Names and pronunciation
(dar′-oh-loo′-tuh-mide) Nubeqa
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Drug reference
(dar′-oh-loo′-tuh-mide) Nubeqa
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Func. class.: Antineoplastic- hormone
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ACTION: Competitively inhibits andro gen binding, AR nuclear translocation, and androgen receptor-mediated transcription
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USES: Nonmetastatic castration-resistant prostate cancer
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SIDE EFFECTS CNS: Fatigue GI: Elevated LFTs, hyperbilirubinemia, diarrhea, nausea GU: Hot flashes HEMA: Neutropenia, anemia MS: MS pain CV: Hyper/hypotension, heart failure INTEG: Rash
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INTERACTIONS Avoid use with CYP3A4, UGT1A9, UGT1A1
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DOSAGE AND ROUTES • Adults: PO 600 mg bid until disease progression or unacceptable toxicity
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Administer: • Patient should be receiving a gonado- tropin-releasing hormone (GnRH) ana- log or has had a bilateral orchiectomy • Give with food • Have the patient swallow the tablet whole; do not crush or chew • If a dose is missed, it should be taken as soon as the patient remembers before the next scheduled dose; do not take 2 doses at the same time if a dose is missed
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Assess: • Prostate cancer: decreasing signs/ symptoms of prostate cancer • Hepatic/renal disease: monitor for hepatic and renal involvement • Pregnancy: males with female part- ners of reproductive potential should avoid pregnancy and use effective con- traception during and ≥1 wk after treat- ment
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Evaluate: Therapeutic response: decreased pro- gression of prostate cancer
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Pregnancy: patients with female partners of reproductive potential should avoid pregnancy and use effec- tive contraception during and ≥1 wk after treatment; there is a possibility of infertility
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PHARMACOKINETICS Use with food, increases bioavailability by 2- to 2.5-fold; protein binding (albumin) 92% for darolutamide, 99.8% active metabolite, keto-darolutamide; half-life 20 hr, 63.4% excreted urine, 32.4% feces (30% unchanged); metabolized by CYP3A4, UGT1A9, and UGT1A1, a BCRP inhibitor, inhibits OATP1B1 and OATP1B3l
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• Adults: PO 600 mg bid until disease progression or unacceptable toxicity
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