Version May 2024
Interstitial pneumonitis has been reported in 2% of patients in controlled clinical trials in patients exposed to nilutamide. A small study in Japanese patients 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 in postmarketing. 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 diffusing capacity of lungs for carbon monoxide (DLco). Most cases occurred within the first 3 months of treatment with nilutamide, and most reversed with discontinuation of therapy. A routine chest x-ray should be performed prior to initiating treatment with nilutamide. 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 nilutamide. If symptoms occur, nilutamide should be immediately discontinued until it can be determined if the symptoms are drug related.
Note: Correct electrolyte abnormalities prior to nilutamide initiation (in patients at risk for QT prolongation).
Prostate cancer, metastatic: Oral: 300 mg once daily (starting the same day or day after surgical castration) for 30 days, followed by 150 mg once daily. Consider therapy discontinuation in patients with evidence of disease progression.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling.
Hepatic impairment at treatment initiation:
Mild or moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling.
Severe impairment: Use is contraindicated.
Hepatotoxicity during treatment: ALT >2 × ULN or jaundice: Discontinue nilutamide.
Pulmonary symptoms (exertional dyspnea, new or worsening dyspnea, cough, chest pain, and fever): Immediately discontinue nilutamide until it can be determined if the symptoms are drug-related.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Endocrine & metabolic: Hot flash (28%)
Ophthalmic: Night blindness (13%)
1% to 10%:
Cardiovascular: Hypertension (5%)
Gastrointestinal: Constipation (7%), nausea (10%)
Hepatic: Increased serum alanine aminotransferase (8%), increased serum aspartate aminotransferase (8%)
Nervous system: Dizziness (7%)
Ophthalmic: Visual disturbance (7%)
<1%: Respiratory: Interstitial pneumonitis
Frequency not defined: Hepatic: Hepatitis
Postmarketing:
Dermatologic: Loss of body hair (Janknegt 1993), loss of scalp hair (Janknegt 1993)
Endocrine & metabolic: Gynecomastia (Crawford 2018)
Genitourinary: Mastalgia (Crawford 2018)
Hepatic: Hepatotoxicity (including fulminant hepatic failure) (Merwat 2009)
Ophthalmic: Blurred vision (Rashid 2019)
Miscellaneous: Disulfiram-like reaction (Rashid 2019)
Hypersensitivity to nilutamide or any component of the formulation; severe hepatic impairment; severe respiratory insufficiency.
Canadian labeling: Additional contraindications (not in the US labeling): Use in women and children.
Concerns related to adverse effects:
• Hematologic: Anemia may occur with testosterone suppression. Aplastic anemia has been reported rarely.
• Hepatotoxicity: Hepatitis or marked increases in liver enzymes leading to nilutamide discontinuation occurred in a small percentage of patients. Rare postmarketing cases of hospitalization or deaths due to severe liver injury have been reported. Hepatotoxicity generally occurred within first 3 to 4 months of therapy. Signs/symptoms of hepatic dysfunction include nausea, vomiting, abdominal pain, anorexia, fatigue, flu-like symptoms, dark urine, jaundice, and/or right upper quadrant tenderness.
• Interstitial pneumonitis: Interstitial pneumonitis has been reported with nilutamide. There have been rare postmarketing reports of interstitial changes, including pulmonary fibrosis that led to hospitalization and death. 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 diffusing capacity of lungs for carbon monoxide (DLco). Most cases occurred within the first 3 months of nilutamide treatment, and most reversed with nilutamide discontinuation. Instruct patients to report any new or worsening shortness of breath that they experience while on nilutamide.
• Vision effects: Impaired adaptation to darkness, abnormal vision, and colored vision have been reported.
Disease-related concerns:
• Cardiovascular disease: Androgen-deprivation therapy may increase the risk for cardiovascular disease (Levine 2010). Androgen deprivation therapy with other antiandrogen agents has resulted in prolongation of the QT/QTc interval (Garnick 2004); evaluate risk versus benefit in patients with congenital long QT syndrome, heart failure, frequent electrolyte abnormalities, and in patients taking medication known to prolong the QT interval. Correct electrolyte abnormalities prior to nilutamide initiation.
• Decreased bone mineral density: Prolonged use of antiandrogen therapy is associated with decreased bone mineral density and an increased risk of osteoporosis and fracture (Smith 2003); alcohol abuse, familial history of osteoporosis, and/or chronic use of drugs capable of decreasing bone mass (eg, corticosteroids) may increase risk. Evaluate risk carefully before initiating therapy.
• Diabetes: Hyperglycemia has been observed; use with caution in patients with diabetes.
Other warnings/precautions:
• Antiandrogen withdrawal syndrome: Patients with disease progression while receiving antiandrogen therapy may experience clinical improvement with discontinuation of the antiandrogen.
• Ethanol use: Some patients experience intolerance (facial flushing, hypotension, malaise) when alcohol is combined with nilutamide. Instruct patients to avoid alcohol.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Nilandron: 150 mg [contains corn starch]
Generic: 150 mg
Yes
Tablets (Nilandron Oral)
150 mg (per each): $124.00
Tablets (Nilutamide Oral)
150 mg (per each): $225.24
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Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Anandron: 50 mg
Oral: Administer with or without food.
This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Nilutamide may cause teratogenicity, reproductive toxicity, and has a structural or toxicity profile similar to existing hazardous agents.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Prostate cancer, metastatic: Treatment of metastatic prostate cancer (stage D2) (in combination with surgical castration).
Nilutamide may be confused with apalutamide, bicalutamide, darolutamide, enzalutamide, flutamide, nilotinib.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alcohol (Ethyl): Nilutamide may enhance the adverse/toxic effect of Alcohol (Ethyl). Specifically, nilutamide may increase the likelihood of alcohol intolerance (eg, facial flushing, malaise, hypotension). Risk X: Avoid combination
Choline C 11: Antiandrogens may diminish the therapeutic effect of Choline C 11. Risk C: Monitor therapy
Flotufolastat F18: Antiandrogens may diminish the diagnostic effect of Flotufolastat F18. Management: Therapies targeting the androgen pathway may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of these therapies on the performance of flotufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Gallium Ga 68 PSMA-11: Antiandrogens may diminish the therapeutic effect of Gallium Ga 68 PSMA-11. Management: Therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact on the performance of gallium Ga 68 PSMA-11 (gozetotide) is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Indium 111 Capromab Pendetide: Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination
Piflufolastat F18: Antiandrogens may diminish the diagnostic effect of Piflufolastat F18. Management: Therapies targeting the androgen pathway may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of these therapies on the performance of piflufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Animal reproduction studies have not been conducted. Nilutamide is not indicated for use in patients who could become pregnant.
Nilutamide is not indicated for use in females.
Monitor serum transaminases at baseline, at regular intervals for the first 4 months of treatment, and periodically thereafter; assess LFTs at the first sign or symptom suggestive of liver dysfunction; if nilutamide is discontinued, closely follow liver function tests (LFTs) until resolution. Blood glucose and/or glycosylated hemoglobin (HbA1c) in patients with diabetes (baseline and periodic). Consider baseline and periodic electrolyte and ECG monitoring in patients at risk for QT prolongation. Chest x-ray (at baseline); consider pulmonary function testing (at baseline). Bone-mineral density (as clinically indicated in patients at risk of osteoporosis). Monitor for signs/symptoms of liver dysfunction, cardiovascular disease, and interstitial pneumonitis. Monitor for vision changes. If initiating nilutamide in patients who are on warfarin, closely monitor prothrombin time. Monitor adherence.
Cardiovascular monitoring for patients with prostate cancer: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking; baseline and serial ECGs are recommended in patients at risk of QTc prolongation during androgen deprivation therapy (ADT); estimate 10-year cardiovascular disease risk in patients without cardiovascular disease at baseline; assess cardiovascular risk annually during ADT (ASCO [Armenian 2017]; ESC [Lyon 2022]).
Nilutamide is a nonsteroidal antiandrogen which blocks testosterone effects at the androgen receptor level, preventing androgen response.
Absorption: Rapid and complete
Metabolism: Hepatic (extensive), forms active metabolites
Half-life elimination: Terminal: 38 to 59 hours; Metabolites: 59 to 126 hours
Excretion: Urine (62%; <2% as unchanged drug); feces (1% to 7%)
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