due to an idiosyncratic metabolic mechanism. Despite restrictions on its indications and treatment duration introduced in 1997, cases of severe liver damage have continued to be notified in France.
Status:
Investigational
Source:
INN:diclofurime [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diclofurime is a powerful coronary vasodilator, which lowers the resistance of large coronary arteries and decreases the O2 consumption of the myocardium. The activity of diclofurime is similar to digitalis: increase of cardiac flow, bradycardia, redistribution of the blood to peripheral area. These properties demonstrated in dogs have been confirmed in patients with cardiac diseases. Diclofurime is the antianginal agent. It might be effective in the control of cardiac arrhythmias since it exhibited both local anesthetic-like and calcium antagonistic properties. Diclofurime appears to be one of the most active and best tolerated drugs for long-term oral treatment of arterial hypertension.
Status:
Investigational
Source:
INN:quintiofos
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Quintiofos is phosphonothioic ester derivative patented by Farbenfabriken Bayer A.-G. as insecticide and ascaricide, particularly against parasites of the larger animals.
Status:
Investigational
Source:
INN:tameridone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tameridone is a neurotransmitter antagonist was developed as a psychotropic agent for use in veterinary. Information about the current use of this drug is not available.