Relugolix when co-administered with P-glycoprotein inhibitors is associated with the highest risk for drug-drug interactions in patients with prostate cancer. Relugolix is a gonadotropin-releasing hormone antagonist that is significantly affected by P-glycoprotein inhibitors, which increase its plasma levels. Co-administration with P-glycoprotein and strong CYP3A inducers also reduces the efficacy of relugolix. These factors make relugolix particularly prone to clinically significant drug-drug interactions when combined with commonly used drugs.
Although flutamide can interact with warfarin, requiring monitoring and possible dose adjustments, these interactions are relatively well-characterized and manageable. The level of interaction risk is not as severe or broad as that of relugolix with P-glycoprotein inhibitors.
Bicalutamide has some drug-drug interaction potential owing to CYP3A4 inhibition and protein-binding displacement effects, but these are not as extensive or complex as those seen with relugolix. Triptorelin is a luteinizing hormone–releasing hormone agonist and, like others in this class, is not known to cause significant drug-drug interactions. Bicalutamide and triptorelin have been used in combination with androgen deprivation therapy and have not been reported to have high drug-drug interaction rates.
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Cite this: Mary L. Windle. Rapid Rx Quiz: Dangerous Drug Interactions – Medscape – May 16, 2025.