ABSTRACT
Objective
To evaluate the effect of food on the pharmacokinetics (PK) of fluzoparib capsule.
Methods
PK data were obtained after fluzoparib treatment in a crossover design study. Single-dose fluzoparib (120 mg) was administered under fasted and fed conditions to 16 healthy subjects. Metabolism and transformation fluzoparib were analyzed by liquid chromatograph-tandem mass spectrometry in the first period. Safety was also assessed.
Results
The absorption rate of fluzoparib was slower in the fed group (tmax delayed by 3 h), and peak exposure (Cmax) of fluzoparib in plasma decreased by 19.8% (p < 0.05) compared with the fasted group. The area under the curve (AUC) of fluzoparib was not statistically different between the fasted and fed conditions. The 90% confidence intervals for the Cmax and AUC0-∞ were 69.77–92.24% and 84.88–102.26%, respectively. Five, seven, and five fluzoparib metabolites were isolated from plasma, urine, and feces samples, respectively. Most treatment-emergent adverse events were grade I or II.
Conclusions
The presence of food decreased the absorption rate and peak exposure time of fluzoparib; however, the AUC did not significantly change compared with the fasted condition. Therefore, oral administration does not alter the efficacy and safety profile of fluzoparib.
Acknowledgments
The authors would like to thank the volunteers enrolled in this trial, as well as the staff who contributed to this trial.
Declaration of interest
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in, or financial conflict with, the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Author contributions
The authors are solely responsible for the design and conduct of this study. MW and YHD performed a review of the topic, and wrote and revised the manuscript. HZ took part in analyzing pharmacokinetics data. JXS and HC took part in the analysis and interpretation of data, and prepared all figures and tables. All the authors approved the final version of the manuscript.
Reviewer disclosures
Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.