Erleada 240mg Tablets
It is used to treat prostate cancer. If you have been given this drug for some other reason, talk with your doctor for more information. This drug may be used with other drugs to treat your health condition. If you are also taking other drugs, talk with your doctor about the risks and side effects that may happen.
Drug Class
Antineoplastic agent
Pharmacologic Class
Androgen receptor inhibitor
Pregnancy Category
Not available
FDA Approved
Feb 2018
DEA Schedule
Not Controlled
Overview
What is this medicine?
Erleada is a medicine used to treat prostate cancer in men. It works by blocking the effects of male hormones (androgens) that can make prostate cancer grow. It is taken once a day by mouth.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
Swallowing Your Medication
Swallow the tablet whole. Do not chew, break, or crush it. If you have trouble swallowing the tablet whole, you can mix it with water. To do this, place your dose in a cup and add water as follows:
For a dose of 1 tablet, add about 2 teaspoons (10 mL) of plain water.
For a dose of 4 tablets, add about 4 teaspoons (20 mL) of plain water.
Make sure the tablets are fully covered with water. Wait 2 minutes for the tablets to break up and spread out, then stir. Add 2 tablespoons (30 mL) of orange juice, applesauce, or plain water, and stir again. Swallow the mixture immediately. Rinse the cup with plain water and drink to ensure you take the entire dose.
Using a Feeding Tube
If you have a feeding tube, you can use this medication as directed by your healthcare provider. Be sure to flush the feeding tube after administering the medication.
Storing Your Medication
Store your medication at room temperature, protected from light and moisture. Keep it in a dry place, such as a closet or drawer, and avoid storing it in a bathroom. Store the medication in its original container, and do not remove the antimoisture cube or packet. Keep all medications in a safe place, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. If you don't remember until the next day, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
Swallowing Your Medication
Swallow the tablet whole. Do not chew, break, or crush it. If you have trouble swallowing the tablet whole, you can mix it with water. To do this, place your dose in a cup and add water as follows:
For a dose of 1 tablet, add about 2 teaspoons (10 mL) of plain water.
For a dose of 4 tablets, add about 4 teaspoons (20 mL) of plain water.
Make sure the tablets are fully covered with water. Wait 2 minutes for the tablets to break up and spread out, then stir. Add 2 tablespoons (30 mL) of orange juice, applesauce, or plain water, and stir again. Swallow the mixture immediately. Rinse the cup with plain water and drink to ensure you take the entire dose.
Using a Feeding Tube
If you have a feeding tube, you can use this medication as directed by your healthcare provider. Be sure to flush the feeding tube after administering the medication.
Storing Your Medication
Store your medication at room temperature, protected from light and moisture. Keep it in a dry place, such as a closet or drawer, and avoid storing it in a bathroom. Store the medication in its original container, and do not remove the antimoisture cube or packet. Keep all medications in a safe place, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. If you don't remember until the next day, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Continue to receive your prescribed androgen deprivation therapy (ADT) as directed by your doctor.
- Take Erleada at the same time each day, with or without food.
- Do not crush, chew, or split the tablets. Swallow them whole.
- If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses at once.
- Report any new or worsening side effects to your doctor immediately.
- Maintain good bone health (e.g., calcium and vitamin D supplementation, weight-bearing exercise) as advised by your doctor.
- Monitor blood pressure regularly as instructed by your doctor.
- Avoid driving or operating machinery if you experience dizziness or seizures.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
240 mg orally once daily
Dose Range:
240 - 240 mg
Condition-Specific Dosing:
non-metastatic castration-resistant prostate cancer (nmCRPC):
240 mg orally once daily
metastatic castration-sensitive prostate cancer (mCSPC):
240 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required
Moderate:
No dose adjustment required
Severe:
No dose adjustment required (limited data, monitor for adverse reactions)
Dialysis:
Not available (limited data, monitor for adverse reactions)
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
No dose adjustment required (Child-Pugh B)
Severe:
Not recommended (Child-Pugh C) due to lack of data
Pharmacology
Mechanism of Action
Apalutamide is an androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. It inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is also an active AR inhibitor and exhibits similar in vitro activity to apalutamide.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (high absolute bioavailability)
Tmax:
2 hours (range 1-5 hours)
FoodEffect:
No clinically significant effect of food on exposure
Distribution:
Vd:
276 L (apparent volume of distribution)
ProteinBinding:
96% (apalutamide), 95% (N-desmethyl apalutamide)
CnssPenetration:
Limited (low brain-to-plasma ratio in animal studies, but seizures have been reported)
Elimination:
HalfLife:
Approximately 3 days (75-80 hours) for apalutamide and N-desmethyl apalutamide at steady state
Clearance:
Not available
ExcretionRoute:
Feces (65%), Urine (24%)
Unchanged:
1.2% (urine), 1.5% (feces) of unchanged apalutamide
Pharmacodynamics
OnsetOfAction:
Not precisely defined for clinical effect (chronic therapy)
PeakEffect:
Steady-state concentrations reached within 4 weeks
DurationOfAction:
Not precisely defined (chronic therapy)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of high blood pressure: severe headache, dizziness, fainting, or changes in vision.
Signs of high blood sugar: confusion, drowsiness, excessive thirst or hunger, frequent urination, flushing, rapid breathing, or fruity-smelling breath.
Signs of high potassium levels: abnormal heartbeat, confusion, weakness, lightheadedness, dizziness, numbness or tingling, or shortness of breath.
Signs of low thyroid levels: constipation, sensitivity to cold, memory problems, mood changes, or abnormal burning, numbness, or tingling sensations.
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision.
Chest pain or pressure.
Shortness of breath.
Seizures.
Swelling in the arms or legs.
Bone pain.
Low white blood cell counts can increase the risk of infection. If you experience symptoms like fever, chills, or sore throat, contact your doctor immediately.
Severe and potentially life-threatening lung problems can occur. If you experience new or worsening lung or breathing problems, such as cough or shortness of breath, seek medical help right away.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions, can occur. These reactions can affect internal organs and be life-threatening. If you notice symptoms like red, swollen, blistered, or peeling skin; red or irritated eyes; sores in your mouth, throat, nose, eyes, genitals, or skin; fever; chills; body aches; shortness of breath; or swollen glands, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only minor ones. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Fatigue or weakness.
Joint pain.
Decreased appetite.
Weight loss.
Hot flashes.
Diarrhea.
* Upset stomach.
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of high blood pressure: severe headache, dizziness, fainting, or changes in vision.
Signs of high blood sugar: confusion, drowsiness, excessive thirst or hunger, frequent urination, flushing, rapid breathing, or fruity-smelling breath.
Signs of high potassium levels: abnormal heartbeat, confusion, weakness, lightheadedness, dizziness, numbness or tingling, or shortness of breath.
Signs of low thyroid levels: constipation, sensitivity to cold, memory problems, mood changes, or abnormal burning, numbness, or tingling sensations.
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision.
Chest pain or pressure.
Shortness of breath.
Seizures.
Swelling in the arms or legs.
Bone pain.
Low white blood cell counts can increase the risk of infection. If you experience symptoms like fever, chills, or sore throat, contact your doctor immediately.
Severe and potentially life-threatening lung problems can occur. If you experience new or worsening lung or breathing problems, such as cough or shortness of breath, seek medical help right away.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions, can occur. These reactions can affect internal organs and be life-threatening. If you notice symptoms like red, swollen, blistered, or peeling skin; red or irritated eyes; sores in your mouth, throat, nose, eyes, genitals, or skin; fever; chills; body aches; shortness of breath; or swollen glands, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only minor ones. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Fatigue or weakness.
Joint pain.
Decreased appetite.
Weight loss.
Hot flashes.
Diarrhea.
* Upset stomach.
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- New or worsening high blood pressure (headache, dizziness, blurred vision)
- Seizures (loss of consciousness, convulsions, confusion)
- Rash (especially severe, widespread, or blistering)
- Chest pain, shortness of breath, numbness or weakness on one side of the body, sudden severe headache, problems with vision or speech (signs of heart attack or stroke)
- New or worsening bone pain, swelling, or deformity (signs of fracture)
- Severe fatigue
- Severe diarrhea
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in these situations, as it may harm an unborn baby or increase the risk of pregnancy loss. Discuss your situation with your doctor.
* Potential interactions with other medications or health conditions. Inform your doctor and pharmacist about all the medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure that it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in these situations, as it may harm an unborn baby or increase the risk of pregnancy loss. Discuss your situation with your doctor.
* Potential interactions with other medications or health conditions. Inform your doctor and pharmacist about all the medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure that it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
There is a risk of seizures associated with this medication, particularly if you have a history of certain brain blood vessel problems, take other medications that may increase the risk of seizures, or have previously experienced seizures, brain injury, stroke, or brain cancer. To minimize the risk of injury, avoid activities that could be hazardous if you were to lose consciousness. Consult your doctor for guidance.
This medication may increase your risk of falling, which can lead to serious complications such as fractures. Discuss your risk of falling and potential fractures with your doctor.
Regular blood pressure checks are crucial while taking this medication, as it may cause high blood pressure. Additionally, there is a risk of bleeding in the brain and blood vessel disease in the brain or heart, which can be life-threatening. If you have a history of high blood pressure, high blood sugar (diabetes), or high cholesterol or triglycerides, inform your doctor. If you have any questions or concerns, be sure to discuss them with your doctor.
This medication may also cause elevated cholesterol and triglyceride levels. Consult your doctor to discuss this potential risk. If you have diabetes, inform your doctor, as this medication may affect your blood sugar levels. Monitor your blood sugar levels as directed by your doctor.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
It is essential to note that this medication is present in semen. Do not donate semen while taking this medication and for 3 months after your last dose. This medication may also affect fertility. Discuss this potential risk with your doctor.
If your partner may become pregnant, use effective birth control while taking this medication and for 3 months after your last dose. If your partner becomes pregnant, notify your doctor immediately. If your partner is already pregnant, use a condom during sexual activity to minimize the risk of exposure.
There is a risk of seizures associated with this medication, particularly if you have a history of certain brain blood vessel problems, take other medications that may increase the risk of seizures, or have previously experienced seizures, brain injury, stroke, or brain cancer. To minimize the risk of injury, avoid activities that could be hazardous if you were to lose consciousness. Consult your doctor for guidance.
This medication may increase your risk of falling, which can lead to serious complications such as fractures. Discuss your risk of falling and potential fractures with your doctor.
Regular blood pressure checks are crucial while taking this medication, as it may cause high blood pressure. Additionally, there is a risk of bleeding in the brain and blood vessel disease in the brain or heart, which can be life-threatening. If you have a history of high blood pressure, high blood sugar (diabetes), or high cholesterol or triglycerides, inform your doctor. If you have any questions or concerns, be sure to discuss them with your doctor.
This medication may also cause elevated cholesterol and triglyceride levels. Consult your doctor to discuss this potential risk. If you have diabetes, inform your doctor, as this medication may affect your blood sugar levels. Monitor your blood sugar levels as directed by your doctor.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
It is essential to note that this medication is present in semen. Do not donate semen while taking this medication and for 3 months after your last dose. This medication may also affect fertility. Discuss this potential risk with your doctor.
If your partner may become pregnant, use effective birth control while taking this medication and for 3 months after your last dose. If your partner becomes pregnant, notify your doctor immediately. If your partner is already pregnant, use a condom during sexual activity to minimize the risk of exposure.
Overdose Information
Overdose Symptoms:
- Exaggerated known adverse reactions (e.g., seizures, rash, fatigue)
What to Do:
There is no specific antidote for apalutamide overdose. In the event of an overdose, discontinue Erleada and provide general supportive care, including monitoring for adverse reactions. Call 1-800-222-1222 (Poison Control Center).
Drug Interactions
Major Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort) - may decrease apalutamide exposure
- Strong CYP3A4 substrates with narrow therapeutic index (e.g., fentanyl, alfentanil, quinidine, cyclosporine, tacrolimus, sirolimus, ergot alkaloids, pimozide) - apalutamide is a strong CYP3A4 inducer
- CYP2C8 substrates with narrow therapeutic index (e.g., repaglinide) - apalutamide is a moderate CYP2C8 inducer
- CYP2C9 substrates with narrow therapeutic index (e.g., warfarin, phenytoin) - apalutamide is a moderate CYP2C9 inducer
- CYP2C19 substrates with narrow therapeutic index (e.g., S-mephenytoin, clopidogrel) - apalutamide is a moderate CYP2C19 inducer
- P-gp substrates with narrow therapeutic index (e.g., digoxin, dabigatran etexilate) - apalutamide is a moderate P-gp inducer
- BCRP substrates with narrow therapeutic index (e.g., rosuvastatin, sulfasalazine) - apalutamide is a moderate BCRP inducer
Moderate Interactions
- Moderate CYP3A4 inducers (e.g., bosentan, efavirenz) - may decrease apalutamide exposure
- Acid-reducing agents (e.g., PPIs, H2 blockers, antacids) - no clinically significant effect on apalutamide absorption
- Drugs that prolong QT interval (e.g., antiarrhythmics, antipsychotics) - monitor ECG and electrolytes due to potential for QT prolongation with apalutamide
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Serum testosterone
Rationale: To confirm castration levels (should be <50 ng/dL or <1.7 nmol/L) as apalutamide is used in castration-resistant or castration-sensitive settings.
Timing: Prior to initiation
PSA (Prostate-Specific Antigen)
Rationale: Baseline marker for disease activity and response to therapy.
Timing: Prior to initiation
Blood pressure
Rationale: Apalutamide can cause hypertension.
Timing: Prior to initiation
Cardiovascular risk factors
Rationale: Assess for pre-existing conditions that may increase risk of ischemic heart disease or stroke.
Timing: Prior to initiation
Seizure history
Rationale: Apalutamide can cause seizures; assess for predisposing factors.
Timing: Prior to initiation
Bone mineral density (BMD)
Rationale: Androgen deprivation therapy (ADT) and apalutamide can increase fracture risk.
Timing: Prior to initiation (consider DEXA scan)
Routine Monitoring
PSA (Prostate-Specific Antigen)
Frequency: Periodically (e.g., every 3 months or as clinically indicated)
Target: Decrease from baseline, ideally undetectable
Action Threshold: Rising PSA may indicate disease progression
Serum testosterone
Frequency: Periodically (e.g., every 3 months or as clinically indicated)
Target: <50 ng/dL or <1.7 nmol/L (castration level)
Action Threshold: Rising testosterone may indicate inadequate castration or non-compliance with ADT
Blood pressure
Frequency: Regularly (e.g., weekly for first few months, then monthly)
Target: Within normal limits (e.g., <140/90 mmHg)
Action Threshold: Sustained elevation requiring antihypertensive therapy or dose modification
Signs/symptoms of seizures
Frequency: Ongoing clinical monitoring
Target: Absence of seizures
Action Threshold: Occurrence of seizure requires dose interruption or discontinuation
Signs/symptoms of ischemic heart disease or stroke
Frequency: Ongoing clinical monitoring
Target: Absence of events
Action Threshold: Occurrence of event requires medical management and consideration of treatment interruption
Signs/symptoms of falls/fractures
Frequency: Ongoing clinical monitoring
Target: Absence of events
Action Threshold: Occurrence of event requires medical management
Skin rash
Frequency: Ongoing clinical monitoring
Target: Absence of severe rash
Action Threshold: Severe rash (e.g., Grade 3 or 4) requires dose interruption or discontinuation
Symptom Monitoring
- Fatigue
- Rash (especially severe or widespread)
- Arthralgia (joint pain)
- Diarrhea
- Hypertension (headache, dizziness, blurred vision)
- Hot flush
- Falls
- Fractures (new pain, swelling, deformity)
- Seizures (loss of consciousness, convulsions, confusion)
- Chest pain, shortness of breath, weakness on one side of body, slurred speech (signs of cardiac/cerebrovascular events)
Special Patient Groups
Pregnancy
Contraindicated in pregnant women. Apalutamide can cause fetal harm and loss of pregnancy. Based on animal studies and its mechanism of action, apalutamide can cause adverse developmental effects.
Trimester-Specific Risks:
First Trimester:
High risk of fetal harm/loss
Second Trimester:
High risk of fetal harm/loss
Third Trimester:
High risk of fetal harm/loss
Lactation
Not recommended during lactation. It is unknown if apalutamide or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, women should not breastfeed during treatment with Erleada and for 2 days after the last dose.
Infant Risk:
High risk (potential for serious adverse reactions)
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Not indicated for use in pediatric patients.
Geriatric Use
No dose adjustment is required based on age. Of the total number of patients in clinical studies, 74% were 65 years and over, and 32% were 75 years and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. However, a higher incidence of falls and fractures was observed in patients âĨ75 years of age compared to younger patients.
Clinical Information
Clinical Pearls
- Apalutamide is an oral androgen receptor inhibitor used in both non-metastatic and metastatic castration-resistant prostate cancer, and metastatic castration-sensitive prostate cancer.
- Patients must continue androgen deprivation therapy (ADT) concurrently with apalutamide.
- Counsel patients on the risk of seizures, falls, and fractures. Monitor for these events.
- Skin rash is a common side effect; manage symptomatically or with dose interruption/reduction if severe.
- Apalutamide is a strong inducer of several CYP enzymes and transporters, leading to numerous potential drug interactions. Review concomitant medications carefully.
- Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose.
Alternative Therapies
- Enzalutamide (Xtandi)
- Darolutamide (Nubeqa)
- Abiraterone acetate (Zytiga) + Prednisone
- Docetaxel (chemotherapy)
- Cabazitaxel (chemotherapy)
- Radium-223 dichloride (Xofigo)
- Sipuleucel-T (Provenge)
Cost & Coverage
Average Cost:
$12,000 - $15,000 per 30 tablets
Insurance Coverage:
Specialty Tier (Tier 4 or 5) - requires prior authorization and may have high co-pays/coinsurance
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.