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.
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.