Results of the first-in-man, dose-escalation study of a prostate-specific membrane antigen antibody–drug conjugate (PSMA ADC) have been reported. This therapy is designed to bind to PSMA+ cells specifically, internalize and release the drug into the cell. PSMA ADC has shown promise in preclinical models. In this study, the conjugate showed antitumour activity at doses ≤2.5 mg/kg in a cohort of 52 men with metastatic castration-resistant prostate cancer (mCRPC) and toxic effects were acceptable. Thus, this new therapy has promise for treating mCRPC.