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Potential Drug–Drug Interactions of AR-targeted
Therapies
Apalutamide Enzalutamide Darolutamide
Drug category Example 1,2
Interactions 3 Interactions 4 Interactions 5
ACEI/ARBs Losartan ✓ ✓
Alpha -adrenergic Tamsulosin, Silodosin, Alfuzosin,
1A
receptor antagonists Doxazosin ✓ ✓
Analgesics Fentanyl, Oxycodone ✓ ✓
Antibiotics Clarithromycin, Rifampin ✓ ✓ ✓* †
Antifungals Itraconazole ✓ ✓ ✓*
Warfarin ✓ ✓
Clopidogrel ✓ ✓
Antithrombotics
Dabigatran ✓
Apixaban, Rivaroxaban ✓ ✓
Beta-blockers Bisoprolol ✓ ✓
PDE5 Inhibitors Sildenafil, Tadalafil ✓ ✓
ACEI = Angiotensin-converting enzyme; ARB = Angiotensin receptor blocker; PDE5 = Phosphodiesterase-5 1. FDA. https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/DrugInteractionsLabeling/ucm093664.htm;
*If P-gp and strong CYP3A4 inhibitors are used together, monitor patients more frequently for darolutamide 2. Lexicomp Online, Pediatric and Neonatal Lexi-Drugs Online, 2020; 3. ERLEADA Product Monograph, 2019; 4. XTANDI® Product
adverse reactions. Avoid concomitant use of P-gp and strong or moderate CPY3A4 inducers. Monograph, 2019; 5. NUBEQA® (darolutamide) Product Monograph, 2020
†
