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Abiraterone Acetate or Enzalutamide
Abiraterone acetate inhibits CYP17A1 to block androgen synthesis, while enzalutamide antagonizes the androgen receptor, both reducing androgen-driven prostate cancer growth.
Abiraterone acetate inhibits CYP17A1 to block androgen synthesis, while enzalutamide antagonizes the androgen receptor, both reducing androgen-driven prostate cancer growth. Used for Metastatic castration-resistant prostate cancer (mCRPC), Non-metastatic castration-resistant prostate cancer (nmCRPC).
At a glance
| Generic name | Abiraterone Acetate or Enzalutamide |
|---|---|
| Sponsor | National Cancer Institute, Naples |
| Drug class | Androgen synthesis inhibitor (abiraterone) / Androgen receptor antagonist (enzalutamide) |
| Target | CYP17A1 (abiraterone) / Androgen receptor (enzalutamide) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Abiraterone acetate is a prodrug that inhibits 17α-hydroxylase/17,20-lyase (CYP17A1), a key enzyme in testosterone and DHT synthesis, thereby depleting intratumoral androgens. Enzalutamide is an androgen receptor antagonist that blocks AR signaling downstream. Together or individually, these agents suppress the androgen axis critical for castration-resistant prostate cancer (CRPC) progression.
Approved indications
- Metastatic castration-resistant prostate cancer (mCRPC)
- Non-metastatic castration-resistant prostate cancer (nmCRPC)
Common side effects
- Hypertension
- Hypokalemia
- Fatigue
- Hot flashes
- Diarrhea
- Seizures (enzalutamide)
- Hepatotoxicity
Key clinical trials
- A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02) (PHASE1, PHASE2)
- A Study of Opevesostat (MK-5684) Versus Alternative Next-generation Hormonal Agent (NHA) in Metastatic Castration-resistant Prostate Cancer (mCRPC) Post One NHA (MK-5684-004) (PHASE3)
- A Study of Tinengotinib (TT-00420) in Combination With Standard Treatments in People With Prostate Cancer (PHASE1, PHASE2)
- Study of Opevesostat (MK-5684) Versus Alternative NHA in mCRPC (MK-5684-003) (PHASE3)
- A Study of Tazemetostat With Enzalutamide or Abiraterone/Prednisone in Participants With Advanced Prostate Cancer (PHASE1, PHASE2)
- Study of AMG 509 in Participants With Metastatic Castration-Resistant Prostate Cancer (PHASE1)
- A Study to Learn About the Investigational Medicine Called PF-06821497 (Mevrometostat) in Men With mCRPC Who Were Previously Treated With Abiraterone Acetate for Prostate Cancer (MEVPRO-1). (PHASE3)
- Targeted Treatment for Metastatic Prostate Cancer, The PREDICT Trial (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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