Pharmacologic therapies (primarily antimuscarinic agents) have been the mainstay of treatment for overactive bladder. In their traditional forms, these drugs produce variable efficacy, a moderate prevalence of side effects, and rare occurrences of cure. The search for newer and better formulations and derivatives of this class of medication (as well as novel therapies) is ongoing, fueled primarily by the high prevalence of overactive bladder and the tremendous number of healthcare dollars spent on current therapy. In the present article, we discuss recent advances in the development of new antimuscarinic agents, important progress in understanding the mechanism of action of this class of drug, and the impact these developments have had on clinical practice.