Dabigatran etexilate

A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM; 10-fold less potent for Trypsin and no activity against Factor Xa, Plasmin, tPA and activated protein C; exhibits strong and long-lasting anticoagulant effects ex vivo and strong oral activity in different animal species.Thrombosis Approved (In Vitro) :Dabigatran etexilate (BIBR 1048; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively.Dabigatran etexilate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively.Dabigatran etexilate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey.