Class/mechanism: Antiandrogen; androgen receptor inhibitor (ARI). Apalutamide competitively inhibits activity mediated by the androgen receptor (AR) by binding directly to the AR ligand-binding domain, nuclear translocation, DNA binding, and AR-mediated transcription. A metabolite of apalutamide,
N-desmethyl apalutamide, also exhibits some AR inhibiting activity, about 1/3 that of apalutamide.
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Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 2/14/2018: FDA approved "for patients with non-metastatic castration-resistant prostate cancer (NM-CRPC)."
- 9/17/2019: Approved for patients with metastatic castration-sensitive prostate cancer (mCSPC).
Also known as
- Code name: ARN-509
- Brand name: Erleada