Drug intelligence / Profile preview

dazmegrel

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Dazmegrel is a **small molecule** drug that selectively inhibits **thromboxane-A synthase** (also called thromboxane synthetase), the enzyme responsible for converting prostaglandin H2 to thromboxane A2, a potent promoter of platelet aggregation and vasoconstriction[1][3][4][7]. By inhibiting this enzyme, dazmegrel prevents the formation of thromboxane A2, thereby reducing platelet aggregation and exerting an antithrombotic effect. Developed in the 1980s for cardiovascular and anti-thrombotic indications, particularly in the context of stroke and other thrombotic disorders, it was studied both as a monotherapy and in combination with aspirin[4]. Dazmegrel is an imidazole derivative and has been used in several preclinical and clinical studies, but there is no evidence that it progressed to regulatory approval.

Other names
dazmegrelDazmegrelum3-(Imidazol-1-ylmethyl)-2-methylindole-1-propionic acid3-[3-(imidazol-1-ylmethyl)-2-methylindol-1-yl]propanoic acid3-(1H-imidazole-1-yl-methyl)-2-methyl-1H-indole-1-propanoic acid
02

Targets

TBXAS1 (Thromboxane A2 synthase)

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