NILANDRON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NILANDRON (NILANDRON).
Competitive inhibitor of androgen binding to androgen receptors, reducing androgen-mediated growth of prostate cancer cells. Also inhibits testicular and adrenal androgen synthesis.
| Metabolism | Hepatic via hydroxylation and glucuronidation; metabolites excreted renally and fecally. |
| Excretion | Renal: 55-60% as unchanged drug; fecal: 20-30% as metabolites; biliary: minor (<10%). |
| Half-life | Terminal elimination half-life: 7-8 hours; clinically relevant for twice-daily dosing. |
| Protein binding | 99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 1.8-2.5 L/kg; indicates extensive distribution into tissues, including prostate. |
| Bioavailability | Oral: 80-90% (well absorbed with food). |
| Onset of Action | Oral: 2-4 hours for steady-state plasma concentrations; clinical effects on androgen-dependent symptoms within 2-4 weeks. |
| Duration of Action | Twice-daily dosing maintains therapeutic levels; clinical effects persist for 1-2 weeks after discontinuation due to residual androgen receptor blockade. |
300 mg orally three times a day.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min; contraindicated in GFR <30 mL/min. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). No adjustment for mild to moderate. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dose. |
| Geriatric use | No specific dose adjustment; monitor for hepatic and pulmonary toxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NILANDRON (NILANDRON).
| Breastfeeding | Not indicated for breastfeeding women. Nilutamide is excreted in rat milk; human data unavailable. M/P ratio unknown. Due to potential serious adverse reactions in nursing infants, breastfeeding is contraindicated during therapy and for at least 2 weeks after last dose. |
| Teratogenic Risk | Nilutamide is contraindicated in pregnancy. In animal studies, it caused embryotoxicity and teratogenicity at doses lower than human therapeutic doses. First trimester exposure is associated with risk of ambiguous genitalia in male fetuses due to antiandrogenic effects. No adequate human studies exist; risk cannot be excluded in all trimesters. |
■ FDA Black Box Warning
Hepatotoxicity: Severe liver injury, including hepatic failure, has been reported. Measure serum transaminases at baseline and periodically; discontinue if jaundice or ALT >3x ULN.
| Serious Effects |
["Severe hepatic impairment","Hypersensitivity to nilutamide or any component"]
| Precautions | ["Monitor liver function tests before and during therapy","Hepatotoxicity","Peripheral edema","Gynecomastia","Breast tenderness","Adrenal insufficiency","Hyperglycemia in diabetic patients"] |
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| Fetal Monitoring | Not applicable in pregnancy as use is contraindicated. In women of reproductive potential, perform pregnancy test prior to initiation. Monitor for signs of hepatotoxicity, pulmonary toxicity, and interstitial pneumonitis. Regular liver function tests and chest imaging recommended. In men, monitor PSA and testosterone levels. |
| Fertility Effects | Nilutamide impairs spermatogenesis and reduces fertility in male rats. In humans, it suppresses testicular steroidogenesis and may cause reversible oligospermia. Antiandrogenic effects may impair gonadal function in both sexes. Long-term use leads to reduced libido and erectile dysfunction. |