Nilutamide

Mechanism-of-action class: Androgen Receptor Antagonists.

• Metastatic Prostate Cancer Nilutamide Tablets are indicated for use in combination with surgical castration for the treatment of metastatic prostate cancer (Stage D 2 ). For maximum benefit, treatment with Nilutamide Tablets must begin on the same day as or on the day after surgical castration.ICD-10: C61

• Nilutamide 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.contraindicated

The recommended dosage is 300 mg once a day for 30 days, followed thereafter by 150 mg once a day. Nilutamide Tablets can be taken with or without food.

Interstitial Pneumonitis 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 Nilutamide Tablets, and most reversed with discontinuation of therapy. A routine chest X-ray should be performed prior to initiating treatment with Nilutamide Tablets. 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 Tablets. If symptoms occur, Nilutamide Tablets 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 Nilutamide Tablets. 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 Nilutamide Tablet patients in controlled clinical trials.

Clinical Trial Experience The following adverse experiences were reported during a multicenter clinical trial comparing Nilutamide Tablets + surgical castration versus placebo + surgical castration. The most frequently reported (greater than 5%) adverse experiences during treatment with Nilutamide Tablets in combination with surgical castration are listed below. For comparison, adverse experiences seen with surgical castration and placebo are also listed. Adverse Experience Nilutamide Tablets + surgical castration (N=225) % All Placebo + surgical castration (N=232) % All Cardiovascular System Hypertension 5.3 2.6 Digestive System Nausea 9.8 6.0 Constipation 7.1 3.9 Endocrine System Hot flushes 28.4 22.4 Metabolic and Nutritional System Increased AST 8.0 3.9 Increased ALT 7.6 4.3 Nervous System Dizziness 7.1 3.4 Respiratory System Dyspnea 6.2 7.3 Special Senses Impaired adaptation to dark 12.9 1.3 Abnormal vision 6.7 1.7 Urogenital System Urinary tract infection 8.0 9.1 The overall incidence of adverse experiences was 86% (194/225) for the Nilutamide Tablets group and 81% (188/232) for the placebo group. The following adverse experiences were reported during a multicenter clinical trial comparing Nilutamide Tablets + leuprolide versus placebo + leuprolide. The most frequently reported (greater than 5%) adverse experiences during treatment with Nilutamide Tablets in combination with leuprolide are listed below. For comparison, adverse experiences seen with leuprolide and placebo are also listed.

Pregnancy Animal reproduction studies have not been conducted with nilutamide. It is also not known whether nilutamide can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Nilutamide should be given to a pregnant woman only if clearly needed.

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.

• Jul 15, 2016ANDAANDA207631Ani Pharms

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

• Nilandron, Tablet, 150 mg (NDC 59212-111-14)To be discontinued
  Sponsor: Advanz Pharma (US) Corp.
  Updated Dec 1, 2025
• Nilandron, Tablet, 150 mg (NDC 66993-212-38)To be discontinued
  Sponsor: Advanz Pharma (US) Corp.
  Updated Dec 1, 2025

1. 1Prostatic Specific Antigen Increased1216%
2. 2Pain811%
3. 3Arthralgia79.6%
4. 4Fatigue79.6%
5. 5Asthenia68.2%
6. 6Disease Progression68.2%
7. 7Feeling Abnormal68.2%
8. 8Prostate Cancer Metastatic68.2%
9. 9Apathy56.8%
10. 10Burning Sensation56.8%
11. 11Death56.8%
12. 12Diverticulitis56.8%
13. 13Dyspnoea56.8%
14. 14Flatulence56.8%
15. 15Hot Flush56.8%

The 10 most recently updated of 14 ClinicalTrials.gov registrations naming Nilutamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Antiandrogen Therapy and Radiation Therapy With or Without Docetaxel in Treating Patients With Prostate Cancer That Has Been Removed by Surgery
  Completed · Phase 2 · Phase 3 · Interventional · 612 enrolled · NRG Oncology
  NCT03070886updated 2026-05-07
• Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for Oligometastatic pRosTate Cancer
  Recruiting · Phase 2 · Phase 3 · Interventional · 464 enrolled · VA Office of Research and Development
  NCT04787744updated 2026-04-08
• Finite Androgen Ablation With or Without Abiraterone Acetate and Prednisone in Treating Patients With Recurrent Prostate Cancer
  Active not recruiting · Phase 2 · Interventional · 310 enrolled · M.D. Anderson Cancer Center
  NCT01786265updated 2026-02-20
• Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer
  Recruiting · Phase 3 · Interventional · 1,273 enrolled · SWOG Cancer Research Network
  NCT03678025updated 2025-09-11
• RE-sensitizing With Supraphysiologic Testosterone to Overcome REsistance (The RESTORE Study)
  Completed · Phase 2 · Interventional · 112 enrolled · Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins
  NCT02090114updated 2022-06-27
• Observational Study of Docetaxel Exposure in Metastatic Prostate Cancer Patients
  Completed · Observational · 35 enrolled · Saladax Biomedical, Inc.
  NCT02376296updated 2022-02-17
• Hormone Therapy in Treating Patients With Rising PSA Levels Following Radiation Therapy for Prostate Cancer
  Completed · Phase 3 · Interventional · 1,386 enrolled · NCIC Clinical Trials Group
  NCT00003653updated 2021-06-23
• Hormone Therapy With or Without Surgery or Radiation Therapy in Treating Patients With Prostate Cancer
  Completed · Phase 3 · Interventional · 361 enrolled · NCIC Clinical Trials Group
  NCT00002633updated 2020-04-03
• Chemotherapy Plus Hormone Therapy Versus Androgen Suppression in Treating Patients With Metastatic or Unresectable Prostate Cancer
  Completed · Phase 3 · Interventional · 306 enrolled · M.D. Anderson Cancer Center
  NCT00002855updated 2018-10-31
• Vaccine Therapy Plus Sargramostim and Interleukin-2 Compared With Nilutamide Alone in Treating Patients With Prostate Cancer
  Completed · Phase 2 · Interventional · National Cancer Institute (NCI)
  NCT00020254updated 2015-04-29

Frequently asked questions

How does Nilutamide work?

Mechanism-of-action class: Androgen Receptor Antagonists.

What is Nilutamide used for?

According to FDA labeling, Nilutamide carries indications including: Metastatic Prostate Cancer Nilutamide Tablets are indicated for use in combination with surgical castration for the treatment of metastatic prostate cancer (Stage D 2 ). For maximum benefit, treatment with Nilutamide Tablets must begin on the same day as or on the day after surgical castration.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Nilutamide?

Nilutamide is classified as Anti-androgens, Androgen Receptor Inhibitor, Androgen Receptor Antagonists, Testicular Endocrine Activity Alteration.

What are the brand names for Nilutamide?

Nilutamide is marketed under brand names including Nilandron.

What are the contraindications for Nilutamide?

Nilutamide labeling lists contraindications including: Nilutamide 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.. Always consult the full prescribing information and a clinician.