Apalutamide

Apalutamide is a prescription medication used for the treatment of prostate cancer. 

• Apalutamide is available under various brand names: Erleada

Common side effects of Apalutamide include:

• hot flashes,
• tiredness,
• joint pain,
• nausea,
• decreased appetite,
• weight loss, and
• decreased sexual interest or ability

Serious side effects of Apalutamide include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• unusual weight gain,
• cold intolerance,
• slow heartbeat,
• constipation,
• muscle weakness,
• increased risk for fractures,
• sore throat,
• fever,
• chills,
• cough,
• chest, jaw, and left arm pain,
• shortness of breath,
• unusual sweating,
• weakness on one side of the body,
• trouble speaking,
• sudden vision changes,
• confusion,
• seizure,
• severe dizziness, and
• skin rash (no matter how mild)

Rare side effects of Apalutamide include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 60 mg

Prostate Cancer

Adult dosage

• 240 mg orally every day

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Apalutamide has severe interactions with the following drugs:
  • cabotegravir
  • doravirine
  • fostemsavir
  • isavuconazonium sulfate
  • lonafarnib
  • lorlatinib
  • mavacamten
  • nirmatrelvir
  • nirmatrelvir/ritonavir
• Apalutamide has serious interactions with at least 351 other drugs.
• Apalutamide has moderate interactions with at least 154  other drugs.
• Apalutamide has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Apalutamide?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Apalutamide?”

Cautions

• Cerebrovascular and ischemic cardiovascular events, including events leading to death, are reported; monitor for signs and symptoms of ischemic heart disease and cerebrovascular disorders; optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia; consider discontinuing if Grade 3 or 4 events occur.
• Falls and fractures reported; evaluate the patient for risk; monitor and manage patients at risk for fractures according to established treatment guidelines and consider the use of bone-targeted agents; falls were not associated with loss of consciousness or seizure.
• Seizures reported; permanently discontinue if a seizure occurs during treatment; unknown whether anticonvulsants will prevent seizures with apalutamide; there is no clinical experience in re-administering therapy to patients who experienced a seizure.
• Advise patients of the risk of developing a seizure while on therapy and harm, to themselves or others, that could occur from a sudden loss of memory while engaging in activities.
• Based on its mechanism of action, apalutamide can cause fetal harm and loss of pregnancy if administered to pregnant women.
• Drug interaction overview
• Strong CYP2C8 or CYP3A4 inhibitors
  • Coadministration with strong CYP2C8 or CYP3A4 inhibitors is predicted to increase the steady-state exposure of the active apalutamide moieties
  • No initial dose adjustment is necessary; however, reduce the dose based on tolerability
  • Mild or moderate CYP2C8 or CYP3A4 inhibitors are not expected to affect apalutamide levels
• CYP3A4, CYP2C9, CYP2C19, and UGT substrates
  • Apalutamide is a strong inducer of CYP3A4 and CYP2C19, a weak inducer of CYP2C9, and it induces UDP-glucuronosyltransferase (UGT)
  • Drugs primarily metabolized by CYP3A4, CYP2C19, or CYP2C9 can result in lower exposure to these medications; use alternate medications when possible or evaluate for loss of activity if medication is continued
  • Caution if UGT substrates must be coadministered with apalutamide and evaluated for loss of activity
• P-gp, BCRP, or OATP1B1 substrates
  • Apalutamide is a weak inducer of P-gp, BCRP, and OATP1B1 clinically
  • Coadministration of apalutamide with these substrates can result in lower exposure to these drugs; caution if these substrates must be coadministered with apalutamide and evaluated for loss of activity

Pregnancy & Lactation

• The safety and efficacy of the drug have not been established in females. There are no available data on use in pregnant women to inform a drug-associated risk
• Based on findings from animals and its mechanism of action, the drug can cause fetal harm and loss of pregnancy when administered to a pregnant female
• In an animal reproduction study, oral administration of the drug to pregnant rats during and after organogenesis resulted in fetal abnormalities and embryo-fetal lethality at maternal exposures greater than or equal to 2 times the human clinical exposure (AUC) at the recommended dose
• The drug is not indicated for use in females, so animal embryo-fetal developmental toxicology studies were not conducted
• Contraception
  • Based on the mechanism of action and findings in an animal reproduction study, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose
• Infertility
  • Based on animal studies, it may impair fertility in males of reproductive potential
• Lactation
  • Not indicated for use in females
  • No data are available on the presence of human milk or its effect on the breastfed child or milk production