ERLEADA - Drug Interactions

SUMMARY  

• Apalutamide is primarily metabolized by CYP2C8 and CYP3A4 to form active metabolite, N-desmethyl apalutamide. Co-administration of a strong CYP2C8 or CYP3A4 inhibitor is predicted to increase the steady-state exposure of the active moieties (sum of unbound apalutamide plus the potency-adjusted unbound N-desmethyl-apalutamide). Reduce the ERLEADA dose as recommended for adverse reactions.^1-3 Please refer to local labeling for guidance and additional considerations.
• Apalutamideis a strong inducer of CYP3A4 and CYP2C19, and a weak inducer of CYP2C9, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and organic anion transporting polypeptide 1B1 (OATP1B1). Apalutamide decreases exposure of substrates of CYP3A4, CYP2C19, CYP2C9, P-gp, BCRP, or OATP1B1, which may decrease the effectiveness of these substrates. Consider alternative agents when possible or evaluate for loss of activity of the substrate if concomitant use cannot be avoided.^1,3-5

DRUG INTERACTIONS

For up-to-date drug interaction, pharmacokinetic, and pharmacodynamic clinical data pertaining to specific medicinal agents, please review the local labeling of ERLEADA and/or contact the manufacturers of these agents for additional information.

Literature Search

A literature search of MEDLINE^®, Embase^®, BIOSIS Previews^®, and Derwent Drug File (and/or other resources, including internal/external databases) was conducted on
08 September 2025.