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.
Patients with bilateral orchiectomy should take a GnRH analog concurrently.
When darolutamide is used concurrently with docetaxel for metastatic castration-sensitive prostate cancer, administer the 1st of 6 cycles of docetaxel within 6 wk after the initiation of darolutamide.
PO Administer twice daily with food. DNC: Swallow tablets whole; do not crush, break, or chew.
Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient to take missed dose as soon as remembered, but do not double doses.
Advise patient that therapy may ↑ risk of seizures. Avoid activities where a sudden loss of consciousness could cause serious harm to self or others. Notify health care provider immediately if seizure symptoms occur.
Advise patient to immediately notify health care provider of chest pain or difficulty breathing.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Rep: May cause fetal harm. Advise men with female partners of reproductive potential to use effective contraception for 1 wk after last dose. Inform patient that darolutamide may impair fertility.