Evaluation of Drug–Drug Interaction Potential Between the Oral Antibiotic Zoliflodacin and the CYP3A4 Inhibitor Itraconazole: A Phase 1 Study in Healthy Participants
Zoliflodacin is a first-in-class oral spiropyrimidinetrione antibiotic being developed for patients with uncomplicated gonorrhea, including those infected with multidrug-resistant strains. Because zoliflodacin is metabolized by cytochrome P450 3A4 (CYP3A4), concomitant administration with a CYP3A inhibitor has the potential to increase zoliflodacin plasma exposure. The aim of this phase 1 drug–drug interaction (DDI) study was to assess the effect of the strong CYP3A4 inhibitor itraconazole on the pharmacokinetics (PK) and safety of a 3 g single oral dose of zoliflodacin.
Authors
Alison Luckey, Kajal B. Larson, Noha Rayad, Markus Heep, Sophie Delhomme, Gabrielle Kornmann, John P. Mueller, John P. O’Donnell, Seamus O’Brien, Rainard Fuhr, Jean-Yves Gillon