Thrombin inhibitors A new generation of antithrombotics

作者: S STONE

DOI: 10.1016/1050-1738(95)00049-F

关键词: AntithromboticHirudinMedicineHeparinUnstable anginaDiscovery and development of direct thrombin inhibitorsThrombinThrombusFibrinPharmacology

摘要: Abstract The activity of thrombin is central to the processes fibrin generation and platelet aggregation, which are inherent in thrombus formation. As a result x-ray crystallographic studies over last 5 years, we now have firm knowledge structural basis for specific interactions with components coagulation system. Moreover, crystal structures will assist development inhibitors desired pharmacological properties, such as oral availability. Several already clinical trials antithrombotic agents and, although only small been completed date, preliminary results encouraging. Hirudin Hirulog ™ appear offer advantages heparin, current mainstay therapy, several indications including unstable angina, thrombolytic coronary angioplasty.

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