• Prostate and other male cancers

Erleada Generic Name & Formulations

General Description

Apalutamide 60mg, 240mg; tabs.

Pharmacological Class

Androgen receptor inhibitor.

How Supplied

Tabs 60mg—120; 240mg—30


Generic Availability


Mechanism of Action

Apalutamide binds directly to the ligand-binding domain of the androgen receptor (AR), thereby inhibiting AR nuclear translocation, inhibiting DNA binding, and impeding AR-mediated transcription.

Erleada Indications


Metastatic castration-sensitive prostate cancer. Non-metastatic, castration-resistant prostate cancer.

Erleada Dosage and Administration


Swallow whole (alternate methods of administration if difficulty swallowing tab; see full labeling). Take with or without food. 240mg once daily. Give concurrent GnRH analog or patient should have had bilateral orchiectomy. Dose modifications: see full labeling.


Not established.

Erleada Contraindications

Not Applicable

Erleada Boxed Warnings

Not Applicable

Erleada Warnings/Precautions


Monitor for ischemic heart disease, cerebrovascular disorders; consider discontinuation for Grade 3/4 events. Manage CV risk factors (eg, hypertension, diabetes, dyslipidemia) optimally. Risk of seizures; permanently discontinue if occurs. Evaluate for fracture risk (monitor/manage based on guidelines; consider bone-targeted agents) and fall risk (esp. elderly). Monitor for severe cutaneous adverse reactions; interrupt therapy if suspected; permanently discontinue if confirmed. Embryo-fetal toxicity. Advise males (w. female partners of reproductive potential) to use effective contraception during and for 3 months after the last dose.

Erleada Pharmacokinetics


Mean absolute oral bioavailability: ~100%. Median time to achieve peak plasma concentration (tmax): 2 hours (range: 1–5 hours).


Plasma protein bound: 96% (apalutamide); 95% (N-desmethyl apalutamide). 


CYP2C8, CYP3A4. 


Renal (65%), fecal (24%). Half-life: ~3 days.

Erleada Interactions


Potentiated by strong CYP2C8 or CYP3A4 inhibitors; reduce dose based on tolerability. Antagonizes drugs metabolized by CYP3A4, CYP2C19, or CYP2C9; use alternatives when possible. Caution with concomitant P-gp, BCRP, OATP1B1, or UGT substrates.

Erleada Adverse Reactions

Adverse Reactions

Fatigue, arthralgia, rash, decreased appetite, fall, weight decreased, hypertension, hot flush, diarrhea, fracture; ischemic CV events, cerebrovascular disorders, severe cutaneous adverse reactions (eg, SJS, TEN, DRESS).

Erleada Clinical Trials

See Literature

Erleada Note

Not Applicable

Erleada Patient Counseling

See Literature