Nilutamide
Nilutamide is a first-generation non-steroidal androgen-receptor antagonist used with surgical or medical castration in metastatic prostate cancer. It is distinguished by unusual side effects — delayed dark adaptation, alcohol intolerance, and interstitial pneumonitis — and is now rarely chosen over newer agents.
01 Overview
Marketed as Nilandron/Anandron, nilutamide blocks the androgen receptor and was among the earliest AR antagonists. It is used almost exclusively in combination with castration for advanced prostate cancer.
Its distinctive adverse effects, particularly visual disturbance in dim light and a disulfiram-like reaction to alcohol, along with rare pulmonary toxicity, have limited its use compared with bicalutamide.
02 Mechanism
Competitively antagonises the androgen receptor, blocking testosterone and DHT signalling. Used alongside castration since it does not lower serum androgens alone.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Prostate cancer | 150–300 mg/day | Oral | 300 mg/day for 30 days, then 150 mg/day, with castration |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Androgen-receptor blockadeImproves outcomes with castration in metastatic prostate cancer. | Strong | Clinical | |
| Delayed disease progressionCombined androgen blockade delays progression versus castration alone in some trials. | Progression benefit | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Delayed adaptation to darknessSlowed visual recovery when moving from light to dark, e.g. night driving. | Mild | Very common | Clinical | |
| Interstitial pneumonitisRare but serious inflammatory lung disease. | Severe | Rare | Clinical | |
| Alcohol intoleranceFacial flushing and malaise after alcohol (disulfiram-like). | Mild | Common | Clinical |