dabigatran etexilate mesylate polymorph II

BIBR 1048 MS polymorph II is a specific crystalline polymorph (Polymorph II) of dabigatran etexilate mesylate, an oral prodrug of the direct thrombin inhibitor dabigatran (BIBR 953 ZW). Developed by Boehringer Ingelheim, dabigatran etexilate is rapidly converted in vivo by esterases to its active form, which binds to and inhibits both free and clot-bound thrombin, preventing thrombus formation. While the polymorph I form of dabigatran etexilate mesylate was ultimately selected for the commercialized product (Pradaxa) due to superior crystallization and processing properties, Polymorph II was evaluated in early clinical development. Specifically, Boehringer Ingelheim completed a Phase 1 randomized crossover trial in 2004 comparing the bioavailability of 150 mg HPMC capsules of Polymorph II versus Polymorph I in healthy subjects.

Other names

dabigatran etexilate polymorph II