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

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Showing 521 - 530 of 4342 results

Status:
Investigational
Source:
INN:cethromycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cethromycin is a ketolide antibiotic derived from erythromycin A being investigated for use in community-acquired pneumonia and other respiratory tract infections. Cethromycin possesses reliable activity against the bacteria most commonly associated with community-acquired pneumonia including S. pneumoniae, H. influenzae, M. catarrhalis, M. pneumoniae, C. pneumoniae, and L. pneumophila. Unlike fluoroquinolones, cethromycin has a narrower spectrum of activity against gram-negative bacteria, which may reduce the risk of collateral damage and the incidence of Clostridium difficile infection. It offers an advantage over telithromycin in that hepatotoxicity does not seem to be a concern. The FDA denied approval of cethromycin for the treatment of CAP in 2009, requesting more efficacy data.
MKC-1 is an orally available cell cycle inhibitor with downstream targets that include tubulin and the importin-β family. MKC-1 has shown broad antitumor activity in preclinical models. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. MKC-1 had been in phase II clinical trials for the treatment of ovarian cancer, endometrial cancer, pancreatic cancer and breast cancer. This compound was originally discovered by Roche, then licensed to EntreMed (now CASI Pharmaceuticals) the exclusive worldwide rights to develop and commercialize. However, no recent development has been reported.
Status:
Investigational
Source:
INN:terciprazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Terciprazine was developed as an antihypertensive agent that has never been marketed. Information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:dezinamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dezinamide is a potential antiepileptic drug that binds to the voltage-sensitive sodium channel. It is a metabolite of fluzinamide. It was active in preventing maximal seizures induced in mice or rats by electroshock and threshold seizures induced in mice by metrazol, bicuculline, and picrotoxin. It was predominantly active against tonic-clonic seizures. Adverse experiences included headache, ataxia, blurred vision, diplopia, dizziness, lightheadedness, and mild confusion. Dezinamide development was discontinued because of toxicity problems not observed with the metabolite.
Status:
Investigational
Source:
INN:fluprostenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:flosatidil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Status:
Investigational
Source:
INN:fluperamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluperamide was developed as an antiperistaltic agent for the treatment of diarrhea. However, information about the current use of the drug is not available.
Status:
Investigational
Source:
NCT00033384: Phase 2 Interventional Completed Breast Cancer
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



CI 1040 is an inhibitor of the mitogen-activated protein (MAP) kinase signal transduction pathway and has been shown to specifically inhibit MAP kinase kinase (MEK). CI 1040 was being developed by Parke-Davis (formerly a division of WarnerLambert, Now Pfizer) as an anticancer agent. It was the initial MEK inhibitor to undergo clinical evaluation based on promising preclinical activity. However, its development has been discontinued.
Status:
Investigational
Source:
INN:texacromil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Texacromil is a benzopyran derivative patented by C. M. Industries S. A. as passive cutaneous anaphylaxis inhibitor
Lomeguatrib is a O6-methylguanine-DNA-methyl-transferase inhibitor which was developed by AstraZeneca for the treatment of cancer. It was tested in phase I and II of clinical trials for the treatment of colorectal cancer, melanoma and other solid tumors.