New anticoagulants for venous thromboembolic disease.

Venous thromboembolic disease, including deep vein thrombosis and pulmonary embolism, is a cause of significant mortality and morbidity. In the US, approximately 260000 cases are diagnosed annually. Current drugs for the prevention and treatment of venous thromboembolism (VTE) include heparin, low-molecular-weight heparins and warfarin. Since they possess several disadvantages, researchers are investigating improved anticoagulants. To understand how any promising anticoagulant would work, a review of the pathophysiology and regulation of the coagulation cascade is provided. The more prominent drugs reviewed include tissue factor pathway inhibitor protein, nematode anticoagulant protein, Factor IX inhibitors, anti-Factor Xa inhibitors (DX-9065a (Daiichi Seiyaku Co Ltd), YM-60828 (Yamanouchi Pharmaceutical Co Ltd), fondaparinux, idraparinux (Sanofi-Synthelabo/NV Organon)), selective thrombin inhibitors (oral heparin, ximelagatran (AstraZeneca plc)) and enhancers of natural anticoagulants (activated protein C, ART-123 (Asahi Kasei Pharma Corp)).

Hematological studies on naturally occurring substances. VI. Effects of an animal crude drug "chan su" (bufonis venenum) on blood coagulation, platelet aggregation, fibrinolysis system and cytotoxicity.

During the screening test of the animal crude drug "Chan su" (Chinese name, toad-cake), the venom of Bufo bufo gargorizans CANTOR (Bufonidae), on blood coagulation, platelet aggregation, fibrinolysis system and cytotoxicity, the ethyl acetate extract showed promotive action on platelet aggregation and remarkable cytotoxic activity on HeLa-S3 cells. Nine kinds of bufadienolides were isolated from the ethyl acetate extract by bioactivity-guided fractionation and were identified by chemical and spectral analysis.