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格派沙星:首个获批用于治疗单纯性尿路感染的新型三氮杂蒽类抗生素。

Gepotidacin: The first-in-class triazaacenaphthylene antibiotic approved for the treatment of uncomplicated urinary tract infections.

作者信息

Hu Shasha, Yu Haizhou, Gao Jianjun

机构信息

Department of Pathology, The Affiliated Hospital of Qingdao University, Qingdao, Shandong, China.

Department of Anesthesiology, Weihai Central Hospital Affiliated with Qingdao University, Weihai, Shandong, China.

出版信息

Drug Discov Ther. 2025 May 9;19(2):129-130. doi: 10.5582/ddt.2025.01028. Epub 2025 Apr 11.

DOI:10.5582/ddt.2025.01028
PMID:40222947
Abstract

Uncomplicated urinary tract infection (uUTI) is a common bacterial infection in women. While the condition typically has a favorable prognosis, the widespread use of antibiotics has led to increasingly bacterial resistance, reducing the efficacy of traditional antibiotics. On March 25, 2025, the US Food and Drug Administration approved gepotidacin for the treatment of uUTIs caused by susceptible bacteria in female adult and pediatric patients 12 years of age and older weighing at least 40 kg. Gepotidacin is the first triazaacenaphthylene antibiotic approved for clinical use. It selectively binds to and inhibits both bacterial DNA gyrase and topoisomerase IV, disrupting bacterial DNA replication through a unique mechanism and thereby killing the pathogen. Results of clinical trials indicated the non-inferiority of gepotidacin compared to the current standard therapy, nitrofurantoin. The most frequently reported adverse reaction to gepotidacin was mild to moderate diarrhea. The approval of gepotidacin represents a progress in antibiotic innovation, offering novel perspectives on drug development while spurring global efforts to tackle the escalating challenge of antimicrobial resistance.

摘要

单纯性尿路感染(uUTI)是女性常见的细菌感染。虽然这种疾病通常预后良好,但抗生素的广泛使用导致细菌耐药性日益增加,降低了传统抗生素的疗效。2025年3月25日,美国食品药品监督管理局批准了格派沙星用于治疗12岁及以上、体重至少40kg的成年女性和儿科患者中由易感细菌引起的uUTI。格派沙星是首个获批用于临床的三氮杂萘类抗生素。它选择性地结合并抑制细菌DNA旋转酶和拓扑异构酶IV,通过独特机制破坏细菌DNA复制,从而杀死病原体。临床试验结果表明,与当前标准疗法呋喃妥因相比,格派沙星并不逊色。格派沙星最常报告的不良反应是轻度至中度腹泻。格派沙星的获批代表了抗生素创新的一项进展,为药物研发提供了新视角,同时激励全球努力应对日益严峻的抗菌药物耐药性挑战。

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