Thursday, December 19, 2013
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Factor Xa; thrombin
(factor IIa; F2)
In vitro and rat studies identified a dual factor Xa and
thrombin inhibitor that could help treat thrombosis. In vitro, the
blocked both factor Xa and thrombin with low nanomolar potency. In a rat
model of venous thrombosis, i.v. and oral dosing of SAR107375 had
antithrombotic activity. In a rat model of arterial thrombosis, oral dosing
of SAR107375 decreased bleeding compared with oral dosing of the factor Xa
or the thrombin inhibitor Pradaxa
and had comparable antithrombotic activity. Next steps include further
assessing advantages of SAR107375 such as reduced bleeding risks relative to
Ingelheim GmbH markets the thrombin inhibitor Pradaxa to
AG and Johnson
& Johnson market Xarelto to treat deep vein thrombosis
(DVT), fibrillation, pulmonary embolism (PE), stroke and VTE.
Published online Dec. 19, 2013
Patent application filed
covering inhibitor; licensed to an undisclosed Chinese company
Meneyrol, J. et al. J.
Med. Chem.; published online Oct. 31, 2013;
Contact: Gilbert Lassalle, Sanofi R&D, Toulouse, France
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