人用截短侧耳素类新药Lefamulin的研究进展

Advances of Lefamulin:a new pleuromutilin antibiotic

Lefamulin(BC-3781)是第一个治疗系统性细菌感染的截短侧耳素类人用药物,属于半合成抗生素。在2019年8月由美国FDA批准用于治疗社区获得性细菌性肺炎(community-acquired bacterial pneumonia,CABP),商品名为Xenleta。Lefamulin通过与细菌核糖体50S亚基的肽基转移酶中心结合,阻断了肽基转移过程进而抑制了蛋白质合成。Lefamulin具有广泛的抗革兰阳性细菌活性,同时对CABP相关的非典型微生物(肺炎支原体)也具有较强的抗菌活性。本文针对截短侧耳素类新药Lefamulin的作用机制、抗菌谱、临床前和临床试验数据等四个方面进行综述。

Lefamulin(BC-3781)is a semi-synthetic pleuromutilin antibiotic,approved for the treatment of community-acquired bacterial pneumonia(CABP)by Food and Drug Administration(USA)in August 2019,with the commodity name of Xenleta.It is the first pleuromutilin antibiotics used for systemic treatment of bacterial infections in human.Lefamulin binds to the peptidyl transferase center of the 50 S ribosomal subunit to prevent peptide transfer,thus inhibits protein synthesis.Lefamulin displays expanded activity against gram-positive organisms,and also shows high activity against atypical microorganism like Mycoplasma pneumoniae.This review discusses the mechanism,bacterial spectrum of activity,preclinical and clinical data of Lefamulin.