Oral pharmacotherapy has become the first-line therapy for the majority of patients with erectile dysfunction (ED) of broad-spectrum etiology since the introduction of oral sildenafil, a potent, selective inhibitor of phosphodiesterase type 5 (PDE5). More than 3 years following the launch of sildenafil have made us informed fully about the mechanism of sildenafil, its clinical efficacy and safety, and appropriate use of the drug. Recently, the efficacy and tolerability of another potent, selective inhibitors of PDE5, vardenafil and tadalafil have been reported one after another and their phase 3 clinical studies worldwide have just finished. The PDE5 inhibitors are contraindicated in patients taking nitrates and may be restricted in others. The recent introduction of sublingual (SL) apomorphine, a centrally acting dopaminergic agonist with known erectogenic effects, could provide patients and clinicians with an additional option in the treatment of ED, although its efficacy and safety need to be verified further by worldwide clinical studies. We are in face of the era of multiple oral agents available for the treatment of ED. Due to the complex nature of individual patient-oriented goals and the multifactorial nature of ED, choices are needed that can be adapted to the requirements and responses of the individual patients. In this review, an overview of the pharmacokinetics, efficacy and safety of the oral PDE5 inhibitors, sildenafil, vardenafil and tadalafil, and sublingual apomorphine are provided.