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Nilutamide

Class: Antineoplastic Agents
- Antiandrogens
VA Class: AN900
Chemical Name: 5,5-Dimethyl-3-(4-nitro-3-[trifluoromethyl)phenyl]-2,4-imidazolidinedione
Molecular Formula: C12H10F3N3O4
CAS Number: 63612-50-0
Brands: Nilandron

Medically reviewed by Drugs.com on Oct 22, 2020. Written by ASHP.

Warning

    Interstitial Pneumonitis
  • Interstitial pneumonitis, rarely resulting in hospitalization or death, reported. Manifestations generally occurred within the first 3 months of therapy and resolved following discontinuance of the drug.

  • Immediately discontinue therapy if dyspnea or worsening of preexisting dyspnea occurs. (See Interstitial Pneumonitis under Cautions.)

Introduction

Antineoplastic agent; a nonsteroidal antiandrogen structurally and pharmacologically related to bicalutamide and flutamide.

Uses for Nilutamide

Prostate Cancer

Adjunct to orchiectomy in the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (stage D2).

Slows progression of the disease, relieves bone pain associated with metastatic disease, and improves overall survival rate after long-term therapy (8.5 years).

Nilutamide Dosage and Administration

General

  • Determine PSA concentrations periodically during therapy to monitor therapeutic response, including successful remission or possible progression of cancer.

  • If PSA concentrations increase substantially and consistently during therapy, evaluate the possibility of clinical progression.

Administration

Oral Administration

Administer orally once daily without regard to meals.

Dosage

Adults

Prostate Cancer
Oral

300 mg once daily for 30 days, followed by 150 mg given once daily thereafter. For maximum benefit, initiate nilutamide on the day of or the day after orchiectomy.

Duration of therapy depends on the duration of clinical response of the patient.

Cautions for Nilutamide

Contraindications

  • Severe hepatic impairment.

  • Severe respiratory insufficiency.

  • Known hypersensitivity to nilutamide or any ingredient in the formulation.

Warnings/Precautions

Warnings

Interstitial Pneumonitis

Interstitial pneumonitis reported (i.e., progressive exertional dyspnea, cough, chest pain, fever, interstitial or alveolo-interstitial changes on chest radiographs, and pulmonary function tests show a restrictive pattern with decreased carbon monoxide diffusing capacity), rarely resulting in hospitalization or death. Manifestations generally occurred within the first 3 months of therapy and resolved following discontinuance of the drug.

Obtain a chest radiograph prior to the initiation of therapy. Baseline pulmonary function tests also may be considered.

Immediately discontinue therapy if dyspnea or worsening of preexisting dyspnea occurs; perform tests to determine if respiratory symptoms are drug related.

Hepatic Effects

Severe hepatic injury (i.e., hepatitis, increased serum transaminase concentrations) reported, sometimes resulting in hospitalization and/or rarely death; generally occurred within the first 3–4 months of therapy.

Measure serum transaminase concentrations prior to initiation of therapy, at regular intervals during the first 4 months of treatment, and periodically thereafter. Immediately measure serum transaminase concentrations if clinical signs or symptoms suggestive of liver dysfunction (e.g., nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like symptoms, dark urine, jaundice, or right upper quadrant tenderness) occur. Discontinue immediately and closely monitor liver function if jaundice develops or serum ALT concentration is >2 times ULN.

Use in Women

Safety and efficacy not established in women.

Not intended for use in women, particularly for nonserious or non-life-threatening conditions.

Hematologic Effects

Isolated cases of aplastic anemia reported, but a causal relationship with nilutamide not established.

General Precautions

Ocular Effects

Possible difficulty in visual adaptation to changes in light level; delays, ranging from seconds to a few minutes, in adapting to changes from light to dark reported. Such effect may not diminish during continued therapy with the drug. To minimize this effect, advise patients to wear tinted glasses during exposure to bright light.

Alcohol Intolerance

Possible alcohol intolerance (e.g., facial flushing, malaise, hypotension); avoid concomitant use.

Specific Populations

Pregnancy

Category C. (See Use in Women under Cautions.)

Pediatric Use

Safety and efficacy not established.

Common Adverse Effects

Hypertension, nausea, constipation, hot flushes, increased AST/ALT concentrations, dizziness, impaired adaptation to dark, abnormal vision.

Interactions for Nilutamide

Inhibits the activity of CYP isoenzymes; may reduce the metabolism of drugs metabolized by these systems.

Specific Drugs

Drug

Interaction

Comment

Alcohol

Possible alcohol intolerance (e.g., facial flushing, malaise, hypotension)

Avoid concomitant use

Phenytoin

Increased plasma phenytoin concentrations

Monitor for phenytoin toxicity and adjust dosages as needed

Theophylline

Increased plasma theophylline concentrations

Monitor for theophylline toxicity and adjust dosages as needed

Vitamin K antagonists (e.g., warfarin sodium)

Increased plasma vitamin K antagonist concentrations

Monitor PT and adjust dosages as needed

Nilutamide Pharmacokinetics

Absorption

Bioavailability

Rapidly and completely absorbed to yield high and persistent plasma concentrations.

Distribution

Plasma Protein Binding

Moderately bound to plasma proteins; minimally bound to erythrocytes.

Elimination

Metabolism

Extensively metabolized in the liver and lungs by CYP isoenzymes to mainly inactive metabolites.

Elimination Route

Eliminated almost exclusively by hepatic metabolism. Excreted principally in urine as metabolites; <2% is excreted unchanged in urine.

Half-life

Mean elimination half-life is approximately 30–59 hours following a single 100–300-mg dose.

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C). Protect from light.

Actions

  • Pure antiandrogen, possesses no intrinsic estrogenic, antiestrogenic, progestational, antiprogestational, or adrenocortical activity.

  • Competitively blocks nuclear androgen receptors in target tissues (e.g., prostate, seminal vesicles, adrenal cortex).

  • Blockade of androgen receptors in the hormone-sensitive tumor cells may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis.

  • The relative binding affinity of nilutamide at androgen receptors is less than that of bicalutamide, but similar to that of hydroxyflutamide, the active metabolite of flutamide.

Advice to Patients

  • Risk of interstitial pneumonitis. Importance of immediately notifying clinicians of dyspnea or worsening of preexisting dyspnea.

  • Risk of hepatic toxicity. Importance of notifying clinicians if symptoms of nausea, vomiting, abdominal pain, or jaundice occur.

  • Risk of delay in visually adapting to changes from light to dark. Importance of wearing tinted glasses during exposure to bright light and of exercising caution when driving at night or through tunnels.

  • Risk of alcohol intolerance (e.g., facial flushing, malaise, hypotension). Importance of avoiding alcohol consumption if such intolerance occurs.

  • Importance of taking only as prescribed; do not interrupt or discontinue therapy unless otherwise instructed by a clinician.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Nilutamide

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

150 mg

Nilandron (with povidone)

Sanofi-Aventis

AHFS DI Essentials™. © Copyright 2021, Selected Revisions November 1, 2005. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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