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 Trifluoroacetic Acid Salt is a major metabolite of Dabigatran (D100090) in humans. Four isomeric acylglucuronides of Dabigatran were isolated and purified from urine of dosed rhesus monkeys. NMR analysis confirmed the structures of the four metabolites as the 1-O-acylglucuronide (β anomer) and the 2-O-, 3-O-, and 4-O-acylglucuronides (α and β anomers).
A metabolite of Dabigatran.
The major metabolite of Dabigatran (D100090) in humans. Four isomeric acylglucuronides of Dabigatran were isolated and purified from urine of dosed rhesus monkeys. ?NMR analysis confirmed the structures of the four metabolites as the 1-O-acylglucuronide (β anomer) and the 2-O-, 3-O-, and 4-O-acylglucuronides (α and β anomers).
