Effect of a high-fat meal on the pharmacokinetics of the des-F(6)-quinolone BMS-284756.
OBJECTIVE
To evaluate the effects of a high-fat meal on the systemic exposure of oral BMS-284756.


METHODS
Open-label, randomized, two-way crossover study.


METHODS
Clinical research facility.


METHODS
Fourteen healthy individuals.


METHODS
Participants received two single 400-mg doses of BMS-284756, separated by at least 1 week. One dose was given while participants were fasting, and one dose was given within 5 minutes of consumption of a high-fat meal.


RESULTS
Serial blood samples were collected, and plasma samples were analyzed for BMS-284756 using a validated liquid chromatography with tandem mass spectrometry detection method. Maximum plasma concentration and area under the plasma concentration-time curve (AUC) after the high-fat meal were 19% and 11% lower, respectively, than those in the fasted state. The 90% confidence intervals for the ratios of means (0.71-0.94 and 0.85-0.93, respectively) satisfied predefined equivalence criteria. Equivalence of the AUC values for BMS-284756 in fed and fasted individuals indicates that the presence of food should not affect the efficacy of this drug.


CONCLUSIONS
Single doses of BMS-284756 were safe and well tolerated and may be taken without regard to meals.
Gajjar
Diptee A
DA
Department of Clinical Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000, USA.
Sukoneck
Samuel C
SC
Bello
Akintunde
A
Ge
Zhiyu
Z
Christopher
Lisa
L
Grasela
Dennis M
DM
D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002853:Chromatography, Liquid; D018592:Cross-Over Studies; D004041:Dietary Fats / Q000494:pharmacology*; D004347:Drug Interactions; D005215:Fasting / Q000097:blood; D005260:Female; D024841:Fluoroquinolones; D006207:Half-Life; D006801:Humans; D007211:Indoles; D008297:Male; D013058:Mass Spectrometry; D015363:Quinolones
D000890:Anti-Infective Agents; D004041:Dietary Fats; D024841:Fluoroquinolones; D007211:Indoles; D015363:Quinolones; C419689:garenoxacin