Comprehensive metabolite profiling of 10-methoxycamptothecin in rats by ultraperformance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry

10-Methoxycamptothecin (MCPT), a natural camptothecin derivative, shows notable anticancer activity. Using UPLC-QTOF-MS, this study characterized MCPT metabolite profiles in rats, detecting 14 metabolites in urine, 5 in bile, 7 in feces, and 2 in plasma. The findings indicated that phase I metabolites of MCPT were primarily formed via demethylation, demethoxylation, and hydroxylation, while phase II metabolites mainly included glucuronide and sulfate of MCPT and its phase I metabolites. MCPT, hydroxycamptothecin, and the subsequent glucuronide conjugates were the predominant forms of MCPT in rats. This study provided a comprehensive overview of the metabolite profile of MCPT in rats.