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

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Showing 541 - 550 of 10251 results

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 Unknown status 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:ethylmethylthiambutene [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ethylmethylthiambutene is a potent analgesic compatible with morphine. It possesses addiction liability similar to that of morphine.
Status:
Investigational
Source:
NCT03867253: Phase 2 Interventional Completed Mild to Moderate Alzheimer's Disease
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04575038: Phase 2 Interventional Completed COVID-19 Infection
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Brequinar is a synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. Brequinar had been in phase II clinical trials by Bristol-Myers Squibb for the treatment of cancer and transplant rejection. However, this research has been discontinued. Brequinar had been also in preclinical studys for the treatment of cytomegalovirus infections. However, this research has been discontinued.
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:relcovaptan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Relcovaptan is a potent, orally active nonpeptide vasopressin V1a antagonist that was undergoing clinical development with Sanofi-Synthélabo (formerly Sanofi) in France. SR49059 is specifically and selectively antagonizes the effect of vasopressin on the V1a receptor in animals’ and in humans. The drug has been shown to have an excellent safety profile in single and repeated dose toxicological studies in animals. In the human uterus in vitro, SR49059 caused a dose-dependent inhibition of vasopressin V1a receptor-mediated activity of myometrial strips and isolated uterine arteries. In vivo in nonpregnant women, an inhibition of vasopressin-induced uterine activity has been observed.