Apalutamide — Drug Monograph
Brand names: Erleada
Drug class: Hormonal Agent
Mechanism of Action
Apalutamide is a selective second-generation androgen receptor (AR) inhibitor. It binds directly to the ligand-binding domain of the AR, preventing androgen binding, AR nuclear translocation, and AR-mediated DNA transcription of genes that drive prostate cancer cell growth. This results in decreased tumor cell proliferation and increased apoptosis. Like enzalutamide, it is more potent than first-generation antiandrogens and lacks agonist activity in the setting of AR overexpression.
FDA Indications
- Treatment of adult patients with non-metastatic castration-resistant prostate cancer (nmCRPC)
- Treatment of adult patients with metastatic castration-sensitive prostate cancer (mCSPC)
Common Side Effects
- Fatigue
- Hypertension
- Rash
- Diarrhea
- Nausea
- Weight loss
- Arthralgia
- Hot flush
- Fractures
- Hypothyroidism
Clinical Pearl
Apalutamide is associated with a specific maculopapular rash in about 25% of patients, which usually occurs within the first 3 months and often responds to topical steroids or dose interruption. Unlike enzalutamide, it requires baseline and periodic monitoring of TSH because it can cause hypothyroidism. Because it is a very strong enzyme inducer, pharmacists must perform a thorough medication reconciliation for drug-drug interactions, particularly with anticoagulants like warfarin or DOACs. Be…
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