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. |
| Molecular Weight | 317.3 |
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 | Contraindicated due to risk of feminization of male fetus: nilutamide is an antiandrogen that can inhibit androgen receptor signaling, leading to ambiguous genitalia or other developmental anomalies in male fetuses. |
| 2nd trimester | Contraindicated: continued risk of fetal harm; animal studies show teratogenic effects including urogenital abnormalities. |
| 3rd trimester | Contraindicated: potential for neonatal withdrawal or hormonal effects; no safe dose established. |
Clinical note
Comprehensive clinical and safety monograph for NILANDRON (NILANDRON).
| Placental transfer | Crosses the placenta in animals; human data limited but presumed transfer due to molecular weight <500 Da and lipophilicity. |
| Breastfeeding | Not recommended during breastfeeding. Nilutamide is excreted in animal milk; human data absent. Potential for severe adverse effects in nursing infant, including antiandrogenic effects. |
■ 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 |
Hypersensitivity to nilutamide or any componentSevere hepatic impairment (Child-Pugh C)Interstitial pneumonitis or pulmonary fibrosisPregnancyWomen of childbearing potential unless adequate contraception used
| Precautions | Monitor liver function tests before and during therapy, Hepatotoxicity, Peripheral edema, Gynecomastia, Breast tenderness, Adrenal insufficiency, Hyperglycemia in diabetic patients |
| Food/Dietary | No specific food interactions reported. Administer with meals to reduce GI intolerance. |
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| Lactation Rating | L5 (Contraindicated) |
| 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. |
| 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. |
| Clinical Pearls | Nilandron (nilutamide) is an antiandrogen for metastatic prostate cancer. Monitor liver function tests (LFTs) monthly for first 4 months due to risk of hepatitis. Administer with food to reduce GI upset. Delayed dark adaptation is common; warn patients about driving at night. Interstitial pneumonitis is a rare but serious adverse effect; discontinue if dyspnea or cough develops. Dosage adjustment required for moderate hepatic impairment (Child-Pugh B). |
| Patient Advice | Take with food to decrease stomach upset. · May cause difficulty adjusting to darkness; avoid night driving until you know how this drug affects you. · Report any yellowing of skin/eyes, dark urine, or abdominal pain immediately (signs of liver problems). · Report new or worsening shortness of breath or cough. · Do not stop taking without consulting your doctor. |