Prostaxen 60

Prostate Cancer

May take with or without food

Prostate Cancer Indicated for nonmetastatic, castration-resistant prostate cancer (NM-CRPC) 240 mg (ie, four 60-mg tablets) PO qDay

Pregnancy

Androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR; inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription Administration caused decreased tumor cell proliferation and increased apoptosis, leading to decreased tumor volume in mouse xenograft models of prostate cancer

Falls and fractures reported; evaluate patient for risk; monitor and manage patients at risk for fractures according to established treatment guidelines and consider use of bone-targeted agents Seizures reported; permanently discontinue if a seizure occurs during treatment; unknown whether anticonvulsants will prevent seizures with apalutamide Advise patients of risk of developing a seizure while on therapy and harm, to themselves or others, that could occur from sudden loss of memory while engaging in activities

>10% All Grades Hypercholesterolemia, nonfasting (76%) Anemia (70%) Hyperglycemia (70%) Hypertriglyceridemia, nonfasting (67%) Leukopenia (47%) Lymphopenia (41%) Fatigue (39%) Hyperkalemia (32%) Hypertension (25%) Rash (24%) Diarrhea (20%) Nausea (18%) Arthralgia (16%) Fall (16%) Weight decreased (16%) Hot flush (14%) Fracture (12%) Decreased appetite (12%) Peripheral edema (11%) >10% Grades 3-4 Hypertension (14%) 1-10% Hypothyroidism (8%) Pruritus (6.2%) Ischemic heart disease (3.7%) Heart failure (2.2%) 1-10% Grades 3-4 Rash (5%) Fracture (3%) Fall (2%) Hypertriglyceridemia, nonfasting (2%) Lymphopenia (2%) Hyperkalemia (2%) Hyperglycemia (2%) Fatigue (1%) Weight decreased (1%) Diarrhea (1%)

Pregnancy Contraindicated during pregnancy Based on its mechanism of action, the drug can cause fetal harm and potential loss of pregnancy There are no available data regarding use in pregnant women 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, may impair fertility in males of reproductive potential Lactation Not indicated for use in females

Coadministration with strong CYP2C8 or CYP3A4 inhibitors is predicted to increase the steady-state exposure of the active apalutamide moieties Apalutamide is a strong inducer of CYP3A4 and CYP2C19, a weak inducer of CYP2C9, and it induces UDP-glucuronosyltransferase (UGT)