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评估类细菌素作为一种针对人类细菌感染的替代疗法的可行性。

Evaluating the feasibility of lantibiotics as an alternative therapy against bacterial infections in humans.

出版信息

Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):675-80. doi: 10.1517/17425255.2011.573478. Epub 2011 Apr 27.

Abstract

Since the commercialization and ubiquitous use of antibiotics in the 20th century, there has been a steady increase in the number of reports on resistant bacteria. In recent years, this situation has become even more dramatic. The relatively slow development of new drugs, especially those with novel modes of action on target bacteria, is not paired with the rapid rate of resistance appearance. Lantibiotics form a group of antimicrobial peptides of bacterial origin with a dual mechanism of action not shared by other therapeutic compounds in use. They have a high potency to inhibit diverse (multidrug resistant) bacteria, combined with a low tendency to generate resistance. These properties make lantibiotics attractive candidates for clinical applications. This paper discusses some of the most recent results obtained in lantibiotic clinical application, paying special attention to the pharmacokinetic and pharmacodynamic properties they display. The objective of this paper is to give insight into the actual clinical applicability of lantibiotics and to point to the unexplored aspects that should be addressed in future research. The authors feel that lantibiotics could increase the number of second line antibiotics for systemic use in the future; however, further research is still needed before this is possible.

摘要

自 20 世纪抗生素商业化和广泛应用以来,关于耐药菌的报告数量稳步增加。近年来,这种情况变得更加严重。新药物的发展相对缓慢,特别是那些针对靶细菌具有新型作用模式的药物,与耐药性的快速出现并不匹配。类细菌素是一类具有双重作用机制的细菌来源的抗菌肽,与其他正在使用的治疗化合物不同。它们具有抑制多种(多药耐药)细菌的高效力,同时不易产生耐药性。这些特性使类细菌素成为临床应用的有吸引力的候选药物。本文讨论了类细菌素临床应用中获得的一些最新结果,特别关注它们表现出的药代动力学和药效动力学特性。本文的目的是深入了解类细菌素的实际临床适用性,并指出未来研究中应解决的未探索方面。作者认为,类细菌素可能会增加未来用于全身系统使用的二线抗生素数量;然而,在这成为可能之前,仍需要进一步的研究。

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