Orally active prostacyclin-mimetic RS-93427: therapeutic potential in vascular occlusive disease associated with atherosclerosis.
RS-93427 is a potent, orally active prostacyclin-mimetic that is very rapidly absorbed but with generally long-lived actions in most species. It has antithrombotic, thrombolytic, and antivasospastic potential. Alone among several tested PGI-mimetics, it inhibits release of platelet mitogens more potently than its ability to inhibit aggregation. It also inhibits mitogen release from macrophages and vascular endothelial cells. RS-93427 is also potent at inhibiting macrophage accumulation of cholesteryl esters. These data suggest a broad spectrum of potential therapeutic utility for RS-93427 via the oral route. It might be useful both in acute manifestations of vascular occlusive disease involving thrombosis and vasospasm, in addition to the more chronic conditions involving intimal hyperplasia (as in arteriovenous grafts) and possibly frank atherosclerosis. Much work remains to be done, including examination of RS-93427 in chronic studies with various dosage forms, particularly in the study of atherosclerosis.
D000284:Administration, Oral; D000818:Animals; D001157:Arterial Occlusive Diseases / Q000150:complications / Q000188:drug therapy*; D001161:Arteriosclerosis / Q000150:complications / Q000188:drug therapy*; D001682:Biological Availability; D001952:Bridged-Ring Compounds / Q000008:administration & dosage / Q000627:therapeutic use*; D005342:Fibrinolysis / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects; D013927:Thrombosis / Q000188:drug therapy; D014664:Vasodilation / Q000187:drug effects
D001952:Bridged-Ring Compounds; C050064:RS 93427-007