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APALUTAMIDE
Apalutamide binds to the androgen receptor, blocking its function and reducing tumor growth.
Apalutamide is a marketed androgen receptor inhibitor used primarily for metastatic castration-sensitive prostate cancer. Its key strength lies in its mechanism of action, which effectively blocks the androgen receptor, thereby reducing tumor growth. The primary risk is the key composition patent expiry in 2028, which could lead to increased competition from generics.
At a glance
| Generic name | APALUTAMIDE |
|---|---|
| Target | Androgen Receptor (AR) |
| Modality | Small molecule |
| Phase | FDA-approved |
| First approval | 2018 |
Mechanism of action
Apalutamide works by binding to the androgen receptor, which prevents it from moving into the nucleus and binding to DNA. This stops the receptor from activating genes that promote tumor growth, leading to reduced tumor size and increased cancer cell death.
Approved indications
- Metastatic castration-sensitive prostate cancer
- Non-metastatic castration-resistant prostate cancer
Common side effects
- arthralgia
- rash
- pruritus
- hot flush
- hypertension
- diarrhea
- muscle spasm
- dysgeusia
- hypothyroidism
- ILD/pneumonitis
- white blood cell decreased
- hypertriglyceridemia
Drug interactions
- Strong CYP2C8 or CYP3A4 Inhibitors
- Substrates of CYP3A4, CYP2C9, CYP2C19, P-gp, BCRP, or OATP1B1
Key clinical trials
- Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer and Suboptimal PSA Response (PHASE3)
- Multi-arm Multi-modality Therapy for Very High Risk Localized and Low Volume Metastatic Prostatic Adenocarcinoma (PHASE2)
- Testing the Effects of Low Dose Apalutamide on Prostate-Specific Antigen (PSA) Levels in Men Scheduled for Removal of the Prostate Gland (PHASE2)
- A Study of Apalutamide Combined With GnRH Agonist in Participants With Androgen Receptor Positive Salivary Gland Carcinoma (PHASE2)
- Exploration of Treatment Effect of Novel Hormone Therapy Combined With Local Treatment Based on PSMA PET/CT Evaluation in mHSCP Patients (PHASE2)
- A Study of Apalutamide (ARN-509) in Men With Non-Metastatic Castration-Resistant Prostate Cancer (PHASE3)
- Active Surveillance With or Without Apalutamide Treatment in Low Risk Prostate Cancer (PHASE2)
- A Study of Apalutamide (JNJ-56021927, ARN-509) Plus Androgen Deprivation Therapy (ADT) Versus ADT in Participants With mHSPC (PHASE3)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- APALUTAMIDE CI brief — competitive landscape report
- APALUTAMIDE updates RSS · CI watch RSS