The Pharmacological Profile of the α1A-Adrenoceptor Antagonist Silodosin

Silodosin, formerly known as KMD-3213, is a novel α-blocker for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia. It has unprecedented selectivity for α1A-adrenoceptors, as compared to both α1B- and α1D-adrenoceptors, exceeding selectivity of all currently used α-blockers. Such selectivity has been shown in vitro with cloned receptor subtypes as well as in a range of isolated human and animal tissues. It translates into in vivo functional uroselectivity in multiple animal species with efficacy against voiding dysfunction combined with a low degree of cardiovascular effects in both animals and patients. These properties make silodosin a clinically promising new agent.