人用截短侧耳素类抗生素的研究现状与发展趋势  

Research Status and Development Trend of Pleuromutilin Antibiotics for Human Use

作　　者：孙影[1] 周紫薇[1] 李思谦[1] 郑珩[1] 顾觉奋[1] 

机构地区：[1]中国药科大学生命科学与技术学院,南京210009

出　　处：《国外医药（抗生素分册）》2017年第3期99-108,共10页World Notes on Antibiotics

基　　金：江苏高校优势学科建设工程资助项目(PAPD);大学生创新创业训练计划项目

摘　　要：为了应对日益严重的细菌耐药性问题,人们不断研发具有新型作用机制的抗菌药物,其中截短侧耳素及其衍生物作为重要的一类兽用抗生素,具有独特的作用机制,其特点不易产生交叉耐药性。已经上市的泰妙菌素、沃尼妙林均具有抗菌谱广及较强的抗菌活性,而2007年4月批准的瑞他莫林是近二十年来首个新的局部应用的抗菌药物,被认为是第一个人用截短侧耳素衍生物,标志着截短侧耳素类从兽用跨越到人用领域。本文就截短侧耳素的作用机制、耐药机制、人用截短侧耳素的临床研究现状以及新型截短侧耳素衍生物研发等方面的最新进展做简要概述。In order to cope with the increasingly serious problem of bacterial resistance, scientific researchers have developed a series of antimicrobial agents with new mechanisms. As an important class of veterinary antibiotics, pleuromutilin and its derivatives were shown with a unique mechanism of action and not easy to produce cross- resistance with antibiotics currently in clinical use. Successively listed tiamulin and valnemulin also have the advantages of wider antimicrobial spectrum and stronger antibacteria! activity, and in April 2007, retapamulin has been approved as a topical antibacterial agents in the last 20 years, which was also the first pleuromutilin derivatives for human use. It was a sign that this antibiotic had achieved a leap from the beast to man. In this paper, an overview of the action and resistance mechanism, clinical research situation of pleuromutilin for human use and the development of new pleuromutilin derivatives were briefly discussed.

关 键 词：人用截短侧耳素 作用机制 耐药机制 新型截短侧耳素衍生物 

分 类 号：R978.1[医药卫生—药品]