Pharmacokinetics, bioequivalence, and safety of two formulations of Toremifene citrate tablets in healthy Chinese participants under fasted and fed conditions

Toremifene is presently administered to treat hormone receptor-positive metastatic breast cancer in postmenopausal women. Currently, there is limited information available regarding the pharmacokinetic profile of Toremifene Citrate in the Chinese population. This study aims to investigate the pharmacokinetics, bioequivalence, and safety of toremifene citrate tablets in healthy Chinese participants under fasted and Fed Conditions. This study was designed as a randomized, open-label, two-period, two-sequence, crossover bioequivalence trial conducted in healthy adult Chinese participants under both fasted and fed conditions. 30 healthy Chinese adult participants, including both males and postmenopausal females (natural or surgically menopausal for more than one year), were enrolled in each condition. Each participant received a 60 mg single dose of Torimifene Citrate Tablets in each period, with a 28-day washout period. The concentration of Toremifene in plasma was measured with a dependable and sensitive LC–MS/MS technique. The main pharmacokinetic parameters (C max , AUC 0–72 h ) were converted by natural logarithm and analyzed by analysis of variance (ANOVA). The study results demonstrated that the test and reference formulations of toremifene were bioequivalent and well tolerated, with no serious adverse reactions noted. Trial registration: ChiCTR2600129105.