Apalutamide
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From MedlinePlus, U.S. National Library of Medicine
Dosing in kidney impairment
This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.
Dosing in liver impairment
Recommended Dosage in Patients with Severe Hepatic Impairment The recommended dosage of ERLEADA for patients with severe hepatic impairment (Child-Pugh Class C) is 120 mg orally once daily [see Use in Specific Populations and Clinical Pharmacology ] .
Preparation and administration
Alternate Methods of Administration Disperse Tablet(s) in Water and Administer with Orange Juice, Applesauce, or Additional Water For patients who cannot swallow tablets whole, the recommended dose of ERLEADA tablet(s) can be dispersed in non-carbonated water and then administered with either orange juice, applesauce, or additional water as follows: Place the entire prescribed dose of ERLEADA tablet(s) in a cup.
Do not crush or split the tablet(s). For one 240 mg tablet: Add about 2 teaspoons (10 mL) of non-carbonated water to make sure that the tablet is completely immersed in water. For 60 mg tablets (prescribed dose of 240 mg, 180 mg, or 120 mg): Add about 4 teaspoons (20 mL) of non-carbonated water to make sure that the tablets are completely immersed in water.
Wait 2 minutes until the tablet(s) are broken up and spread out, then stir the mixture. Add 2 tablespoons (30 mL) of either orange juice, applesauce, or additional water and stir the mixture. Swallow the mixture immediately. Rinse the cup with enough water to make sure the whole dose is taken and drink it immediately. Do not store ERLEADA that is mixed with non-carbonated water, orange juice, or applesauce for later use.
Administer Tablet(s) Through a Feeding Tube ERLEADA tablet(s) can be administered through a feeding tube 8 French or greater as follows: For one 240 mg tablet: Place the tablet in the barrel of the syringe (use at least a 20 mL syringe) and draw up 10 mL of non-carbonated water into the syringe. For 60 mg tablets (prescribed dose of 240 mg, 180 mg, or 120 mg): Place the entire prescribed dose of ERLEADA tablets in the barrel of the syringe (use at least a 50 mL syringe) and draw up 20 mL of non-carbonated water into the syringe.
Wait 10 minutes and then shake vigorously to disperse contents completely. Administer immediately through the feeding tube. Refill the syringe with non-carbonated water and administer. Repeat until no tablet residue is left in the syringe or feeding tube.
Drug interactions
Check apalutamide against a medication listLabel text (4 paragraphs)
Concomitant use with medications that are sensitive substrates of CYP3A4, CYP2C19, CYP2C9, UGT, P-gp, BCRP, or OATP1B1 may result in loss of activity of these medications. ( 7.2 )
7.1 Effect of Other Drugs on ERLEADA Strong CYP2C8 or CYP3A4 Inhibitors Reduce the ERLEADA dose as recommended for adverse reactions [see Dosage and Administration (2.2) ] . 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).
7.2 Effect of ERLEADA on Other Drugs Substrates of CYP3A4, CYP2C9, CYP2C19, P-gp, BCRP, or OATP1B1 Refer to the Prescribing Information for these substrates. Consider alternative agents when possible or evaluate for loss of activity of the substrate if concomitant use cannot be avoided. Apalutamide is a strong inducer of CYP3A4 and CYP2C19, a weak inducer of CYP2C9, and an inducer of P-gp, BCRP, and OATP1B1. Apalutamide decreases exposure of substrates of CYP3A4, CYP2C19, CYP2C9, P-gp, BCRP, or OATP1B1 [see Clinical Pharmacology (12.3) ] , which may decrease the effectiveness of these substrates.
7.3 Laboratory Test Interference ERLEADA can interfere with certain digoxin immunoassays (e.g., Chemiluminescent Microparticle Immunoassays), resulting in falsely elevated digoxin plasma concentration results. Notify the laboratory conducting the digoxin plasma concentration assay to use an appropriate method in patients receiving ERLEADA and digoxin [see Warnings and Precautions (5.8) ] .
Contraindications
None. ( 4 ) None.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary The safety and efficacy of ERLEADA have not been established in females. Based on findings from animals and its mechanism of action, ERLEADA can cause fetal harm and loss of pregnancy when administered to a pregnant female [see Clinical Pharmacology (12.1) ] . There are no available data on ERLEADA use in pregnant women to inform a drug-associated risk. In an animal reproduction study, oral administration of apalutamide to pregnant rats during and after organogenesis resulted in fetal abnormalities and embryo-fetal lethality at maternal exposures ≥ 2 times the human clinical exposure (AUC) at the recommended dose (see Data ) .
Data Animal Data In a pilot embryo-fetal developmental toxicity study in rats, apalutamide caused developmental toxicity when administered at oral doses of 25, 50 or 100 mg/kg/day throughout and after the period of organogenesis (gestational days 6–20). Findings included embryo-fetal lethality (resorptions) at doses ≥50 mg/kg/day, decreased fetal anogenital distance, misshapen pituitary gland, and skeletal variations (unossified phalanges, supernumerary short thoracolumbar rib(s), and small, incomplete ossification, and/or misshapen hyoid bone) at ≥25 mg/kg/day. A dose of 100 mg/kg/day caused maternal toxicity.
The doses tested in rats resulted in systemic exposures (AUC) approximately 2, 4 and 6 times, respectively, the AUC in patients.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
Not the price at the counterThese are not what a patient pays at the pharmacy counter. They are what pharmacies, health plans, and government buyers pay, before manufacturer rebates. A patient's cost depends on their insurance (copay, coinsurance, or deductible) or the pharmacy's cash price.