A protein kinase inhibitor, fasudil (AT-877): A novel approach to signal transduction therapy

The protein kinase inhibitor fasudil is the first clinically effective signal transduction therapy for vascular diseases. Fasudil significantly dilates spastic arteries in canine cerebral and swine coronary artery vasospasm models. It augments MLC phosphorylation in vasospastic arteries. Phosphorylation of MLC is one of the most important steps in vascular smooth muscle contraction. Fasudil inhibits several protein kinases that regulate smooth muscle contraction. Several clinical studies demonstrate that fasudil is a safe and useful drug. Its discovery demonstrates how molecular medicine is providing us with the tools for the development of novel therapeutics, that are likely to improve treatment of vascular diseases.