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

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Showing 171 - 180 of 1126 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

IRDABISANT is a histamine H3 receptor inverse agonist with potential therapeutic utility in cognition enhancement.
Status:
Investigational
Source:
INN:lancovutide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LANCOVUTIDE, also known as duramycin, is a 19-amino-acid tetracyclic peptide antibiotic. It is in clinical development for the treatment of cystic fibrosis (CF). It activates an alternative chloride channel in lung epithelial cells by elevating intracellular calcium levels, and may potentially compensate for CF transmembrane conductance regulator deficiency in the airway epithelium and increase the volume of the airway surface liquid.
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.
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.
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.
Status:
Investigational
Source:
INN:dotarizine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dotarizine was developed as antimigraineur. Dotarizine inhibited the 5-HT2A response in a concentration-dependent manner. The mechanism of blockade by dotarizine of cerebral vessels contractility has three components: (i) presynaptic inhibition of noradrenaline release; (ii) blockade of postsynaptic vascular 5-HT receptors; (iii) blockade of Ca(2+)entry into the vascular smooth muscle cell cytosol. The compound does not affect the vascular receptors for noradrenaline, angiotensin II or prostaglandin F(2alpha). Dotarizine had a pronounced protective effect against electric seizures.
Status:
Investigational
Source:
INN:elacridar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Elacridar is an oral bioenhancer that targets multiple drug resistance in tumors. Elacridar is a strong and relatively specific inhibitor of P-gp and BCRP, two main efflux transporters. Development of elacridar is assumed to have been discontinued.
Status:
Investigational
Source:
INN:lecozotan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LECOZOTAN, a benzodioxanylpiperazine derivative, is a selective serotonin 1A receptor antagonist. It was in development for the symptomatic treatment of cognitive deficits in Alzheimer's disease.
Status:
Investigational
Source:
INN:cadazolid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cadazolid is a new antibiotic in development for the treatment of Clostridium difficile-associated diarrhea. Cadazolid is active against all (including linezolid- and moxifloxacin-resistant) Clostridium difficile strains. In phase I and II clinical trials, cadazolid was shown to be safe, well tolerated, and efficacious positioning itself as a potential future viable therapeutic option for CDI. Using a series of macromolecular labeling, in vitro transcription/translation, and topoisomerase studies, it was determined that protein synthesis inhibition via the oxazolidinone moiety is the primary mechanism of action of cadazolid. Cadazolid is in phase III clinical trials by Actelion Pharmaceuticals for the treatment of Clostridium difficile infection. The US FDA has designated cadazolid as both a Qualified Infectious Disease Product (QIDP) and a Fast Track development program for this indication.
Status:
Investigational
Source:
NCT01931241: Phase 1 Interventional Unknown status Hypercholesterolemia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Hyodeoxycholic acid, also known as HDCA, is a secondary bile acid. Natural 6alpha-hydroxylated bile acids are receptor-specific activators of nuclear liver X receptor alpha (LXRalpha), a nuclear receptor regulating the expression of the cholesterol 7alpha-hydroxylase gene. AHRO-001 (Hyodeoxycholic acid) is in phase I clinical trials for the treatment of atherosclerosis. Through a complex signaling processes utilizing LXR receptors, the compound is designed to increase the efficiency of cholesterol efflux using the HDL cells, which act on all cholesterol in the arterial circulation as well as in the lipid core of plaque deposits in the artery walls. Use of AHRO-001 has shown no adverse effects on morbidity, mortality or toxicity and has been well tolerated at high doses.