Developed in Japan, argatroban was the first licensed synthetic direct thrombin inhibitor, originally developed by Mitsubishi Pharma Corporation (MPC) as an anticoagulant. Argatroban was licensed out to Encysive Pharmaceuticals Inc., which evaluated argatroban as an anticoagulant for use in Heparin-Induced-Thrombocytopenia type II (HIT type II) in trials carried out in the USA. Argatroban was approved for this condition in the USA in 2000 and sub-licensed to GlaxoSmithKline (GSK) for marketing in the USA and Canada.

Recently approved in some European countries, argatroban is marketed for anticoagulation in adult patients with heparin-induced thrombocytopenia type II (HIT type II) who require parenteral antithrombotic therapy. Argatroban is given as a continuous intravenous infusion.

Argatroban acts by selectively and reversibly binding to the active site of thrombin and inhibits thrombin induced or catalyzed associated reactions. Thrombin is a key enzyme in the regulation of coagulation and in the generation of thrombus or blood clots.

Evidence for the efficacy of argatroban was obtained from the results of two clinical trials including over 500 patients.