Erleada

/ Janssen

The recommended dose is 240 mg (four 60 mg tablets) administered orally once daily. Swallow the tablets whole. The drug can be taken with or without food.
Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.
Dose Modification: If a patient experiences a greater than or equal to Grade 3 toxicity or an intolerable side effect, hold dosing until symptoms improve to less than or equal to Grade 1 or original grade, then resume at the same dose or a reduced dose (180 mg or 120 mg), if warranted.

Treatment of patients with non-metastatic, castration-resistant prostate cancer (NM-CRPC).

Hypersensitivity to the active substance or to any of the excipients.
Women who are or may become pregnant.

Falls and Fractures: Falls and fractures occurred in patients receiving Apalutamide. Evaluate patients for fracture and fall risk. Patients at risk for fractures should be monitored according to established treatment guidelines and consider use of bone targeted agents.
Seizure: Seizure occurred in patients receiving Apalutamide. Permanently discontinuation in necessary in patients who develop a seizure during treatment. It is unknown whether anti-epileptic medications will prevent seizures with Apalutamide.
See prescribing information for full details.

Hypothyroidism, pruritus, ischemic heart, heart failure.
See prescribing information for full details.

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. Mild or moderate inhibitors of CYP2C8 or CYP3A4 are not expected to affect the exposure of apalutamide.
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.

Pregnancy: The drug can cause fetal harm and potential loss of pregnancy.
Lactation: ERLEADA is not indicated for use in females. There are no data on the presence of apalutamide or its metabolites in human milk, the effect on the breastfed child, or the effect on milk production.
See prescribing information for full details.

There is no known specific antidote for apalutamide overdose. In the event of an overdose, the drug should be discontinued and general supportive measures until clinical toxicity has been diminished or resolved.