Patients with non-valvular atrial fibrillation or venous thromboembolism typically require anticoagulation prophylaxis/treatment. Direct oral anticoagulants (DOACs) offer certain advantages over warfarin and heparins, but there remains a significant unmet need for anticoagulant agents with better risk-benefit profiles than currently available treatments. We have identified a new class of highly potent and selective direct thrombin inhibitors (VE-DTIs) with a unique mode of action. VE-DTIs prevent clot formation with efficacy similar to that of the DOACs in in vivo rodent models of arteriovenous shunt and tissue-factor venous stasis thrombosis. In addition to their strong anticoagulation properties, the VE-DTIs demonstrate significantly lower bleeding in several rodent bleeding models compared to the DOACs. In this poster we will present in vitro and in vivo ADMET and efficacy results for a series of promising lead compounds.

Novel, highly selective direct thrombin inhibitors: In vivo studies demonstrate efficacy with lower bleeding risk

253rd National Meeting (2017)

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