ERLEADA (Apalutamide) – Oral Prostate Cancer Treatment by Janssen Products

ERLEADA (apalutamide) is an oral medication approved for treating certain types of prostate cancer. It is specifically used for metastatic castration-sensitive prostate cancer and non-metastatic castration-resistant prostate cancer in adult male patients. It works by blocking androgen receptors, which play a key role in prostate cancer growth.

• Treatment of metastatic castration-sensitive prostate cancer (mCSPC).
• Treatment of non-metastatic castration-resistant prostate cancer (nmCRPC).
• Intended for use in male patients who are also receiving a gonadotropin-releasing hormone (GnRH) analog or have undergone bilateral orchiectomy.

Apalutamide

Apalutamide inhibits androgen receptors, preventing androgens such as testosterone from stimulating prostate cancer cells. This suppression of androgen receptor signaling helps to slow down or stop the growth of prostate cancer cells that require these hormones to grow.

Recommended Dose

The usual dose of ERLEADA is 240 mg taken orally once daily. Tablets should be swallowed whole and can be taken with or without food.

Special Populations

For patients with severe hepatic impairment (Child-Pugh Class C), the dose should be reduced to 120 mg orally once daily.

Concomitant Therapy

ERLEADA treatment must be combined with a GnRH analog or be used in patients who have had bilateral orchiectomy.

Dose Modifications for Adverse Reactions

• Withhold ERLEADA for Grade 3 or 4 adverse reactions or other intolerable side effects.
• Consider permanent discontinuation for Grade 3 or 4 cerebrovascular or ischemic cardiovascular events, severe interstitial lung disease/pneumonitis, or confirmed severe cutaneous adverse reactions (SCARs).
• For other adverse effects, resume treatment at the same or a reduced dose (180 mg or 120 mg) once symptoms improve to mild or baseline.

Alternate Administration

For patients unable to swallow tablets whole, tablets can be dispersed in non-carbonated water and mixed with orange juice, applesauce, or additional water immediately before administration. Do not store the mixture for later use.

ERLEADA tablets can also be administered via feeding tube (8 French or greater) following specific preparation instructions involving dispersion in water and immediate administration.

None stated.

Cerebrovascular and Ischemic Cardiovascular Events

Serious cerebrovascular and ischemic cardiovascular events, including deaths, have been reported. Patients should be monitored for symptoms of ischemic heart disease and cerebrovascular disorders. Cardiovascular risk factors such as hypertension, diabetes, and dyslipidemia should be managed appropriately. Consider stopping ERLEADA for severe (Grade 3 or 4) events.

Fracture Risk

Patients receiving ERLEADA have an increased risk of fractures. Evaluate fracture risk before and during treatment and manage accordingly, including considering bone-targeted agents.

Falls

Falls have been more frequent, especially in elderly patients. Assess fall risk during treatment.

Seizure

Seizures have occurred in about 0.4% of patients. ERLEADA must be permanently discontinued if a seizure occurs. Patients should be warned about the risk and advised to avoid activities where sudden loss of consciousness is dangerous.

Severe Cutaneous Adverse Reactions (SCARs)

Rare but potentially fatal skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported. Monitor patients closely for rash and other symptoms; interrupt treatment if SCAR is suspected and discontinue permanently if confirmed.

Interstitial Lung Disease (ILD)/Pneumonitis

Fatal and life-threatening ILD or pneumonitis cases have been reported. Monitor for respiratory symptoms; withhold ERLEADA if suspected and permanently discontinue if severe or if no other cause is identified.

Embryo-Fetal Toxicity

ERLEADA can cause fetal harm if administered to a pregnant female. Males with female partners of reproductive potential should use effective contraception during treatment and for 3 months after the last dose.

Interference with Digoxin Assays

ERLEADA may cause falsely elevated plasma digoxin concentration results in certain immunoassays. Laboratories should be notified to use appropriate methods to avoid misinterpretation.

Common Adverse Reactions (≥10%)

• Fatigue
• Arthralgia (joint pain)
• Rash
• Decreased appetite
• Falls
• Weight loss
• Hypertension
• Hot flush
• Diarrhea
• Fracture

Serious Adverse Reactions

• Cerebrovascular and ischemic cardiovascular events including death
• Seizure
• Severe cutaneous adverse reactions such as SJS/TEN and DRESS
• Interstitial lung disease/pneumonitis

Apalutamide can interfere with certain digoxin immunoassays, leading to falsely high digoxin levels. Inform laboratory personnel to use an appropriate assay method.

Pregnancy and Contraception

ERLEADA can cause fetal harm and pregnancy loss based on animal studies. It should not be used by females. Males with partners of reproductive potential must use effective contraception during treatment and for 3 months after stopping ERLEADA.

Lactation

Safety and efficacy in females, including nursing mothers, have not been established.

Store ERLEADA tablets according to the product packaging instructions.