Benign prostatic hyperplasia (BPH) affects the majority of aging men, with medical therapy representing the first-line treatment of lower urinary tract symptoms (LUTS). This article comprehensively examines current medical therapies, their mechanisms, efficacy, and optimal patient selection strategies through a literature review of pivotal clinical trials, systematic reviews, and treatment guidelines from 2000 to 2024. Medical therapy for BPH/LUTS has evolved from symptom management to disease modification, and combination therapy with alpha-1 adrenergic antagonists and 5-alpha reductase inhibitors represents optimal treatment of men with moderate-to-severe symptoms and enlarged prostates (≥30 mL).