Drug intelligence / Profile preview

dabigatran etexilate mesylate polymorph I

Development stage
Approved
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

BIBR 1048 MS Polymorph I is a specific crystalline polymorph (Polymorph I) of dabigatran etexilate mesylate, an orally active small molecule prodrug developed by Boehringer Ingelheim. Upon oral administration, dabigatran etexilate mesylate is rapidly converted by esterase-catalyzed hydrolysis to its active form, dabigatran (BIBR 953 ZW), which acts as a direct and selective thrombin inhibitor. By binding to both free and clot-bound thrombin, dabigatran prevents the conversion of fibrinogen to fibrin, thereby inhibiting coagulation and thrombus formation. BIBR 1048 MS Polymorph I is the primary crystalline form used in the commercial formulation of Pradaxa, which is indicated for the prevention and treatment of thromboembolic conditions, including deep vein thrombosis (DVT), venous thromboembolism (VTE), and stroke or systemic embolism in patients with non-valvular atrial fibrillation.

Brand names
PradaxaRendix
Other names
dabigatran etexilate mesilate polymorph Idabigatran etexilate mesylate polymorph Idabigatran etexilate polymorph Idabigatran polymorph I
02

Targets

APC (Activated protein C)F2 (Thrombin)F10 (Factor Xa)PLG (Plasminogen)PLAT (Tissue-type plasminogen activator)PRSS1 (Trypsin family)

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