apalutamide

General

Pronunciation:
a-pa-loo-ta-mide

Trade Name(s)

  • Erleada

Ther. Class.
antineoplastics

Pharm. Class.
androgen receptor inhibitors

Indications

Non-metastatic castration-resistant prostate cancer.

Action

  • 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.

Therapeutic Effect(s):

Decreased growth and spread of prostate cancer.

Pharmacokinetics

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

Distribution: Extensively distributed to tissues.

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

Metabolism and 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.

TIME/ACTION PROFILE (plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown2 hrunknown

Contraindication/Precautions

Contraindicated in:

  • OB: Avoid use in pregnancy (may cause fetal harm).

Use Cautiously in:

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

Adverse Reactions/Side Effects

CNS: SEIZURES, falls, fatigue

CV: hypertension, peripheral edema

Derm: hot flush, rash, pruritus

Endo: hyperglycemia, hypothyroidism

F and E: hyperkalemia

GI: ↓ appetite, diarrhea, nausea

GU: ↓ fertility (males)

Hemat: anemia, leukopenia, lymphopenia

Metabolic: ↓ weight, hypercholesterolemia, hypertriglyceridemia

MS: arthralgia, fracture

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

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.

Route/Dosage

PO (Adults) 240 mg once daily.

Availability

Tablets: 60 mg

Assessment

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

Lab Test Considerations:

May cause ↑ TSH levels.

Potential Diagnoses

Implementation

  • 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.
    • 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).

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.
  • 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. 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.

Evaluation/Desired Outcomes

Decreased growth and spread of prostate cancer.

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