Absorption: 30% absorbed following oral administration; absorption ↑ with food.
Distribution: Extensively distributed to tissues.
Protein Binding: Darolutamide: 92%; Keto-darolutamide: 99.8%.
Metabolism and Excretion: Primarily metabolized in the liver by the CYP3A4 isoenzyme as well as by UGT1A1 and UGT1A9 to an active metabolite (keto-darolutamide). Primarily excreted in urine (63%, 7% as unchanged drug) and 32% excreted in feces (30% as unchanged drug).
Monitor for fatigue, pain in extremities, and rash during therapy.
Monitor for signs and symptoms of ischemic heart disease. Optimally manage hypertension, diabetes, and dyslipidemia. If Grade 3–4 ischemic heart disease occurs, permanently discontinue darolutamide.
Instruct patient to take darolutamide as directed. Take missed doses as soon as remembered, but do not take two doses together to make up for a missed dose. Advise patient to read Patient Information before starting therapy.
Advise patient darolutamide may ↑ risk of seizures. Avoid activities where a sudden loss of consciousness could cause serious harm to self or others. Notify health care professional immediately if seizure symptoms occur.
Advise patient to immediately notify health care professional of chest pain or difficulty breathing.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: May cause fetal harm. Advise male patients with female partners of reproductive potential to use effective contraception and avoid breastfeeding during and for 1 wk after last dose. Inform patient that darolutamide may impair fertility.