Plants produce many secondary metabolites that lead to defensive mechanisms and regulate signaling for defense against herbivores, pests, and diseases. The plant secondary metabolites are made of polyphenolic compounds, such as flavonoids, alkaloids, saponins, tannins, glycosides, etc., which are new lead molecules in drug discovery research of aphrodisiacs. Plants and their formulations (external, oral solid and liquid dosage) have been used traditionally to treat various issues, including male penile erectile dysfunction (ED). ED is a chronic disorder characterized by the inability to achieve and sustain a penile erection, resulting in unsatisfying sexual intercourse. This chapter presents a brief overview of male inadequacy, factors influencing the induction of pathophysiology of ED, and corrective modalities and also discusses currently available treatment strategies and their adverse reactions and alternative therapies for safely treating ED.