Saw palmetto extract (SPE) has been widely used as a therapeutic remedy for urinary dysfunction in western countries. Furthermore, as an herb drug, it can be used as an alternative therapy for benign prostatic hyperplasia (BPH) due to its safety and minimum adverse effects. Reportedly, SPE improves the urinary symptoms, which mainly depend on anti-androgenic effects and effects on autonomic receptors in the lower urinary tract. However, the mechanisms of action responsible for the therapeutic roles of SPE have not been fully elucidated. Relevant studies indicate that SPE has some positive effects on the treatment of urological diseases in animals, and clinical trials are ongoing. In this review, we summarize the pharmacological properties and discuss the possible therapeutic mechanisms of SPE in urological diseases, including anti-androgenic effects, effects on autonomic receptors in the lower urinary tract, anti-inflammatory activity, anti-proliferative and pro-apoptotic effects, and highlight a potential therapeutic approach in the clinical treatment of patients with BPH, prostate cancer, chronic prostatitis (CP) and erectile dysfunction (ED).