Development of Fasudil Hydrochloride (Eril®) : A New Protein Kinase Inhibitor

A series of isoquinolinesulfonamide derivatives were synthesized and shown to possess vasodilatory action. 1- (5-Isoquinolinesulfonyl) homopiperazine hydrochloride (fasudil) had more potent vasodilatory effect to vertebral artery than diltiazem. Fasudil inhibits protein kinase and dilates spastic cerebral arteries in the canine two-hemorrhage model. In clinical studies with fasudil administered by intravenous injection in patients who had undergone sugery for subarachnoid hemorrhage, fasudil significantly reduced the occurrence of vasospasm. In Japan, fasudil was approved in june, 1995.