Department of Medicine, Division of Infectious Diseases, Northeast Ohio Medical University, Rootstown, OH, USA.
Department of Medicine, MetroHealth Medical Center, Cleveland, OH, USA.
J Antimicrob Chemother. 2023 May 3;78(5):1137-1142. doi: 10.1093/jac/dkad060.
The ongoing spread of antimicrobial resistance has made the treatment of uncomplicated urinary tract infections (UTIs) and urogenital gonorrhoea increasingly difficult. New oral treatment options are urgently needed. Gepotidacin (previously GSK2140944) is a novel, bactericidal, oral, 'first-in-class' triazaacenaphthylene antibiotic that inhibits bacterial DNA replication by blocking two essential topoisomerase enzymes. Mutations in both enzymes would likely be necessary for resistance to occur, thus raising hopes that the drug will be able to maintain long-term effectiveness. Data from Phase II clinical trials of gepotidacin in UTIs and urogenital gonorrhoea appear promising, and Phase III trials are underway. In this review we summarize the development of gepotidacin and discuss its potential role in clinical practice. If approved, gepotidacin will be the first new oral antibiotic for UTIs in more than 20 years.
抗菌药物耐药性的持续蔓延，使得治疗单纯性尿路感染（UTIs）和泌尿生殖系统淋病越来越困难。迫切需要新的口服治疗选择。 gepotidacin（以前称为 GSK2140944）是一种新型、杀菌、口服、“首创”三氮杂萘并嘧啶类抗生素，通过阻断两种必需的拓扑异构酶来抑制细菌 DNA 复制。发生耐药性可能需要两种酶的突变，因此人们希望该药物能够长期保持有效性。 gepotidacin 在尿路感染和泌尿生殖系统淋病的 II 期临床试验数据令人鼓舞，III 期临床试验正在进行中。在这篇综述中，我们总结了 gepotidacin 的开发情况，并讨论了它在临床实践中的潜在作用。如果获得批准，gpotidacin 将是 20 多年来治疗尿路感染的第一种新型口服抗生素。
