BIBR 953 is a potent, reversible, and direct inhibitor of thrombin with IC50 value of 9.3nM [1].

BIBR 953 shows a favorable selectivity profile and strong activity in vitro with a Ki value of 4.5nM. It also exhibits the best activity profile in vivo following administration to rats. BIBR 953 is designed to be converted into an orally active prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor oral absorption. BIBR 953 inhibits thrombin in a competitive fashion. This inhibition is rapid and reversible. BIBR 953 inhibits both clot-bound and free thrombin. BIBR 953 is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo. Since thrombin can affect cell behavior and response in various tissue types via PAR signaling, BIBR 953 is found to be beneficial in many diseases including inflammation, infection, fibrosis and cancer. Clinical trials show that BIBR 953 is a highly effective anticoagulant with a good safety profile [1, 2].

References:

[1] Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.

[2] van Ryn J, Goss A, Hauel N, Wienen W, Priepke H, Nar H, Clemens A. The discovery of dabigatran etexilate. Front Pharmacol. 2013 Feb 12;4:12.

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