nilutamide (Nilandron)

Indications: - used in combination with LHRH agonist for treatment of metastatic prostate cancer Dosage: 1) 300 mg PO QD for one month, then 2) 150 mg PO QD Pharmacokinetics: 1) well obsorbed orally 2) peak serum levels in 1-4 hours after oral dosing 3) 80% protein bound 4) metabolized extensively by the liver 5) 60% excreted in the urine as metabolites 6) elimination 1/2 life is 38-60 hours Adverse effects: 1) hot flashes 2) gynecomastia 3) nausea/vomiting 4) abnormal liver function tests 5) visual delayed adaptation to darkness 6) interstitial pneumonitis 7) pruritus 8) alcohol intolerance Mechanism of action: - non-steroidal androgen receptor antagonist

General

androgen receptor antagonist; androgen receptor signaling inhibitor (ARSI) antineoplastic endocrine agent

Properties

INHIBITS: androgen receptor MISC-INFO: elimination route LIVER 1/2life 38-60 HOURS protein-binding 80%

References

DrugDex Drug Evaluation, vol 105, 2000