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

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Showing 2431 - 2440 of 42705 results

Status:
Investigational
Source:
NCT00736372: Phase 1 Interventional Completed Metastatic Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



DB05448 (PX-12, 1-methyl propyl 2-imidazolyl disulfide) is a small molecule irreversible inhibitor of the redox protein thioredoxin, which has been associated with cancer and tumor growth. DB05448 stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, DB05448 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of DB05448 with increased patient survival.
Status:
Investigational
Source:
INN:tritiozine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Trithiozine is an alkoxythiobenzamide said to have antisecretory and tranquillising properties without anticholinergic, antihistaminic, or ganglion-blocking effects. Trithiozine in animal studies proved to have a marked anti-secretory and anti-ulcer effect, along with a very low acute and chronic toxicity. Clinical trials with trithiozine have been performed in some European countries. The results of these trials, most of which were conducted on a double-blind basis, and including already several hundreds of patients, have shown that oral trithiozine: exerts a very significant action on both basal and stimulated gastric acid secretion, without a rebound hypersecretion; promotes, in most patients, a complete endoscopic healing of peptic ulcer, in addition to an early symptomatic relief; has a mild sedative action; does not affect the pancreatic secretion; is well tolerated even for long-term (up to 10 months) treatments.
Azamulin [14-O-(5-(2-amino-1,3,4-triazolyl)thioacetyl)-dihydromutilin] is an azole derivative of the pleuromutilin class of antiinfectives. Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources). It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4. Azamulin exhibited remarkable antibacterial activity against all Gram-positive pathogens including MRSA, PRSP, and VRE, except for E. faecalis.
Status:
Investigational
Source:
J Drug Target. Jan 2009;17(1):36-63.: Phase 2 Human clinical trial Completed Cataract/complications/diagnosis/physiopathology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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:
NCT00165802: Phase 1 Interventional Completed Cancer, Malignant Tumors
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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:metescufylline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Metesculetol (permethol) is a vitamin P derivative. It increases capillary resistance and reduces membrane permeability. Permethol is for damaged gums and helps to stop gum bleeding, relieves inflammation and nourishes the gum tissues. It is used as a component of products for oral cavity care.
Status:
Investigational
Source:
INN:tetriprofen
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tetriprofen is a hydratropic acid derivative patented by Swiss chemical company CIBA Ltd as an antinociceptive and anti-inflammatory agent.
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

Showing 2431 - 2440 of 42705 results