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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Anti-androgens
apalutamide
L02BB05
Adult Dosing
- Non-metastatic castration-resistant prostate cancer (nmCRPC): 240 mg orally once daily
- Metastatic castration-sensitive prostate cancer (mCSPC): 240 mg orally once daily
- Administer with a gonadotropin-releasing hormone (GnRH) analog or after bilateral orchiectomy
- Modify dose for Grade 3 or higher toxicities
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of patients with non-metastatic castration-resistant prostate cancer (nmCRPC)
- Treatment of patients with metastatic castration-sensitive prostate cancer (mCSPC)
Mechanism of Action
- Androgen receptor inhibitor
- Binds directly to the ligand-binding domain of the androgen receptor
- Prevents androgen receptor translocation, DNA binding, and gene transcription
- Induces apoptosis and decreases tumor volume in prostate cancer cells
Contraindications
- Pregnancy or women who may become pregnant
- Known hypersensitivity to apalutamide or any of its components
Adverse Reactions
- Fatigue
- Arthralgia
- Rash
- Hypertension
- Hot flashes
- Nausea
- Falls
- Fractures
- Weight decreased
- Seizures
Drug Interactions
- Strong CYP3A4 inducers (e.g., rifampin): May decrease apalutamide efficacy; avoid coadministration
- CYP3A4 and CYP2C19 substrates: Apalutamide is a strong inducer; coadministration decreases plasma concentrations of these drugs
- CYP2C9 substrates: Apalutamide is a strong inducer; coadministration decreases plasma concentrations of these drugs
- P-gp, BCRP, and OATP1B1 substrates: Apalutamide is an inducer; may decrease efficacy of transporter substrates
Curated Content: Needs Vetting Before Put to Clinical Use