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 |