Abstract: The present disclosure discloses use of polaprezinc (Pola) in preparing a drug for treating castration-resistant prostate cancer (CRPC) and belongs to the technical field of biological medicine. The present disclosure provides a new strategy for preparing the drug for treating the CRPC by combining the Pola with an androgen receptor antagonist for the first time and conducts a multi-angle and multi-level verification research. A drug composition combining the polaprezinc and the androgen receptor antagonist can be used for treating castration-resistant prostate cancer, remarkably improves an effect of enzalutamide in inhibiting the castration-resistant prostate cancer, realizes new use of the old drug, can greatly shorten time from drug discovery to clinical transformation, and has important clinical treatment significance.