利福霉素:社区获得性细菌性肺炎领域的新希望。

Q1 Biochemistry, Genetics and Molecular Biology Current Pharmacology Reports Pub Date : 2022-01-01 Epub Date: 2022-07-06 DOI:10.1007/s40495-022-00297-6
Shubham Adhikary, Meher Kaur Duggal, Saraswathy Nagendran, Meena Chintamaneni, Hardeep Singh Tuli, Ginpreet Kaur
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引用次数: 0

摘要

审查目的:社区获得性细菌性肺炎(CABP)仍然是全球关注的健康问题,因为它是导致全球死亡和住院的主要原因。肺炎链球菌和其他感染病菌对大环内酯类药物耐药性的增加导致疾病负担大大增加,而人口结构的变化和合并症的增加又加剧了这一负担。在这种情况下,开发新的抗生素种类至关重要:Lefamulin 又称 BC-3781,是一种主要的胸腺嘧啶类抗生素,已获准在人体静脉注射和口服使用,用于治疗细菌感染。它对革兰氏阳性菌(包括耐甲氧西林菌株)和非典型生物体具有活性,而非典型生物体通常与 CABP 有关。它有一种完全独特的作用机制,即通过阻止 tRNA 与肽转移的结合来抑制蛋白质的合成。C(14)侧链是其药效学和抗菌特性的原因,同时还能帮助克服细菌核糖体的抗药性和突变,提高与靶点氢键的结合数量。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Lefamulin: a New Hope in the Field of Community-Acquired Bacterial Pneumonia.

Purpose of review: Community-acquired bacterial pneumonia (CABP) continues to be a worldwide health concern since it is the major cause of mortality and hospitalisation worldwide. Increased macrolide resistance among Streptococcus pneumoniae and other infections has resulted in a significantly larger illness burden, which has been exacerbated by evolving demography and a higher prevalence of comorbid disorders. Owing to such circumstances, the creation of new antibiotic classes is critical.

Recent findings: Lefamulin, also referred to as BC-3781, is the primary pleuromutilin antibiotic which has been permitted for both intravenous and oral use in humans for the remedy of bacterial infections. It has shown activity against gram-positive bacteria including methicillin-resistant strains as well as atypical organisms which as often implicated in CABP. It has a completely unique mechanism of action that inhibits protein synthesis via way of means of stopping the binding of tRNA for peptide transfer. The C(14) side chain is responsible for its pharmacodynamic and antimicrobial properties, together with supporting in overcoming bacterial ribosomal resistance and mutations improvement amplifying the number of hydrogen bonds to the target site.

Summary: This review aims to highlight the pre-existing treatment options and specific purposes to shed some light upon the development of a new drug lefamulin and its specifications and explore this novel drug's superior efficacy to already existing treatment strategies.

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来源期刊
Current Pharmacology Reports
Current Pharmacology Reports Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
9.30
自引率
0.00%
发文量
35
期刊介绍: Current Pharmacology Reports will: publish cutting-edge reviews on subjects pertinent to all aspects of pharmacology, including drug discovery and development.provide incisive, insightful, and balanced contributions from international leading experts.interest a wide readership of basic scientists and translational investigators in academia and in industry. The Current Pharmacology Reports journal accomplishes its goal by appointing international authorities to serve as Section Editors in key subject areas, such as: epigenetics and epigenomics, chemoinformatics and rational drug design and target discovery, drug delivery and biomaterial, pharmacogenomics and molecular targets and biomarkers, chemical/drug/molecular toxicology, absorption, distribution, metabolism and elimination (ADME), pharmacokinetics (PK) and pharmacodynamics (PD), Modeling & Simulation (M&S) and pharmacometrics, and other related topics in pharmacology including neurology/central nervous system (CNS), cardiovascular, metabolic diseases, cancer, among others. Section Editors for Current Pharmacology Reports select topics for which leading experts contribute comprehensive review articles that emphasize new developments and recently published papers of major importance, highlighted by annotated reference lists. An Editorial Board of internationally diverse members suggests topics of special interest to their country/region and ensures that topics are current and include emerging research. Commentaries from well-known figures in the field are also provided. This journal publishes on a bi-monthly schedule.Please submit here: https://www.editorialmanager.com/phar/default.aspx
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