Novel Agents Targeting the Androgen Receptor in Castration-Resistant Prostate Cancer

VIDEO | 3:00

Medical oncologist Dana Rathkopf from Memorial Sloan Kettering’s Genitourinary Oncology Service discusses therapies for metastatic prostate cancer that target the androgen receptor (AR). This protein is important in the development and progression of prostate cancer.

Our investigators led the first-in-person study of enzalutamide (MDV3100), a next-generation anti-androgen that blocks testosterone from binding to the AR. This study led to further development and approval of the agent enzalutamide for the treatment of men with castration-resistant prostate cancer (CRPC) who already have received chemotherapy. Another AR-targeted therapy, abiraterone acetate, inhibits the adrenal production of testosterone and has recently been approved for the treatment of men with CRPC before as well as after chemotherapy.

Building on these exciting advances in AR-targeted therapies, Memorial Sloan Kettering investigators recently published the results of a phase I study demonstrating the safety and efficacy of the investigational anti-androgen ARN-509. The study used fluoro-dihydrotestosterone PET imaging to show that ARN-509 blocks the AR in humans. Drugs that target the AR may have fewer side effects than conventional chemotherapy agents because they target the AR on prostate cancer cells directly, and may improve outcomes for men with metastatic disease.