Linezolid, an oxazolidinone antibacterial agent with several formulations, has been widely used for over 20 years. This study aimed to compare the bioequivalence, pharmacokinetics, and safety of test and reference linezolid tablets after a single oral dose under fasting/fed conditions. In this open-label, randomized, two-period, crossover, bioequivalence study, 48 healthy volunteers were enrolled equally to fasting or fed groups to receive one 600-mg test or reference linezolid tablet in each period. Pharmacokinetic parameters were calculated using noncompartmental methods. Adverse events (AEs) were recorded to assess safety. The geometric mean terminal half-lives of test and reference formulations were 3.8 and 3.6 hours, respectively, under both fasting and fed conditions. The median time to reach the maximum observed concentration was 1.0 hour (both formulations) in the fasting group, and 2.0 hours (test formulation) and 2.5 hours (reference formulation) in the fed group. No substantial differences were observed in the area under plasma concentration-time curve (AUC) from time 0 to the last sampling time (AUC(0-t)) and the maximum observed concentration (C-max) between formulations. Geometric least square mean ratios for C-max, AUC(0-t), and AUC from time 0 to infinity were approximately 100%, and the corresponding 90% confidence intervals for bioequivalence were within 80%-125%. Ten participants reported 11 AEs; AEs were mild, except for one pregnancy event with an outcome of induced absorption. Bioequivalence between the two linezolid formulations was demonstrated under fasting and fed conditions, and a similar safety profile was observed among healthy Chinese volunteers.