Evaluation of drug–drug interaction potential between the oral antibiotic zoliflodacin and the CYP3A4 inhibitor itraconazole: A phase 1 study in healthy participants

by Luckey A, Larson KB, Rayad N, Heep M, Delhomme S, Kornmann G, Mueller JP, O’Donnell JP, O’Brien S, Fuhr R, Gillon J-Y. Clinical and Translational Science 2026,19(3): e70515. doi: 10.1111/cts.70515

Summary: Zoliflodacin, a first-in-class oral spiropyrimidinetrione antibiotic under development for patients with uncomplicated gonorrhea, is metabolized by cytochrome P450 3A4 (CYP3A4), meaning concomitant administration with a CYP3A inhibitor has the potential to increase zoliflodacin plasma exposure. The authors of this manuscript describe a Phase I study to assess the effect of the strong CYP3A4 inhibitor itraconazole on the pharmacokinetics and safety of a 3 g single oral dose of zoliflodacin in 18 adults. When co-administered with itraconazole, zoliflodacin exposure was essentially unchanged when measured by peak concentration (Cmax) and increased by less than 1.5-fold when measured by area under the plasma-concentration time curve (AUC). Combined with an acceptable safety profile, these results indicate a low DDI potential between zoliflodacin and CYP3A4 inhibitors.

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