Tebipenem, the first oral carbapenem antibiotic
Tebipenem, the first oral carbapenem antibiotic
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DOI：
10.1080/14787210.2018.1496821
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发表时间：
2018-01-01
影响因子：
5.7
通讯作者：
Pucci, Michael J.
中科院分区：
文献类型：
--
作者：
Jain, Akash;Utley, Luke;Pucci, Michael J.
(引言：抗生素耐药病原体引起的感染，特别是革兰氏阴性菌引起的感染，已经越来越难以成功治疗。-内酰胺类抗生素亚类，碳青霉烯类，由于其谱和-内酰胺酶稳定性，已被证明对治疗革兰氏阴性细菌感染有价值。然而，到目前为止，所有上市的碳青霉烯类药物都是用于成人患者的肠外给药。覆盖领域：碳青霉烯一种，tbipenem -pivoxil (TBPM-PI)，是一种口服前药，仅在2009年在日本被批准用于儿科。这篇综述总结了TBPM-PI的临床前和临床数据，该药物再次进入临床开发，这一次是作为第一种口服碳青霉烯类药物用于治疗成人患者的细菌感染。专家评论：在医院和社区环境中，氟喹诺酮耐药和产生esblg的革兰氏阴性病原体日益流行，这是一项迫切的未得到满足的需求。碳青霉烯类传统上被认为是由产生ESBL和AmpC酶的肠杆菌引起的感染的首选药物，因为它们不受这些耐药机制的影响。碳青霉烯，TBPM-PI，提供了一种口服选择，特别是作为降压治疗，用于治疗严重革兰氏阴性感染。
(Introduction: Infections caused by antibiotic-resistant pathogens, particularly Gram-negative bacteria, have become increasingly challenging to successfully treat. The beta-lactam antibiotic subclass, the carbapenems, have proven valuable for the treatment of) such Gram-negative bacterial infections due to their spectrum and -lactamase stability properties. However, all marketed carbapenems to date are parenterally administered to adult patients.Areas covered: One carbapenem, tebipenem-pivoxil (TBPM-PI), is an oral prodrug that was approved in Japan for pediatric use only in 2009. This review summarizes preclinical and clinical data for TBPM-PI, which is now in clinical development again this time for use as the first oral carbapenem available for treatment of bacterial infections in adult patients.Expert commentary: There is an urgent unmet need with an increasing prevalence of fluoroquinolone-resistant and ESBL-producing Gram-negative pathogens in the hospital and community setting. Carbapenems have traditionally been considered the drugs of choice for infections caused by enterobacteria producing ESBL and AmpC enzymes because they are not affected by these resistance mechanisms. The carbapenem, TBPM-PI, offers an oral option, particularly as step-down therapy, for use of this class in the treatment of serious Gram-negative infections.