a-pa-LOO-ta-mide

• Non-metastatic castration-resistant prostate cancer.
• Metastatic castration-sensitive prostate cancer.

• Acts as an androgen receptor inhibitor, preventing the binding of androgen; also inhibits androgen nuclear translocation and DNA interaction.
• Decreases proliferation and induces cell death of prostate cancer cells.

• Decreased growth and spread of prostate cancer.

Absorption: Completely absorbed (100%) following oral administration.

Distribution: Extensively distributed to tissues.

Protein Binding: Apalutamide — 96%; N-desmethyl apalutamide — 95%.

Metabolism/Excretion: Metabolized by the CYP2C8 and CYP3A4 isoenzymes in the liver to an active metabolite (N-desmethyl apalutamide). Primarily excreted in urine (65%) and 24% excreted in feces, with only minimal amounts being excreted as unchanged drug.

Half-life: 3 days.

Contraindicated in:

• OB: Lactation: Not indicated for use in females.

Use Cautiously in:

• History of seizures, underlying brain pathology, cerebrovascular accident, transient ischemic attack, brain metastases or brain arteriovenous malformation (may ↑ risk of seizures)
• Ischemic heart disease, HF, stroke, or TIA
• Rep: Men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: MI, hypertension, peripheral edema, unstable angina.

Derm: hot flush, rash, pruritus.

Endo: hyperglycemia, hypothyroidism.

F and E: hyperkalemia.

GI: ↓appetite, diarrhea, nausea.

GU: ↓fertility (males).

Hemat: anemia, leukopenia, lymphopenia.

Metab: ↓weight, hypercholesterolemia, hypertriglyceridemia.

MS: arthralgia, fracture.

Neuro: SEIZURES, falls, fatigue.

Drug-Drug:

• Strong CYP2C8 and CYP3A4 inhibitors, including gemfibrozil, may ↑ levels and risk of toxicity; may need to ↓ apalutamide dose.
• May ↓ levels of CYP3A4, CYP2C9, and CYP2C19 substrates; avoid concurrent use, when possible.
• May ↓ levels of fexofenadine and rosuvastatin.
• Drugs that ↓ seizure threshold may ↑ risk of seizures.

• PO (Adults): 240 mg once daily.

• Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.
• PO: Administer 4 tablets once daily without regard to food. Swallow tablets whole; do not crush, break, dissolve, or chew.
  • For patients with difficulty swallowing, mix tablets in 4 oz of applesauce by stirring; do not crush tablets. Wait 15 min; stir again. Wait another 15 min; stir mixture until tablets are well mixed with no chunks remaining. Use a spoon; have patient consume mixture right away (do not store). Rinse container with 2 oz of water and drink immediately; repeat rinse a second time to ensure entire dose is taken.
  • If Grade 3 toxicity or intolerable side effects occur, withhold dose for 1 wk or until symptoms improve to Grade 1, then resume at same or reduced dose (180 mg or 120 mg).

Erleada

Therapeutic Classification: antineoplastics

Pharmacologic Classification: androgen receptor inhibitors

• Tablets: 60 mg;

(plasma concentrations)

• Monitor for seizures. Implement seizure precautions. If a seizure occurs during therapy, permanently discontinue apalutamide therapy.
• Assess for falls risk. Institute prevention if indicated.

• May cause ↑ TSH levels.

• Risk for falls (Adverse Reactions, Patient/Family Teaching).

• Instruct patient to take apalutamide as directed at the same time each day. Take missed doses as soon as remembered within the same day. If a whole day is missed, omit dose and take next day's scheduled dose; do not double doses. Advise patient not to interrupt, modify dose, or stop taking apalutamide without consulting health care professional. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• May cause seizures, falls, and fractures. Caution patient to avoid driving and other activities requiring alertness until response to medication is known. Notify health care professional immediately if seizure occurs.
• Advise patient to notify health care professional if rash occurs.
• Advise patient to notify health care professional and go to nearest emergency room if signs and symptoms of cardiac problems (chest pain or discomfort at rest or with activity, shortness of breath) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other Rx, OTC, or herbal products.
• Rep: Caution patients that apalutamide is teratogenic and is not approved for use with females. Advise male patients with female partners of reproductive potential to use effective contraception during and for 3 months after last dose of therapy. May impair fertility in males of reproductive potential.

• Decreased growth and spread of prostate cancer.

NDC Code^*

• 59676- Janssen Products, LP
  • 59676-600- ERLEADA
    • 59676-600-12- 120 TABLET, FILM COATED in 1 BOTTLE (59676-600-12)

• 59676- Janssen Products, LP
  • 59676-600- ERLEADA
    • 59676-600-56- 2 BLISTER PACK in 1 CARTON (59676-600-56) > 28 TABLET, FILM COATED in 1 BLISTER PACK

• 59676- Janssen Products, LP
  • 59676-600- ERLEADA
    • 59676-600-99- 120 TABLET, FILM COATED in 1 BOTTLE (59676-600-99)