Kern Winfried V, Gatermann Sören G
Klinik für Innere Medizin II/Abteilung Infektiologie, Universitätsklinikum Freiburg, Hugstetter Str. 55, 79106, Freiburg, Deutschland.
Institut für medizinische Mikrobiologie, Universität Bochum, Bochum, Deutschland.
Inn Med (Heidelb). 2025 Aug 28. doi: 10.1007/s00108-025-01970-w.
Numerous new developments in antibacterial substances have been observed in recent years. Most of these are further developments of existing classes, especially beta-lactams, including beta-lactamase inhibitors. These included MRSA-active cephalosporins (ceftaroline and ceftobiprole), new, broadly effective combinations of beta-lactams with beta-lactamase inhibitors, and cefiderocol, a new siderophore cephalosporin that uses the bacteria's own iron uptake systems of gram-negative bacteria to better reach the site of action through the outer membrane.In addition to cefiderocol, the most important active ingredients or fixed combinations already available on the German market include ceftazidime-avibactam, ceftolozane-tazobactam, and aztreonam-avibactam. Imipenem-relebactam and meropenem-vaborbactam are also available; Cefepim-enmetazobactam was recently added. The spectra of these substances are different. Cefiderocol and, in the case of Enterobacterales, Aztreonam-Avibactam are suitable for the treatment of infections caused by Gram-negative bacteria with metallo-beta-lactamases.A further development in the field of betalactamase inhibitors are the boronate-based active ingredients, which can inhibit bacterial ESBL enzymes, carbapenemases of the KPC, OXA-48 and partly OXA-23 type, as well as metallo-beta-lactamases. There are few new or newly initiated developments in the field of oral beta-lactams. However, the oral carbapenems, penems, and trinems could become a kind of milestone in the treatment of mycobacteriosis. On the other hand, fixed combinations of beta-lactams plus beta-lactamase inhibitor for the oral treatment of infections caused by ESBL-positive bacteria, some of which are already available abroad (such as cefpodoxime clavulanic acid), are missing. However, interesting new combinations, such as ceftibutene-avibactam for oral use, are in development. Such combinations could also enable the oral treatment of infections by some carbapenemase producers in the future.
近年来，抗菌物质出现了许多新进展。其中大多数是现有类别药物的进一步研发成果，尤其是β-内酰胺类药物，包括β-内酰胺酶抑制剂。这些药物包括对耐甲氧西林金黄色葡萄球菌（MRSA）有效的头孢菌素（头孢洛林和头孢比普）、新型的、疗效广泛的β-内酰胺类与β-内酰胺酶抑制剂的联合用药，以及头孢地尔，一种新型的铁载体头孢菌素，它利用革兰氏阴性菌自身的铁摄取系统，通过外膜更好地到达作用部位。除头孢地尔外，德国市场上已有的最重要的活性成分或固定组合包括头孢他啶-阿维巴坦、头孢托仑-他唑巴坦和氨曲南-阿维巴坦。亚胺培南-瑞来巴坦和美罗培南-万巴巴坦也已上市；头孢吡肟-恩美他唑巴坦最近也已加入。这些药物的抗菌谱各不相同。头孢地尔以及对于肠杆菌科细菌感染而言的氨曲南-阿维巴坦，适用于治疗由产金属β-内酰胺酶的革兰氏阴性菌引起的感染。β-内酰胺酶抑制剂领域的进一步发展是基于硼酸盐的活性成分，它们可以抑制细菌的超广谱β-内酰胺酶（ESBL）、KPC型、OXA-48型以及部分OXA-23型碳青霉烯酶，还有金属β-内酰胺酶。口服β-内酰胺类药物领域几乎没有新的或新启动的研发进展。然而，口服碳青霉烯类、青霉烯类和三烯类药物可能成为治疗分枝杆菌病的一个里程碑。另一方面，用于口服治疗由产ESBL细菌引起感染的β-内酰胺类加β-内酰胺酶抑制剂的固定组合尚不存在，其中一些在国外已有上市（如头孢泊肟酯-克拉维酸）。不过，有趣的新组合，如口服用的头孢布烯-阿维巴坦正在研发中。这类组合未来或许也能实现对一些产碳青霉烯酶细菌感染的口服治疗。
