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<p>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&#xa0;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.</p><p>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.</p><p>A&#xa0;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&#xa0;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.</p>

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Betalaktame und Betalaktamase-Inhibitoren – aktuelle Entwicklungen

  • 期刊论文

  • 发表日期：

    2025年8月28日

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  • Winfried V. Kern,
  • Sören G. Gatermann

摘要

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.