Erleada Apalutamide Tablets

1. Indications and Usage
Metastatic Hormone-Sensitive Prostate Cancer: Indicated for the treatment of adult patients with metastatic hormone-sensitive prostate cancer (mHSPC).
Non-Metastatic Castration-Resistant Prostate Cancer: Indicated for the treatment of adult patients with non-metastatic castration-resistant prostate cancer (nmCRPC).
Requirement: Patients must receive concomitant androgen deprivation therapy (ADT) or have undergone bilateral orchiectomy.
2. Dosage and Administration
Recommended Dose: The recommended dose is 240 mg (four 60 mg tablets) taken orally once daily.
Administration: Tablets must be swallowed whole and can be taken with or without food.
Missed Dose: If a dose is missed, it should be taken as soon as possible on the same day. The next dose should be taken at the regular time; do not take extra doses to make up for a missed one.
Dose Modification: If Grade ≥3 toxicity or intolerable adverse reactions occur, withhold the drug until symptoms improve to Grade ≤1 or baseline. Then resume at the same dose or reduce to 180 mg or 120 mg as necessary.
Alternative Administration: For patients with difficulty swallowing, the tablets can be dispersed in water or taken with applesauce.
3. Mechanism of Action
Androgen Receptor Inhibition: Apalutamide is a small molecule inhibitor of the androgen receptor.
Tumor Suppression: It binds directly to the androgen receptor, inhibiting its nuclear translocation, DNA binding, and transcriptional activity, thereby suppressing tumor growth.
4. Safety and Warnings
Severe Cutaneous Adverse Reactions (SCARs) and Interstitial Lung Disease: Apalutamide may cause severe skin reactions and interstitial lung disease. If confirmed, permanent discontinuation is required.
Seizures: Apalutamide may lower the seizure threshold. Patients with a history of seizures or risk factors should be monitored closely. If a seizure occurs, permanently discontinue the drug.
Fractures and Falls: Monitor for fractures and falls, particularly in elderly patients.
Cardiovascular Risk: Monitor for symptoms of ischemic heart disease and cerebrovascular disease.
5. Adverse Reactions and Clinical Research
Adverse Reactions: The most common adverse reactions (occurring in ≥10% of patients) include fatigue, arthralgia, rash, decreased appetite, falls, weight decreased, hypertension, hot flushes, diarrhea, and fractures.
Clinical Research: Clinical trials (TITAN and SPARTAN) demonstrated that apalutamide significantly improved overall survival and metastasis-free survival in patients with mHSPC and nmCRPC.
6. Drug Interactions
CYP3A4 Inhibitors: Concomitant use with strong CYP3A4 inhibitors should be avoided.
CYP3A4 Inducers: Concomitant use with strong CYP3A4 inducers should be avoided.
Anticonvulsants: Concomitant use with CYP3A4 inducers (e.g., phenytoin, carbamazepine) should be avoided.
Warfarin and Coumarin Derivatives: Monitor INR values closely if used concomitantly.
7. Pharmaceutical Information
Composition: The active ingredient is apalutamide. Excipients include colloidal silicon dioxide, sodium croscarmellose, hydroxypropyl methylcellulose acetate succinate, magnesium stearate, microcrystalline cellulose, and silicified microcrystalline cellulose.
Appearance: Light yellow to gray-green oval film-coated tablets, with “AR 60” debossed on one side.
Storage: Store at 20°C to 25°C (68°F to 77°F).