Anastrozole is currently used as first-line treatment in locally advanced or metastatic breast cancer. A generic anastrozole tablet was developed to offer an alternative to the marketed tablet formulation.The aim of the current study was to evaluate the bioequivalence between the test and reference formulations of anastrozole in a single-dose, 2-period, 2-sequence crossover study with a 21-day washout interval. A total of 26 healthy Chinese female volunteers were enrolled and completed the study, after oral administration of a single dose of 1.0-mg test and reference formulations of anastrozole. Blood samples (3 mL) for pharmacokinetic analysis were collected predose and 20min, 40min, 1, 1h20min, 1h40min, 2, 2h20min, 2h40min, 3, 3.5, 4, 7, 12, 24, 48, and 72 hours postdose and were determined by a fully validated high-pressure liquid chromatography-tandem mass spectrometry method. The evaluated pharmacokinetic parameters, including Cmax, AUC0-t, AUC0-, were assessed for bioequivalence based on current guidelines.