Claire Lin, Matthew J. Hadfield, Ariana Santopietro, Galina Lagos, Liang Cheng, Wafik S. El‐Deiry, Rahul Aggarwal, Anthony Mega, Elias S. Hyams, Benedito A. Carneiro
Advances in antibody-drug conjugate (ADC) technology and identification of new antigen targets are repositioning ADCs as a promising therapeutic platform for metastatic castration-resistant prostate cancer (mCRPC). This review summarizes recent progress in ADC payload and linker chemistry, highlights membrane antigens in prostate cancer that have demonstrated encouraging antitumor activity in clinical trials, and addresses strategies to mitigate off-target toxicity. These advances position ADCs to transform the therapeutic landscape of mCRPC.