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Xtandi (enzalutamide)
Xtandi works by blocking the androgen receptor, a protein that helps prostate cancer cells grow.
Xtandi (enzalutamide) is a small molecule androgen receptor inhibitor developed by Astellas, targeting the androgen receptor to treat prostate cancer. It was FDA-approved in 2012 for the treatment of malignant tumor of prostate and metastasis from malignant tumor of prostate. Xtandi is currently owned by Astellas and has multiple generic manufacturers. As a patented medication, its commercial status is subject to change. Key safety considerations include potential side effects such as fatigue, diarrhea, and hypertension.
At a glance
| Generic name | enzalutamide |
|---|---|
| Sponsor | Astellas Pharma |
| Drug class | Androgen Receptor Inhibitor [EPC] |
| Target | Androgen receptor |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2012 |
| Annual revenue | 4500 |
Mechanism of action
Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors; and consequently, inhibits nuclear translocation of androgen receptors and their interaction with DNA. major metabolite, N-desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in mouse prostate cancer xenograft model.
Approved indications
- Malignant tumor of prostate
- Metastasis from malignant tumor of prostate
Common side effects
- Asthenia/Fatigue
- Back Pain
- Hot Flush
- Constipation
- Arthralgia
- Diarrhea
- Hypertension
- Peripheral Edema
- Dizziness
- Headache
- Musculoskeletal Pain
- Muscular Weakness
Drug interactions
- P-glycoprotein Substrates
- alfentanil
- aprepitant
- aripiprazole
- astemizole
- axitinib
- boceprevir
- bortezomib
- bosentan
- bosutinib
- carbamazepine
- ciclosporin
Key clinical trials
- A Study of Enzalutamide Versus Bicalutamide in Castrate Men With Metastatic Prostate Cancer (PHASE2)
- A Safety and Efficacy Study of Oral MDV3100 in Chemotherapy-Naive Patients With Progressive Metastatic Prostate Cancer (PHASE3)
- Safety and Efficacy Study of MDV3100 in Patients With Castration-Resistant Prostate Cancer Who Have Been Previously Treated With Docetaxel-based Chemotherapy (PHASE3)
- A Study of Enzalutamide Plus Androgen Deprivation Therapy (ADT) Versus Placebo Plus ADT in Patients With Metastatic Hormone Sensitive Prostate Cancer (mHSPC) (PHASE3)
- Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer and Suboptimal PSA Response (PHASE3)
- Enzalutamide and PDS01ADC in PET Positive Recurrent Prostate Cancer (pprPC) Without Testosterone Lowering Therapy (PHASE2)
- 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 to Learn How PF-06821497 (Mevrometostat) Works in Men With Metastatic Castration-resistant Prostate Cancer. (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
| 12502357 | 2033-09-11 | Method of Use |
| 12447128 | 2033-09-11 | Method of Use |
| 11839689 | 2033-09-11 | Formulation |
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Xtandi CI brief — competitive landscape report
- Xtandi updates RSS · CI watch RSS
- Astellas Pharma portfolio CI