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

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Showing 31 - 40 of 502 results

Status:
Investigational
Source:
NCT02783989: Not Applicable Interventional Completed Cardiovascular Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.
Status:
Investigational
Source:
INN:carsatrin [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carsatrin (also known as RWJ 24517) is purinylpiperazine derivative patented by Ortho Pharmaceutical Corp. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+,K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin
Status:
Investigational
Source:
INN:lanraplenib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:deloxolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Deloxolone was devoid of aldosterone-like properties. Deloxolone could be of therapeutic value in peptic ulcer diseases without inducing fluid retention, hypertension and hypokaliemia. Carbenoxolone and deloxolone were orally administered to healthy volunteers in a cross-over double-blind trial. Both the concentration in gastric juice and the output of PGE2, determined by an RIA method in basal conditions and after pentagastrin bolus, increased in drug-treated compared to vehicle-treated subjects thus supporting the hypothesis that cytoprotection might be due to gastric PGE, levels. Moreover, deloxolone induced less marked effects than carbenoxolone on body weight, hematocrit, plasma potassium and proteins, confirming that deloxolone is less similar to aldosterone than the reference drug.
Status:
Investigational
Source:
INN:emilumenib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:saredutant
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.
Status:
Investigational
Source:
INN:venglustat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ibiglustat (GZ/SAR402671 or Genz-682452) is a small molecule inhibitor of glucosylceramide synthase. Ibiglustat has been demonstrated to effectively lower glycosphingolipid synthesis. Genzyme, a Sanofi Company is developing Ibiglustat for the treatment of Parkinson's Disease, Gaucher Disease, and Fabry Disease.
Status:
Investigational
Source:
INN:fidrisertib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01241422: Phase 2 Interventional Completed Asthma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)