Xemilofiban: SC 54684A, xemlofiban.
Xemilofiban [SC 54684, SC 54684A (HCl), xemlofiban], a glycoprotein IIb/IIIa antagonist, is an orally available prodrug of a non-peptide mimetic of the tetrapeptide RGDF. It is converted to the active metabolite, SC 54701 (the free base form of SC 54701A). Development was initiated by Searle (Monsanto). Searle became part of Pharmacia Corporation, which was acquired by, and merged into, Pfizer in April 2003. Searle had co-development and co-marketing agreements with Sankyo in Japan; these have been discontinued. In January 2003, Pharmacia donated the intellectual property for xemilofiban to Western Michigan University. In February 2003, Western Michigan University granted an exclusive worldwide licence of xemilofiban to VDDI Pharmaceuticals (formerly Virtual Drug Development Inc.). Xemilofiban was in a phase III clinical trial, the Evaluation of Xemilofiban in Controlling Thrombotic Events (EXCITE) trial, with Searle (Monsanto) in the US and Europe for the treatment of thrombosis in patients with unstable angina pectoris and acute myocardial infarction undergoing angioplasty. However, as xemilofiban demonstrated no significant clinical benefit, Searle discontinued its development. In Japan, Sankyo discontinued the development of xemilofiban for thrombosis at phase II following Searle's decision to drop the project. VDDI Pharmaceuticals plans to develop xemilofiban in cardiovascular disorders following on from the phase III studies completed by Pharmacia; a restructured dosing schedule and narrowed patient selection will be used. VDDI has research facilities worldwide and will utilise facilities in Ireland for the European clinical development programme; research facilities in the Southwest Michigan Innovation Center are planned while the head office of VDDI is based in Tennessee. Xemilofiban is in phase III development for the treatment of cardiovascular disease in conjunction with percutaneous coronary intervention.
D000787:Angina Pectoris / Q000188:drug therapy; D000818:Animals; D001550:Benzamidines / Q000494:pharmacology* / Q000627:therapeutic use; D002318:Cardiovascular Diseases / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D009203:Myocardial Infarction / Q000188:drug therapy; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors*; D011355:Prodrugs / Q000494:pharmacology* / Q000627:therapeutic use; D013927:Thrombosis / Q000188:drug therapy
D001550:Benzamidines; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D011355:Prodrugs; C091295:xemilofiban