Dabigatran
Etexilate mesylate (BIBR-1048; BIBR 1048MS) is the prodrug of dabigatran which is a potent
and nonpeptidic small molecule anti-thrombotic agent that specifically and reversibly inhibits
both free and clot-bound thrombin by binding to the active site of the
thrombin molecule. Dabigatran (also known as IBR 953) is a potent
nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free
assay. Dabigatran is designed to be converted into an orally active
prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor
oral absorption. Dabigatran inhibits thrombin in a competitive fashion. Dabigatran is used to prevent stroke and harmful blood clots if you have a certain type of irregular heartbeat. Dabigatran is also used to treat blood clots in the veins of your legs or lungs and to reduce the risk of them occurring again. This medication may also be used to prevent these blood clots from forming after hip replacement surgery.