Enzalutamide is a second-generation androgen receptor inhibitor used to treat castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer. It is a second-generation antiandrogen agent that the FDA approved on August 31, 2012.
- Mechanism
- Curator reviewed · 6 references
Enzalutamide is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling pathway without significant AR agonist activity. It inhibits androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with chromosomal DNA to upregulate oncogenes. Enzalutamide binds to the AR with 5 to 8-fold greater affinity than first-generation antiandrogens such as bicalutamide and only 2-3 fold reduced affinity than the natural ligand dihydrotestosterone. Molecular docking showed that enzalutamide binds to the ligand binding domain of the AR distinctive from that of bicalutamide.
- Primary indication
- Enzalutamide is indicated for the treatment of castration-resistant prostate cancer, metastatic castration-sensitive prostate cancer (mCSPC), and non-metastatic castration-sensitive prostate cancer (nmCSPC) with biochemical recurrence at high risk for metastasis (high-risk BCR).Curator reviewed · 7 structured indications
- Formula / weight
- C21H16F4N4O2S · 464.436 g/mol (avg)
- First approval
- Canada, 2013 · United States, 2012 · European Union, 2016
- Code names
- ASP-9785 · MDV-3100
- Brand names
Resolves to
WXCXUHSOUPDCQV-UHFFFAOYSA-NSMILESCNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)FWhat you can answer from here — as of May 26, 2026
Which drugs share a target with Enzalutamide, and which of those have an active Phase 3 trial?
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