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Drug intelligence / Profile preview
dabigatran etexilate
- Development stage
- Approved
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dabigatran etexilate (BIBR 1048) is an orally active small molecule prodrug developed by Boehringer Ingelheim. Upon oral administration, it is rapidly converted by esterases in the body to its active form, dabigatran (BIBR 953 ZW). Dabigatran is a potent, nonpeptidic direct thrombin inhibitor that specifically and reversibly binds to the active site of both free and clot-bound thrombin (coagulation factor IIa), thereby preventing the conversion of fibrinogen to fibrin and inhibiting thrombin-induced platelet aggregation. The drug was approved by the FDA in 2010 under the brand name Pradaxa. It is indicated for the prevention and treatment of venous thromboembolism (VTE), including deep vein thrombosis (DVT) and pulmonary embolism (PE), as well as for the prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation.
- Brand names
- DabigoPradaxPradaxaPradaxarPrazaxa
- Other names
- dabigatrandabigatran etexilate mesilatedabigatran etexilate mesylatedabigatran etexilate methanesulfonate
02
Targets
F2 (Thrombin)
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