Factor xa based anticoagulant compositions

Details Factor xa based anticoagulant compositions Factor xa based anticoagulant compositions

A - Human Necessities

61

K

A61K 38/48 (2006.01) A61K 38/36 (2006.01) A61K 47/48 (2006.01) A61K 51/08 (2006.01) C07K 16/40 (2006.01)

Patent

CA 2060507

An anticoagulant composition containing an effective amount of factor Xa having the active serine site inactivated that functions rapidly and effectively in vivo to suppress coagulation. In a preferred embodiment Factor Xa, a serine esterase that forms a complex vith Factor Va, Ca + +, and phospholipid to catalyze prothrombin activation, is first inactivated with an active site inhibitor, such as dansyl-glu-gly-arg-chloromethyl ketone, to form inactivated factor Xa. In another embodiment, Factor Xa is expressed from a gene sequence wherein the portion encoding the active serine region is modified. The inactivated protein re- tains the ability to bind to endogenous factot Va in vivo, and has a half-life of approximately ten hours. Administration of inac- tive factor Xa to the blood of a patient without in the formation of inactive factor Xa-Va complexes in vivo, thereby inhibiting coagulation.

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