Nilutamide

Nilutamide
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

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Black Box Warning

Warning See full prescribing information for complete Boxed Warning. Interstitial Pneumonia: Interstitial pneumonitis has been reported in 2% of patients in controlled clinical trials in patients exposed to nilutamide. A small study in Japanese subjects showed that 8 of 47 patients (17%) developed interstitial pneumonitis. Reports of interstitial changes including pulmonary fibrosis that led to hospitalization and death have been reported rarely post-marketing. Symptoms included exertional dyspnea, cough, chest pain, and fever. X-rays showed interstitial or alveolo-interstitial changes, and pulmonary function tests revealed a restrictive pattern with decreased DLco. Most cases occurred within the first 3 months of treatment with NILANDRON, and most reversed with discontinuation of therapy. A routine chest X-ray should be performed prior to initiating treatment with NILANDRON. Baseline pulmonary function tests may be considered. Patients should be instructed to report any new or worsening shortness of breath that they experience while on NILANDRON. If symptoms occur, NILANDRON should be immediately discontinued until it can be determined if the symptoms are drug related.

Overview

Nilutamide is an antiandrogen that is FDA approved for the treatment of metastatic prostate cancer. There is a Black Box Warning for this drug as shown here. Common adverse reactions include hypertension, hot sweats, constipation, nausea, dizziness an abnormal vision.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Metastasic Prostate Cancer

• Dosage: The recommended dosage is 300 mg once a day for 30 days, followed thereafter by 150 mg once a day. NILANDRON tablets can be taken with or without food.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Nilutamide in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Nilutamide in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Nilutamide FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Nilutamide in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Nilutamide in pediatric patients.

Contraindications

NILANDRON tablets are contraindicated:

• In patients with severe hepatic impairment (baseline hepatic enzymes should be evaluated prior to treatment)
• In patients with severe respiratory insufficiency
• In patients with hypersensitivity to nilutamide or any component of this preparation.

Warnings

Warning See full prescribing information for complete Boxed Warning. Interstitial Pneumonia: Interstitial pneumonitis has been reported in 2% of patients in controlled clinical trials in patients exposed to nilutamide. A small study in Japanese subjects showed that 8 of 47 patients (17%) developed interstitial pneumonitis. Reports of interstitial changes including pulmonary fibrosis that led to hospitalization and death have been reported rarely post-marketing. Symptoms included exertional dyspnea, cough, chest pain, and fever. X-rays showed interstitial or alveolo-interstitial changes, and pulmonary function tests revealed a restrictive pattern with decreased DLco. Most cases occurred within the first 3 months of treatment with NILANDRON, and most reversed with discontinuation of therapy. A routine chest X-ray should be performed prior to initiating treatment with NILANDRON. Baseline pulmonary function tests may be considered. Patients should be instructed to report any new or worsening shortness of breath that they experience while on NILANDRON. If symptoms occur, NILANDRON should be immediately discontinued until it can be determined if the symptoms are drug related.

Hepatitis

• Rare cases of death or hospitalization due to severe liver injury have been reported post-marketing in association with the use of NILANDRON. Hepatotoxicity in these reports generally occurred within the first 3 to 4 months of treatment. Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in 1% of NILANDRON patients in controlled clinical trials.
• Serum transaminase levels should be measured prior to starting treatment with NILANDRON, at regular intervals for the first 4 months of treatment, and periodically thereafter. Liver function tests should also be obtained at the first sign or symptom suggestive of liver dysfunction, e.g. nausea, vomiting, abdominal pain, fatigue, anorexia, "flu-like" symptoms, dark urine, jaundice, or right upper quadrant tenderness. If at any time, a patient has jaundice, or their ALT rises above 2 times the upper limit of normal, NILANDRON should be immediately discontinued with close followup of liver function tests until resolution.

Use in Women

• NILANDRON has no indication for women, and should not be used in this population, particularly for non-serious or non-life threatening conditions.

Other

• Foreign postmarketing surveillance has revealed isolated cases of aplastic anemia in which a causal relationship with NILANDRON could not be ascertained.

Adverse Reactions

Clinical Trials Experience

he following adverse experiences were reported during a multicenter clinical trial comparing NILANDRON + surgical castration versus placebo + surgical castration. The most frequently reported (greater than 5%) adverse experiences during treatment with NILANDRON tablets in combination with surgical castration are listed below. For comparison, adverse experiences seen with surgical castration and placebo are also listed.

Postmarketing Experience

There is limited information regarding Nilutamide Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Nilutamide Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Nilutamide in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Nilutamide in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Nilutamide during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Nilutamide in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Nilutamide in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Nilutamide in geriatric settings.

Gender

There is no FDA guidance on the use of Nilutamide with respect to specific gender populations.

Race

There is no FDA guidance on the use of Nilutamide with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Nilutamide in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Nilutamide in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Nilutamide in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Nilutamide in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Nilutamide Administration in the drug label.

Monitoring

There is limited information regarding Nilutamide Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Nilutamide and IV administrations.

Overdosage

• One case of massive overdosage has been published. A 79-year-old man attempted suicide by ingesting 13 g of nilutamide (i.e., 43 times the maximum recommended dose). Despite immediate gastric lavage and oral administration of activated charcoal, plasma nilutamide levels peaked at 6 times the normal range 2 hours after ingestion. There were no clinical signs or symptoms or changes in parameters such as transaminases or chest X-ray. Maintenance treatment (150 mg/day) was resumed 30 days later.
• In repeated-dose tolerance studies, doses of 600 mg/day and 900 mg/day were administered to 9 and 4 patients, respectively. The ingestion of these doses was associated with gastrointestinal disorders, including nausea and vomiting, malaise, headache, and dizziness. In addition, a transient elevation in hepatic enzyme levels was noted in one patient.
• Since nilutamide is protein bound, dialysis may not be useful as treatment for overdose. As in the management of overdosage with any drug, it should be borne in mind that multiple agents may have been taken. If vomiting does not occur spontaneously, it should be induced if the patient is alert. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated.

Pharmacology

There is limited information regarding Nilutamide Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Nilutamide Mechanism of Action in the drug label.

Structure

There is limited information regarding Nilutamide Structure in the drug label.

Pharmacodynamics

There is limited information regarding Nilutamide Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Nilutamide Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Nilutamide Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Nilutamide Clinical Studies in the drug label.

How Supplied

NILANDRON 150 mg tablets are supplied in boxes of 30 tablets. Each box contains 3 child-resistant, PVC, aluminum foil-backed blisters of 10 tablets (NDC 24987-111-14). Each white, biconvex, cylindrical (10 mm in diameter) tablet has a triangular logo on one side and an internal reference number (168D) on the other.

Storage

Store at 25°C (77°F); excursions permitted between 15–30°C (59–86°F). Protect from light.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Nilutamide Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Nilutamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Nilutamide Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Nilutamide Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Nilutamide

Clinical data
ATC code	L02BB02 (WHO)
Pharmacokinetic data
Elimination half-life	38.0 to 59.1 hours
Identifiers
IUPAC name 5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl] imidazolidine-2,4-dione
CAS Number	63612-50-0
PubChem CID	4493
DrugBank	APRD00150
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C12H10F3N3O4
Molar mass	317.221 g/mol

Template:Search infobox Steven C. Campbell, M.D., Ph.D.

Overview

Nilutamide is an antiandrogen medication used in the treatment of advanced stage prostate cancer. Nilutamide blocks the androgen receptor, preventing its interaction with testosterone. Because most prostate cancer cells rely on the stimulation of the androgen receptor for growth and survival, nilutamide can prolong life in men with prostate cancer. Nilutamide is marketed under the name Nilandron in the United States.

References

• Kassouf W, Tanguay S, Aprikian AG. Nilutamide as second line hormone therapy for prostate cancer after androgen ablation fails. J. Urol. 2003 May;169(5):1742-4. PMID 12686822