The treatment strategies for prostate cancer (PCa) vary depending on the stage of the disease, with precise staging guiding individualized therapy. In recent years, the discovery of prostate-specific membrane antigen (PSMA) and the application of related targeting technologies have fundamentally transformed the diagnostic and therapeutic landscape of PCa. This article will systematically review the latest advancements in the application of PSMA in prostate cancer from four aspects: molecular mechanisms, diagnostic applications, therapeutic progress, and future challenges, providing a reference for clinical practice.