Pharmacological management of urinary incontinence (UI) is currently based on antimuscarinic and beta-3-agonist drugs. Botulinum toxin A detrusor injections represent an effective but more invasive alternative. This review covers the latest developments of the currently available drugs and the emerging compounds for the treatment of UI. Evidence shows that new antimuscarinics and beta-3-agonists with improved safety profiles may offer unique options to patients intolerant to currently available drugs. Combination therapy proved to be a non-invasive alternative for patients refractory to first-line monotherapy. Exciting advances are ongoing in the research to improve the efficacy/tolerability profile of botulinum toxin, through innovative routes of administration. Several new agents emerged from preclinical studies, some of which have now entered the clinical phase of development and could represent, in the coming years, a new way for the treatment of UI. Recent evidence on the existence of different overactive bladder phenotypes could be the key to tailored treatment. Rather than discovering new molecules, reaching the ability to identify the right drug for the right patient could be the real gamechanger of the future.