Androgen Receptor Pathway Inhibitors

These medicines are newer “second-generation” hormone treatments and are FDA-approved for patients with certain states of advanced prostate cancer:

• High-risk biochemical recurrence (non-metastatic HSPC)
• Metastatic hormone-sensitive prostate cancer (mHSPC)
• Non-metastatic castration-resistant prostate cancer (nmCRPC)
• Metastatic castration-resistant prostate cancer (mCRPC).

You may also hear them referred to as androgen receptor signaling inhibitors (ARSIs) or androgen receptor axis targeted agents (ARATs).

• Abiraterone (Zytiga®, Yonsa®) is approved for mHSPC and mCRPC
• Apalutamide (Erleada®) is approved for mHSPC and nmCRPC
• Darolutamide (Nubeqa®) is approved for mHSPC (in combination with hormone therapy and docetaxel) and nmCRPC
• Enzalutamide (Xtandi®) is approved for high-risk biochemical recurrence, mHSPC, nmCRPC, and  mCRPC

Abiraterone blocks the production of testosterone, while apalutamide, darolutamide, and enzalutamide block the action of testosterone. All are taken orally. Some are approved to be given in combination with other medicines called PARP inhibitors in select patients.

They each have their own safety profile, including side effects and interactions with other medications. You and your doctor will need to consider your prostate cancer as well as any other medical conditions when choosing among these agents. For example, patients who have cardiovascular disease should be monitored closely when using these therapies and may need to be followed by a cardiologist.

Last Reviewed: 12/2023