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

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Showing 181 - 190 of 477 results

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

Class (Stereo):
CHEMICAL (RACEMIC)

Rolgamidine is an antidiarrheal agent. No information on current use of this compound is available.
Status:
Investigational
Source:
NCT00206284: Phase 2 Interventional Completed GERD Without Erosive Esophagitis
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Linaprazan is a member of a new group of acid-suppressing agents, which unlike proton pump inhibitors, act through potassium-competitive inhibition of the H+,K+-ATPase located in the apical membrane of parietal cells. It displayed rapid inhibition of acid production and had a prolonged, dose-dependent duration of effect. Linaprazan reduced porcine renal Na(+),K(+)-ATPase activity by 9+/-2%, demonstrating a high selectivity for H(+),K(+)-ATPase. It provided similar efficacy to esomeprazole in terms of esophagitis healing and heartburn control.
Status:
Investigational
Source:
INN:lodazecar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lodazecar is a benzodiazepine derivative, which does not bind to the brain benzodiazepine receptor. The drug shares some similarity in tertiary structure with the cholesterol molecule. Oral administration of lodazecar in the cholesterol-fed rat is associated with significant changes in plasma lipoproteins and in key enzymes controlling hepatic cholesterol metabolism. In human the treatment reduced both the fractional and the absolute cholesterol absorption and increased fecal neutral sterol excretion by about 50%, serum plant sterol levels were reduced, most probably because of diminished sterol absorption. Biliary cholesterol secretion was unchanged.
Edaglitazone have a clear PPAR-gamma agonist profile, with predominant PPAR-gamma activity and little PPAR-alpha activity. Edaglitazone was reported to significantly improve insulin sensitivity and enhance the rate of glucose oxidation in both the presence and absence of insulin. Additional studies have shown that edaglitazone affects muscle glucose metabolism by additional mechanisms other than PPAR-gamma activation. Phase I clinical studies have revealed that edaglitazone is well-tolerated and capable of significantly improving glucose homeostasis. Edaglitazone had been in phase II clinical trials for the treatment if type 2 diabetes. However, this research has been discontinued.
Status:
Investigational
Source:
INN:glunicate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Glunicate (LG 13979) is a long-acting nicotinic acid derivative that can lower plasma triglyceride levels, while leaving other lipoprotein parameters unaffected. It exerts a dose‐dependent reduction of plasma triglycerides and cholesterol. In rabbits, glunicate provided dose-dependent protection of the arterial wall from atheromatous lesions and from cholesterol and collagen accumulation. It has been shown that glunicate has prolonged activity on plasma free fatty acids and triglycerides, with long lasting and intense activity on plasma cholesterol.
Status:
Investigational
Source:
INN:amiglumide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Amiglumide [CR 1795] is an amino acid derivative with cholecystokinin A antagonist activity. It has potential use for treating gastrointestinal disorders, pancreatitis and biliary dyskinesia. Amiglumide was developed in preclinical trials with Rottapharm in Italy.
Eflucimibe is a new and potent Acyl coenzyme A:cholesterol acyltransferases inhibitor. Eflucimibe effectively decreased plasma cholesterol in cholesterol-fed animals. In animal models, drug restores normolipodemia in endogenous hypercholesterolemic rabbits and prevents the progression of atherosclerosis by decreasing the number of macrophages in the foam cells. Eflucimibe has been in phase II clinical trials for the treatment of atherosclerosis and hyperlipidemia. However, this research has been discontinued.
Status:
Investigational
Source:
INN:mitratapide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mitratapide is a potent inhibitor of the microsomal triglyceride transfer protein used for the treatment of obesity in dogs. The drug was developed by Janssen Pharmaceutica and is chemically related to the antifungal drugs such as itraconazole which were also developed by Janssen. Administration of mitratapide to dogs results in reduced uptake of dietary lipids, dose dependent decreases in serum cholesterol and triglyceride and an increased presence of triglyceride containing droplets in enterocytes. Mitratapide also has a slight appetite decreasing effect that is claimed to be associated with its mode of action. Vomiting, diarrhoea or softened stools may occur during treatment. In most cases, these effects are mild and transient.
Status:
Investigational
Source:
INN:quisultazine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Quisultazine is a phenothiazine derivative patented by MARPHA Societe d'Etude et d'Exploitation de Marques as pentagastrin antagonist. In preclinical studies, Quisultazine weakly inhibited pentagastrin-stimulated gastric secretion but was a powerful inhibitor of nocturnal gastric secretion. Quisultazine possesses a very weak affinity to muscarinic receptors in vitro and in vivo. It has negligible anticholinergic properties in rats and mice at the peripheral level but no effect at the central level.
Status:
Investigational
Source:
NCT00267254: Phase 3 Interventional Completed Hyperlipidemia
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Torcetrapib is a CETP inhibitor which was developed by Pfizer for the treatment of diseases associated with elevated level of cholesterol. The drug was tested in phase III (in combination with atorvastatin) of clinical trials in coronary heart disease patients as well as in patients with hyperlipoproteinemia, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, however its development was terminated due to the high risk of death and heart problems.

Showing 181 - 190 of 477 results