The impact of rifampicin on the pharmacokinetics of fuzuloparib in healthy Chinese male volunteers

Fuzuloparib is a PARP inhibitor metabolized via CYP3A4, raising concern about interactions with strong CYP3A4 inducers such as rifampicin. This single-arm, fixed-sequence study in 16 healthy Chinese male volunteers evaluated fuzuloparib pharmacokinetics before and after eight days of rifampicin pretreatment, with parameters calculated using Phoenix WinNonlin. Rifampicin pretreatment dramatically reduced fuzuloparib systemic exposure, decreasing AUC to about 10% and Cmax to about 32% of levels seen with fuzuloparib alone, though the combination was well tolerated with no severe adverse events. The findings demonstrate that strong CYP3A4 inducers substantially reduce fuzuloparib exposure and should be avoided during fuzuloparib treatment.