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 |