Argatroban is a reversible inhibitor of thrombin (IC50s = 0.01 and 0.09 ?M for the free and clot-bound forms, respectively).1 It is selective for thrombin over factor Xa, trypsin, plasmin, and tissue plasminogen activator (Kis = 0.0045, 53, 0.19, 25.7, and 87.7 ?M, respectively). It inhibits thrombin-induced platelet aggregation in washed isolated guinea pig platelets with an IC50 value of 0.077 ?M.2 Argatroban (3.2 mg/kg, s.c.) decreases thrombus formation in a guinea pig model of iron chloride-induced arterial thrombosis. Formulations containing argatroban have been used in the prevention or treatment of thrombosis in patients with heparin-induced thrombocytopenia.
1.Park, H.D., Lee, S.H., Kim, T.H., et al.Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrugBioorg. Med. Chem. Lett.23(17)4779-4784(2013) 2.Kato, Y., Kita, Y., Hirasawa-Taniyama, Y., et al.Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pigEur. J. Pharmacol.473(2-3)163-169(2003)