Enzalutamide is an androgen receptor (AR) antagonist primarily used in the treatment of prostate cancer, particularly in metastatic castration-resistant prostate cancer (mCRPC) that has progressed after chemotherapy.
Basic Information
English Name: Enzalutamide
Chemical Formula: C21H16F4N4O2S
Molecular Weight: 464.44
CAS Number: 915087-33-1
Indications and Uses
Used to treat advanced male patients with metastatic castration-resistant prostate cancer (mCRPC) that has progressed despite chemotherapy.
In 2018, the FDA expanded the indication to include non-metastatic castration-resistant prostate cancer (NM-CRPC).
Pharmacological Action
Enzalutamide competitively inhibits the binding of androgens to the androgen receptor, blocking the androgen-receptor complex from entering the nucleus and recruiting coactivators.
It also induces apoptosis in tumor cells and has no agonist activity.
