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. 2025 May 16;20(4):627–635. doi: 10.1007/s11523-025-01150-8

Table 2.

A summary of metabolism and potential interactions between ARPIs and relugolix

ARPI CYP3A4 substrate CYP3A4 inducer CYP3A4 inhibitor Possible interaction with relugolix
Apalutamide Yes Strong No Reduces relugolix exposure by inducing CYP3A4, although clinical studies do not show reduced effect of relugolix on testosterone suppression
Enzalutamide Yes Moderate No May reduce relugolix exposure, but clinical studies suggest a neutral net effect due to compensatory mechanisms
Darolutamide Yes Weak No Minimal impact on relugolix; no dose adjustment needed
Abiraterone Yes No Yes May increase relugolix exposure, but no clinical significance noted in studies