Unknown

Dataset Information

0

Effect of food on the pharmacokinetics of zoliflodacin granules for oral suspension: Phase I open-label randomized cross-over study in healthy subjects.


ABSTRACT: Gonorrhea is a sexually transmitted infection for which antibiotic treatment options have declined due to increasing antibiotic resistance. Zoliflodacin, an investigational oral spiropyrimidinetrione antibiotic with activity against Neisseria gonorrhoeae strains that are multidrug-resistant, including to third-generation cephalosporins, is in phase III development for uncomplicated gonorrhea. This phase I, parallel, open-label, randomized, crossover study in healthy adults evaluated the effect of food on the pharmacokinetics of single 3 or 4 g doses of zoliflodacin administered as granules for oral suspension in the fasted state or after consumption of a standardized high-fat meal. Forty-seven out of 48 randomized subjects completed the study. Oral administration of zoliflodacin with food delayed the absorption rate, compared with fasted state, with time to maximum concentration (Tmax ) increasing from 3 to 6 h for the 3 g dose, and 2.5 to 4 h for the 4 g dose, but had no impact on the elimination of zoliflodacin. The maximum concentration (Cmax ) and area under the plasma concentration-time curve from time 0 to 24 h (AUC(0-24) ) significantly increased with food by 52% and 94% for the 3 g dose, and by 89% and 108% for the 4 g dose. Forty-two percent of participants reported a total of 34 treatment-emergent adverse events (TEAEs), which were all considered mild in severity. Headache was the most common TEAE (22/48 subjects, 45.8%) and the only TEAE reported in more than one subject. In conclusion, administration of single 3 and 4 g doses of zoliflodacin as granules for oral suspension, with a high-fat meal was well-tolerated and resulted in statistically significant increases in peak and overall systemic exposure to zoliflodacin.

SUBMITTER: Luckey A 

PROVIDER: S-EPMC10176008 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature

altmetric image

Publications

Effect of food on the pharmacokinetics of zoliflodacin granules for oral suspension: Phase I open-label randomized cross-over study in healthy subjects.

Luckey Alison A   Alirol Emilie E   Delhomme Sophie S   O'Donnell John J   Bettiol Esther E   Mueller John J   O'Brien Seamus S   Gillon Jean-Yves JY  

Clinical and translational science 20230223 5


Gonorrhea is a sexually transmitted infection for which antibiotic treatment options have declined due to increasing antibiotic resistance. Zoliflodacin, an investigational oral spiropyrimidinetrione antibiotic with activity against Neisseria gonorrhoeae strains that are multidrug-resistant, including to third-generation cephalosporins, is in phase III development for uncomplicated gonorrhea. This phase I, parallel, open-label, randomized, crossover study in healthy adults evaluated the effect o  ...[more]

Similar Datasets

| S-EPMC4249579 | biostudies-literature
| S-EPMC7352201 | biostudies-literature
| S-EPMC6824388 | biostudies-literature
| S-EPMC9188616 | biostudies-literature
| S-EPMC5587524 | biostudies-literature
| S-EPMC10651645 | biostudies-literature
| S-EPMC8885939 | biostudies-literature
| S-EPMC10667676 | biostudies-literature
| S-EPMC8743745 | biostudies-literature
| S-EPMC9896679 | biostudies-literature