Contezolid Harbored Equivalent Efficacy to Linezolid in Tuberculosis Treatment in a Prospective and Randomized Early Bactericidal Activity Study

作者：Guanglu Jiang, Rongmei Liu, Yi Xue, Qiping Ge, Lihui Nie, Zizheng Lv, Zhongshun Kong, Jin Shi, Hongmei Chen, Hua Li, Xiaoguang Wu, Li Xie, Yanhua Song, Hairong Huang, Mengqiu Gao · 发表于：Infection and Drug Resistance · 年份：2025 · DOI：10.2147/idr.s499816 · 被引用次数：10 · 研究领域：Tuberculosis Research and Epidemiology、Antimicrobial Resistance in Staphylococcus、Phenothiazines and Benzothiazines Synthesis and Activities

Background: Contezolid (CZD) is an analog of Linezolid (LZD) that has demonstrated potent in vitro and in vivo activity against tuberculosis (TB) while presenting a safer side-effect profile. In this study, we evaluated the early bactericidal activity (EBA) of CZD compared to LZD, with LZD serving as a control. Methods: Naive, smear-positive pulmonary TB patients were enrolled and randomly assigned to receive either a 14-day monotherapy regimen of 600 mg LZD once daily (QD) or 800 mg CZD twice daily (BID). Sputum samples were collected daily starting one day before treatment initiation and continuing throughout the treatment period. Each sample was processed for the enumeration of acid-fast bacilli (AFB) colonies, and time-to-positivity (TTP) during MGIT960 liquid culture was recorded. Results: A total of 10 eligible patients were enrolled in each treatment group, although one patient in the CZD group was later excluded from the analysis. The early bactericidal activity (EBA0-14) was 0.08 ± 0.12 log CFU/mL/day (95% CI: -0.02 to 0.18 CFU/mL/day) in the CZD group, compared to 0.03 ± 0.10 log CFU/mL/day (95% CI: -0.05 to 0.10 CFU/mL/day) in the LZD group. The increase in time-to-positivity (TTP0-14) was 38.6 ± 43.69 hours (95% CI: -1.85 to 79 hours) in the CZD group and 27.7 ± 78.21 hours (95% CI: -28.15 to 83.75 hours) in the LZD group. LZD showed rapid bacterial reduction in sputum during the first two days of treatment, whereas CZD demonstrated superior efficacy after a few d...