Discovery of ximelagatran in an historical perspective.
The oral direct thrombin inhibitor ximelagatran is the first oral anticoagulant since the introduction of the vitamin K antagonists in the early 1940s. A comparison of the discovery and early clinical development of the two classes of oral anticoagulants reveals some similarities but also several differences that illustrate the change in drug discovery over the last half century.
Gustafsson
David
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Department of Cardiovascular Pharmacology, AstraZeneca R&D, Mölndal, Sweden.
D000818:Animals; D000925:Anticoagulants / Q000266:history* / Q000494:pharmacology; D001384:Azetidines / Q000266:history* / Q000494:pharmacology; D001596:Benzylamines; D001777:Blood Coagulation / Q000187:drug effects*; D002417:Cattle; D002986:Clinical Trials as Topic; D015195:Drug Design; D006470:Hemorrhage / Q000139:chemically induced; D049673:History, 20th Century; D006801:Humans; D029903:Melilotus / Q000009:adverse effects; D013917:Thrombin / Q000037:antagonists & inhibitors; D014812:Vitamin K / Q000037:antagonists & inhibitors; D014859:Warfarin / Q000494:pharmacology
D000925:Anticoagulants; D001384:Azetidines; D001596:Benzylamines; D014812:Vitamin K; C426686:ximelagatran; D014859:Warfarin; D013917:Thrombin