TAK-385 + fluconazole

**TAK-385 (relugolix)** is a highly selective, orally active, nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist developed primarily for prostate cancer and other hormone-dependent conditions. TAK-385 works by competitively binding and blocking the GnRH receptor in the pituitary, rapidly suppressing luteinizing hormone (LH) and testosterone or estradiol production without the initial hormone surge seen with GnRH agonists[1][2][3][4]. **Fluconazole** is a triazole antifungal that inhibits fungal cytochrome P450 enzyme 14α-demethylase, disrupting ergosterol synthesis and leading to cell membrane dysfunction; it is commonly used for a variety of fungal infections. The combination **TAK-385 + fluconazole** is not a commercial, fixed-dose product, but has been studied as a drug-drug interaction to evaluate the effect of fluconazole (a strong CYP3A inhibitor) on the pharmacokinetics of TAK-385, since TAK-385 is metabolized by CYP3A. The combination is not indicated as a therapy for any disease, but studied to assess metabolic interactions for clinical safety and dose adjustment[5][7].

Other names

relugolix + fluconazole