apalutamide

Contraindicated in:

None.

Use Cautiously in:

History of seizures, underlying brain pathology, cerebrovascular accident, TIA, 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.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, peripheral edema, MI, unstable angina

Derm: hot flushing, rash, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), pruritus, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

Endo: hyperglycemia, hypothyroidism

F and E: hyperkalemia

GI: diarrhea, nausea

GU: ↓fertility (males)

Hemat: anemia, leukopenia, lymphopenia

Metab: ↓appetite, hypercholesterolemia, hypertriglyceridemia, weight loss

MS: arthralgia, fracture

Neuro: falls, fatigue, SEIZURES

Resp: INTERSTITIAL LUNG DISEASE/PNEUMONITIS

Interactions ⬆ ⬇

Drug-drug:

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

Availability ⬆ ⬇

Tablets: 60 mg; 240 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 240 mg once daily.

US Brand Names ⬆ ⬇

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 effects:

Decreased growth and spread of prostate cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: androgen receptor inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Completely absorbed 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.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of apalutamide to patient. 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.
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.
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 immediately of symptoms of lung problems (e.g., shortness of breath, cough, fever).
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.
Rep: May cause fetal harm. Caution patients that apalutamide is not approved for use by females. Advise male patients with female partners of reproductive potential to use effective contraception during and for 3 mo after last dose of therapy. May impair fertility in males of reproductive potential.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

11014- Catalent Pharma Solutions, LLC
- 11014-0330-
  - 11014-0330-2- 1 BAG in 1 DRUM (11014-0330-2) / 16608 TABLET, FILM COATED in 1 BAG

11014- Catalent Pharma Solutions LLC
- 11014-0485-
  - 11014-0485-2- 1 BAG in 1 DRUM (11014-0485-2) / 10000 TABLET, FILM COATED in 1 BAG

12578- Janssen Pharmaceutica NV
- 12578-621-
  - 12578-621-00- 25 kg in 1 DRUM (12578-621-00)

17314- Janssen Ortho LLC
- 17314-215-
  17314-215-00- 15202 TABLET, FILM COATED in 1 DRUM (17314-215-00)

54893- MSN Laboratories Private Limited
- 54893-0100-
  54893-0100-4- 20 kg in 1 DRUM (54893-0100-4)

54893- MSN Laboratories Private Limited
- 54893-0128-
  54893-0128-1- 50 kg in 1 DRUM (54893-0128-1)

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
- 59676-604- ERLEADA
  - 59676-604-14- 1 BLISTER PACK in 1 CARTON (59676-604-14) / 14 TABLET, FILM COATED in 1 BLISTER PACK

59676- Janssen Products, LP
- 59676-604- ERLEADA
  - 59676-604-30- 30 TABLET, FILM COATED in 1 BOTTLE (59676-604-30)

65267- Janssen Pharmaceutical Sciences Unlimited Company
- 65267-116-
  - 65267-116-00- 25 kg in 1 DRUM (65267-116-00)

68554- Hetero Labs Limited
- 68554-0127-
  68554-0127-1- 5.5 kg in 1 DRUM (68554-0127-1)

71796- Dr. Reddys Laboratories Limited
- 71796-019-
  71796-019-00- 1 kg in 1 DRUM (71796-019-00)

71796- Dr. Reddy's Laboratories Limited
- 71796-033-
  71796-033-00- 1 kg in 1 DRUM (71796-033-00)

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Indications ⬇

Contraind./Precautions ⬆ ⬇