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莱法穆林含有有希望的抗结核活性,可以对抗多药耐药的Mycobacterium结核菌分离物

Jing Wu¹, Yuanfei Ji¹, Weihe Zhang¹

¹National Clinical Laboratory on Tuberculosis, Beijing Key laboratory for Drug-resistant Tuberculosis Research, Beijing Chest Hospital, Capital Medical University, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing, China.

Microbiology spectrum

|October 8, 2025

概括

莱法穆林 (LEF) 在体外和巨细胞内对Mycobacterium tuberculosis表现出强烈的活性. 这种抗生素,特别是与贝达基林结合使用时,在治疗多抗药结核病 (MDR-TB) 方面表现有前途.

科学领域:

微生物学微生物学
传染性疾病传染性疾病
药理学药理学是指药理学的学科.

背景情况:

多药耐药结核病 (MDR-TB) 由于治疗结果不佳,存在重大临床挑战.
乐法穆林 (LEF) 是一种多菌素抗生素,已表现出广泛的格拉姆阳性活性,但其对Mycobacterium tuberculosis (Mtb) 的有效性以前没有得到评估.
研究新型治疗剂对于对抗抗性Mtb菌株至关重要.

研究的目的:

为了评估lefamulin (LEF) 对Mycobacterium tuberculosis (Mtb) 的体外和细胞内抗菌活性.
评估LEF作为治疗Mtb感染的候选药物的潜力,包括MDR-TB.
探索LEF与其他抗结核药物结合的协同潜力.

主要方法:

进行了抗微生物敏感性测试,以确定LEF的最小抑制度 (MIC) 与132个临床Mtb分离物相比.
通过使用巨细胞内的Mtb H37Rv来评估LEF的细胞内活性.
评估了药物相互作用,特别是LEF和贝达基林 (BDQ) 之间的协同作用.

主要成果:

与Mtb临床隔离物相比,LEF的MIC50和MIC90值分别为0.5微克/毫升和1微克/毫升,暂时的流行病学切断值 (ECOFF) 为1微克/毫升.
2μg/mL的LEF抑制了89.88%的细胞内细菌生长,相当于异化 (INH).
在LEF和贝达基林 (BDQ) 之间观察到协同效应 (FIC指数=0.5),没有与其他10种抗结核药物交叉耐药性.

结论:

莱法穆林在体外和细胞内都表现出强烈的抗菌活性对Mtb.
观察到与贝达基林的协同作用使得LEF成为结核病,特别是MDR-TB的有前途的治疗候选药物.
由于LEF缺乏交叉耐药性和良好的活动概况,因此需要进一步研究结核病治疗方案.

关键词:

结核病菌菌菌的结核病菌的结核病菌.抗微生物活性的抗微生物活性.细胞内活动细胞内活动莱法穆林 (Lefamulin) 是一种抗体.

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