Jacobs Michael R, Good Caryn E, Abdelhamed Ayman M, Mack Andrew R, Bethel Christopher R, Marshall Steven H, Hujer Andrea M, Hujer Kristine M, Patel Robin, van Duin David, Fowler Vance G, Rhoads Daniel D, Six David A, Moeck Greg, Uehara Tsuyoshi, Papp-Wallace Krisztina M, Bonomo Robert A
Case Western Reserve University, Cleveland, Ohio, USA.
University Hospitals Cleveland Medical Center, Cleveland, Ohio, USA.
Antimicrob Agents Chemother. 2024 Dec 5;68(12):e0112724. doi: 10.1128/aac.01127-24. Epub 2024 Oct 30.
Ledaborbactam (formerly VNRX-5236), a bicyclic boronate β-lactamase inhibitor with activity against class A, C, and D β-lactamases, is under development as an orally bioavailable etzadroxil prodrug (VNRX-7145) in combination with ceftibuten for the treatment of urinary tract infections. At ceftibuten breakpoints of ≤1 mg/L (EUCAST) and ≤8 mg/L (CLSI), 92.5% and 99.0%, respectively, of 200 carbapenem-resistant isolates, predominantly carbapenemase producing, were susceptible to ceftibuten-ledaborbactam (ledaborbactam tested at a fixed concentration of 4 mg/L) compared to 4.5% and 30.5%, respectively, to ceftibuten alone.
来达硼巴坦(曾用名VNRX - 5236)是一种双环硼酸酯β - 内酰胺酶抑制剂,对A类、C类和D类β - 内酰胺酶具有活性,目前正作为一种口服生物利用度良好的依扎曲沙星前药(VNRX - 7145)与头孢布烯联合开发,用于治疗尿路感染。在头孢布烯≤1 mg/L(欧洲药敏试验委员会)和≤8 mg/L(美国临床和实验室标准协会)的断点浓度下,200株耐碳青霉烯类菌株(主要产碳青霉烯酶)中,分别有92.5%和99.0%对头孢布烯 - 来达硼巴坦(来达硼巴坦固定浓度为4 mg/L)敏感,而单独使用头孢布烯时敏感率分别为4.5%和30.5%。