Apalutamide
Indications
Apalutamide is used for:
Prostate Cancer
Adult Dose
Prostate Cancer
Indicated for nonmetastatic, castration-resistant prostate cancer (NM-CRPC)
240 mg (ie, four 60-mg tablets) PO qDay
Child Dose
Renal Dose
Administration
May take with or without food
Contra Indications
Pregnancy
Precautions
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
Pregnancy-Lactation
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
Interactions
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)
Adverse Effects
Side effects of Apalutamide :
>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%)
Mechanism of Action
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