While antimuscarinic drug therapy has been proven to be effective in the management of patients with symptoms of overactive bladder syndrome, compliance and persistence with medication is often affected by the bothersome antimuscarinic adverse effects of dry mouth, constipation, somnolence and blurred vision. The development of bladder-selective M3-specific antagonists, such as solifenacin, has introduced the possibility of increasing efficacy while minimizing adverse effects. This article will review the preclinical and clinical data surrounding the development of solifenacin as well as providing an overview of the extensive body of evidence supporting its use in the management of patients with overactive bladder syndrome.