WARNINGS
What are the possible side effects of ERLEADA?
ERLEADA may cause serious side effects including:
Heart disease, stroke, or mini-stroke. Bleeding in the brain or blockage of the arteries in the heart or in part of the brain have happened in some people during treatment with ERLEADA and can lead to death. Your healthcare provider will monitor you for signs and symptoms of heart or brain problems during your treatment with ERLEADA. Call your healthcare provider or get medical help right away if you get:
chest pain or discomfort at rest or with activity
shortness of breath
numbness or weakness of the face, arm, or leg, especially on one side of the body
trouble talking or understanding
trouble seeing in one or both eyes
dizziness, loss of balance or coordination, or trouble walking
Fractures and falls. ERLEADA treatment can cause bones and muscles to weaken and may increase your risk for falls and fractures. Falls and fractures have happened in people during treatment with ERLEADA. Your healthcare provider will monitor your risks for falls and fractures during treatment with ERLEADA.
Seizure. Treatment with ERLEADA may increase your risk of having a seizure. You should avoid activities where a sudden loss of consciousness could cause serious harm to yourself or others. Tell your healthcare provider right away if you have a loss of consciousness or seizure. Your healthcare provider will stop ERLEADA if you have a seizure during treatment.
Severe skin reactions. Treatment with ERLEADA may cause severe skin reactions that can lead to death or be life-threatening. Stop taking ERLEADA and tell your healthcare provider or get medical help right away if you develop any of these signs or symptoms of a severe skin reaction:
severe rash or rash that continues to get worse
fever or flu-like symptoms
swollen lymph nodes
blisters or sores in the mouth, throat, nose, eyes, or genital area
blistering or peeling of the skin
Lung problems. Treatment with ERLEADA may cause inflammation of the lungs that can lead to death or be life-threatening. Stop taking ERLEADA and tell your healthcare provider or get medical help right away if you develop any new or worsening symptoms of lung problems, including:
shortness of breath
cough
fever
USES
What is ERLEADA?
ERLEADA is a prescription medicine used for the treatment of prostate cancer:
that has spread to other parts of the body and still responds to a medical or surgical treatment that lowers testosterone, OR
that has not spread to other parts of the body and no longer responds to a medical or surgical treatment that lowers testosterone.
It is not known if ERLEADA is safe and effective in females.
It is not known if ERLEADA is safe and effective in children.
HOW TO USE
How should I take ERLEADA?
Take ERLEADA exactly as your healthcare provider tells you.
Do not stop taking your prescribed dose of ERLEADA without talking with your healthcare provider first.
Take your prescribed dose of ERLEADA 1 time a day, at the same time each day.
Take ERLEADA with or without food.
Swallow ERLEADA tablets whole. Do not crush or split the tablets.
If you cannot swallow ERLEADA tablets whole or if you have a feeding tube, see the “Instructions for Use” for detailed instructions on how to prepare and take a dose of ERLEADA. ERLEADA comes in 2 different strengths (60 mg and 240 mg). Follow the instructions for your prescribed strength of ERLEADA.
If you miss a dose of ERLEADA, take your normal dose as soon as possible on the same day. Return to your normal schedule on the following day. You should not take extra tablets to make up the missed dose.
You should start or continue a gonadotropin-releasing hormone (GnRH) analog therapy during your treatment with ERLEADA unless you have had a surgery to lower the amount of testosterone in your body (surgical castration).
If you take too much ERLEADA, call your healthcare provider or go to the nearest hospital emergency room.
What are the possible side effects of ERLEADA?
ERLEADA may cause serious side effects including:
Heart disease, stroke, or mini-stroke. Bleeding in the brain or blockage of the arteries in the heart or in part of the brain have happened in some people during treatment with ERLEADA and can lead to death. Your healthcare provider will monitor you for signs and symptoms of heart or brain problems during your treatment with ERLEADA. Call your healthcare provider or get medical help right away if you get:
chest pain or discomfort at rest or with activity
shortness of breath
numbness or weakness of the face, arm, or leg, especially on one side of the body
trouble talking or understanding
trouble seeing in one or both eyes
dizziness, loss of balance or coordination, or trouble walking
Fractures and falls. ERLEADA treatment can cause bones and muscles to weaken and may increase your risk for falls and fractures. Falls and fractures have happened in people during treatment with ERLEADA. Your healthcare provider will monitor your risks for falls and fractures during treatment with ERLEADA.
Seizure. Treatment with ERLEADA may increase your risk of having a seizure. You should avoid activities where a sudden loss of consciousness could cause serious harm to yourself or others. Tell your healthcare provider right away if you have a loss of consciousness or seizure. Your healthcare provider will stop ERLEADA if you have a seizure during treatment.
Severe skin reactions. Treatment with ERLEADA may cause severe skin reactions that can lead to death or be life-threatening. Stop taking ERLEADA and tell your healthcare provider or get medical help right away if you develop any of these signs or symptoms of a severe skin reaction:
severe rash or rash that continues to get worse
fever or flu-like symptoms
swollen lymph nodes
blisters or sores in the mouth, throat, nose, eyes, or genital area
blistering or peeling of the skin
Lung problems. Treatment with ERLEADA may cause inflammation of the lungs that can lead to death or be life-threatening. Stop taking ERLEADA and tell your healthcare provider or get medical help right away if you develop any new or worsening symptoms of lung problems, including:
shortness of breath
cough
fever
The most common side effects of ERLEADA include:
feeling very tired
weight loss
joint pain
high blood pressure
rash. Tell your healthcare provider if you get a rash.
hot flash
decreased appetite
diarrhea
fall
fracture
Your healthcare provider may reduce your dose, temporarily stop, or permanently stop treatment with ERLEADA if you have certain side effects.
ERLEADA may cause fertility problems in males, which may affect the ability to father children. Talk to your healthcare provider if you have concerns about fertility. Do not donate sperm during treatment with ERLEADA and for 3 months after the last dose of ERLEADA.
Tell your healthcare provider if you have any side effect that bothers you or that does not go away.
These are not all the possible side effects of ERLEADA.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088
Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use ERLEADA fora condition for which it was not prescribed. Do not give ERLEADA to other people, even if they have the same symptoms that you have. It may harm them. You can ask your healthcare provider or pharmacist for information about ERLEADA that is written for health professionals.
What are the ingredients in ERLEADA?
Active ingredient: apalutamide
Inactive ingredients: 240 mg film-coated tablets: colloidal anhydrous silica, croscarmellose sodium, hydroxypropyl methylcellulose-acetate succinate, silicified microcrystalline cellulose, and magnesium stearate. The coating contains glyceryl monocaprylocaprate, iron oxide black, polyvinyl alcohol, talc, titanium dioxide, and vinyl alcohol grafted copolymer. 60 mg film-coated tablets: colloidal anhydrous silica, croscarmellose sodium, hydroxypropyl ethylcellulose-acetate succinate, magnesium stearate, microcrystalline cellulose, and silicified microcrystalline cellulose. The coating contains iron oxide black, ironoxide yellow, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.
OVERDOSE
If you take too much ERLEADA, call your healthcare provider or go to the nearest hospital emergency room.
MISSED DOSE
If you miss a dose of ERLEADA, take your normal dose as soon as possible on the same day. Return to your normal schedule on the following day. You should not take extra tablets to make up the missed dose.
STORAGE
How should I store ERLEADA?
Store ERLEADA at room temperature between 68-degrees F to 77-degrees F (20-degrees C to 25-degrees C).
ERLEADA comes in a child-resistant bottle.
Store ERLEADA in the original package to protect from light and moisture.
The bottle of ERLEADA contains a desiccant packet to help keep your medicine dry (protect it from moisture). Do not throw away (discard) the desiccant.
Keep ERLEADA and all medicines out of the reach of children.
NOTES
Medication Guide: revision date 08/2024
Prescribing Information: revision date 08/2024
1.) Effect of Other Drugs on ERLEADA
Strong CYP2C8 or CYP3A4 Inhibitors
Co-administration of a strong CYP2C8 or CYP3A4 inhibitor is predicted to increase the steady-state exposure of the active moieties (sum of unbound apalutamide plus the potency-adjusted unbound N-desmethyl-apalutamide). No initial dose adjustment is necessary however, reduce the ERLEADA dose based on tolerability [see the section USE above]. Mild or moderate inhibitors of CYP2C8 or CYP3A4 are not expected to affect the exposure of apalutamide.
2.) Effect of ERLEADA on Other Drugs
CYP3A4, CYP2C9, CYP2C19 and UGT Substrates
ERLEADA is a strong inducer of CYP3A4 and CYP2C19, and a weak inducer of CYP2C9 in humans. Concomitant use of ERLEADA with medications that are primarily metabolized by CYP3A4, CYP2C19, or CYP2C9 can result in lower exposure to these medications. Substitution for these medications is recommended when possible or evaluate for loss of activity if medication is continued. Concomitant administration of ERLEADA with medications that are substrates of UDP-glucuronosyl transferase (UGT) can result in decreased exposure. Use caution if substrates of UGT must be co-administered with ERLEADA and evaluate for loss of activity.
P-gp, BCRP or OATP1B1 Substrates
Apalutamide was shown to be a weak inducer of P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and organic anion transporting polypeptide 1B1 (OATP1B1) clinically. At steady-state, apalutamide reduced the plasma exposure to fexofenadine (a P-gp substrate) and rosuvastatin (a BCRP/OATP1B1 substrate). Concomitant use of ERLEADA with medications that are substrates of P-gp, BCRP, or OATP1B1 can result in lower exposure of these medications. Use caution if substrates of P-gp, BCRP or OATP1B1 must be co-administered with ERLEADA and evaluate for loss of activity if medication is continued.
Before taking ERLEADA, tell your healthcare provider about all your medical conditions, including if you:
have a history of heart disease
have high blood pressure
have diabetes
have abnormal amounts of fat or cholesterol in your blood (dyslipidemia)
have a history of seizures, brain injury, stroke, or brain tumors
are pregnant or plan to become pregnant. ERLEADA can cause harm to your unborn baby and loss of pregnancy (miscarriage).
have a partner who is pregnant or may become pregnant.
Males who have female partners who are able to become pregnant should use effective birth control (contraception) during reatment and for 3 months after the last dose of ERLEADA.
Males should use a condom during sex with a pregnant female.
Talk with your healthcare provider if you have questions about birth control.
are breastfeeding or plan to breastfeed. It is not known if ERLEADA passes into breast milk.
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. ERLEADA can interact with many other medicines.
You should not start or stop any medicine before you talk with the healthcare provider that prescribed ERLEADA.
Know the medicines you take. Keep a list of them with you to show to your healthcare provider and pharmacist when you get a new medicine.
