(en-za-loo-ta-mide) ,


(trade name)


Therapeutic: antineoplastics
Pharmacologic: androgen receptor inhibitors
Pregnancy Category: X


Management of metastatic castration-resistant prostate cancer in patients previously treated with docetaxel.


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.


Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Protein Binding: Enalutamide—97–98%; N-desmethylenzalutamide—95%.
Metabolism and Excretion: Extensively metabolized by the liver (CYP2C8 and CYP3A4 enzyme systems); one metabolite (N-desmethylenzalutamide) has antineoplastic activity. Metabolites are primarily renally excreted, only minimal amounts as unchanged drug.
Half-life: Enalutamide—5.8 days; N-desmethylenzalutamide—7.8–8.6 days.

Time/action profile (improved survival)

PO3 mounknownunknown


Contraindicated in: Pregnancy (may cause fetal harm) or women with child-bearing potential.
Use Cautiously in: History of seizures, underlying brain pathology, cerebrovascular accident, transient ischemic attack (within 12 mo), brain metastases or brain arteriovenous malformation (may increase risk of seizures); Geriatric: elderly may be more sensitive to drug effects; Pediatric: Safe and effective in children has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • seizures (life-threatening)
  • spinal cord compression/cauda equina syndrome (life-threatening)
  • headache (most frequent)
  • weakness (most frequent)
  • anxiety
  • dizziness
  • hallucinations
  • insomnia
  • mental impairment disorders

Ear, Eye, Nose, Throat

  • epistaxis


  • peripheral edema (most frequent)
  • hypertension


  • diarrhea (most frequent)


  • hematuria
  • urinary frequency


  • hot flush (most frequent)
  • dry skin
  • pruritus


  • arthralgia (most frequent)
  • musculoskeletal pain (most frequent)
  • muscular stiffness
  • musular weakness


  • hypoesthesia
  • paresthesia


Drug-Drug interaction

Strong inhibitors of the CYP2C8 enzyme system (including gemfibrozil ) may ↑ blood levels and the risk of adverse reactions/toxicity and should be avoided; if concurrent administration is necessary, dose of enzalutamide should be ↓.Strong/moderate inducers of the CYP3A4 or CYP2C8 enzyme systems (including rifampin ) may alter levels and response and should be avoided.Substrates of the CYP3A4, CYP2C9 (including warfarin) and CYP2C19 systems that have narrow therapeutic indexes should be avoided as their levels and activity may be decreased; careful monitoring is recommended.Concurrent use of drugs that ↓ seizure threshold may ↑ risk of seizures.


Oral (Adults) 160 mg (four 40-mg capsules) once daily; if ≥Grade 3 toxicity or intolerable adverse reactions occur, discontinue for 1 wk and resume at the same or lower dose (80 or 120 mg). Concurrent use of strong CYP2C8 inhibitors—80 mg once daily.


Capsules: 40 mg

Nursing implications

Nursing assessment

  • Monitor for seizures. Implement seizure precautions.
  • Lab Test Considerations: May cause hematuria.

Potential Nursing Diagnoses

Activity intolerance


  • Oral: Administer 4 capsules once daily without regard to food. Swallow capsules whole; do not open, dissolve, or chew.
    • If ≥Grade 3 toxicity or intolerable side effects occur, withhold dose for 1 wk or until symptoms improve to <Grade 2, then resume at same or reduced dose (120 mg or 80 mg).

Patient/Family Teaching

  • Instruct patient to take enzalutamide 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 enzalutamide without consulting health care professional.
  • May cause seizures, dizziness, mental impairment, paresthesia, hypoesthesia, falls, and hallucinations. Caution patient to avoid driving and other activities requiring alertness until response to medication is known. Notify health care professional immediately if loss of consciousness or seizure occurs.
  • Inform patient of common side effects associated with enzalutamide: asthenia/fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper and lower respiratory infection, muscular weakness, dizziness, insomnia, spinal cord compression, cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension. Notify health care professional if falls or problems thinking clearly, or if side effects are bothersome.
  • Caution patients that enzalutamide is teratogenic. Advise patient to avoid pregnancy and breast feeding during and for 3 mo following completion of therapy. Male patients should use a condom if having sex with a pregnant woman, and a condom and another effective method of birth control should be used if having sex with a woman of child-bearing potential.

Evaluation/Desired Outcomes

  • Decreased growth and spread of prostate cancer.
References in periodicals archive ?
Sawyers was instrumental in the discovery and development of leading drugs including imatinib for chronic myelogenous leukemia and enzalutamide and ARN-509 for castration-resistant prostate cancer.
The All Wales Medicines Strategy Group (AWMSG) has approved the use of Enzalutamide, also known as Xtandi, to help prolong the lives of prostate cancer patients who have become resistant to their first hormone treatment.
Enzalutamide will help patients with metastatic castration-resistant prostate cancer (mCRPC) who still show signs of the condition after going through androgen deprivation therapy.
We have summarized the Systemic Therapy in Advanced or Metastatic Prostate Cancer: Evaluation of Drug Efficacy--Androgen Suppression-Based Therapy Alone or Combined With Zoledronic Acid, Docetaxel, Prednisolone, Celecoxib, Abiraterone, Enzalutamide and/or Radiotherapy in Treating Patients With Locally Advanced or Metastatic Prostate Cancer (STAMPEDE) and Phase III Randomized Study of Adjuvant Radiotherapy With Versus Without Concurrent Goserelin in Patients Who Have Undergone Surgery for Recurrent or Refractory Prostate Cancer CGETUG) trials providing further evidence of the benefit of early docetaxel added to hormone therapy in advanced prostate cancer.
AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer, N Engl J Med 2014; 371 :1028-1038
Enzalutamide prolongs life by at least five months in patients who have run out of treatment options - with some surviving much longer.
STOCKTON grandfather Peter Smith is having to fund his own PS3,000 a month treatment for prostate cancer because NICE and NHS England will not provide the required funding for a new drug called enzalutamide (Gazette, 11.
For me to get a drug called Enzalutamide I'm going to have to go on my knees and beg Poots for it.
Mikis Euripides, director of policy and strategy at the charity, said: "It's a kick in the teeth for men facing their last months, especially as other new treatments, such as enzalutamide, have restrictions on use in England and Wales.
As a first action, let's try to reverse the recent illogical decision by the National Institute for Health and Care Excellence (NICE) to restrict access to a life-extending prostate cancer drug enzalutamide.
As a first action, let's try to reverse the recent illogical decision by the National Institute for Health and Care Excellence to restrict access to a life-extending prostate cancer drug enzalutamide.
Other new antineoplastics are the antiandrogen enzalutamide (Xtandi; prostate cancer but could be used for other cancers), the proteasome inhibitor carfilzomib (Kyprolis; multiple myeloma), and the protein synthesis inhibitor omacetaxine (Synribo; leukemia).