dabigatran acyl-b-d-glucuronide

Dabigatran acyl-β-D-glucuronide is a major active metabolite of the thrombin inhibitor dabigatran . The prodrug of dabigatran, dabigatran etexilate , is hydrolyzed by plasma esterases to form dabigatran, which is metabolized primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT2B15 to form dabigatran acyl-β-D-glucuronide. Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma equipotently to dabigatran.

Dabigatran acyl-β-D-glucuronide, an active metabolite of the thrombin inhibitor dabigatran, is synthesized predominantly through the action of the UDP-glucuronosyltransferase isoform UGT2B15. This compound, at a concentration of 0.46 µM, effectively prolongs activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma.