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

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Showing 171 - 180 of 6154 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:glysobuzole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Glysobuzole (stabinol) is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glysobuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.
Status:
Investigational
Source:
INN:mivobulin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity
Status:
Investigational
Source:
NCT04669587: Phase 1/Phase 2 Interventional Recruiting Estrogen Receptor-Positive
(2021)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

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

Class (Stereo):
CHEMICAL (RACEMIC)

Clorisamine is an antihistamine drug developed by Schering in the 1970s. The drug was evaluated in phase 1 clinical trial on healthy volunteers. The results show that in a therapeutic dose of 2 mg the drug did not have any effects which might lead to an impairment of driving ability.
Status:
Investigational
Source:
INN:ketimipramine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

KETIPRAMINE, an imipramine derivative, is a tricyclic antidepressant. In clinical trials, it was found to be as effective as imipramine for the depression treatment, with fewer secondary effects.
Ertiprotafib was originally developed as an inhibitor of PTP1B. Multiple targets of ertiprotafib, in addition to PTP1B inhibition, have been suggested including dual PPARalpha/PPARgamma agonism and IKK-beta inhibition. It normalized the plasma glucose and insulin levels in diabetic animal models and progressed to a phase II clinical trial for the treatment of Type 2 diabetes mellitus. Ertiprotafib development has been discontinued.
Status:
Investigational
Source:
INN:vabametkib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cositecan (BNP1350) is semi-synthetic silicon-containing camptothecin and an inhibitor of topoisomerase I. It was engineered by BioNumerik Pharmaceuticals for superior oral bioavailability, lactone stability, and insensitivity to Pgp/MRP/LRP drug resistance. The compound shows a broad spectrum of activity in experimental human tumors. Cositecan was investigated in clinical trials in patients with malignant melanoma, relapsed or refractory non-small cell lung cancer, ovarian and peritoneal cancer, malignant glioma. The compound had little activity in recurrent glioma and ovarian cancer.
Status:
Investigational
Source:
INN:implitapide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions in apolipoprotein E knockout mice fed a Western-type diet.