Antimicrobial resistance continues to challenge the clinical efficacy of established antibiotics, highlighting the need for innovative therapeutic strategies. Cefepime/zidebactam combines a fourth-generation cephalosporin with a novel diazabicyclooctane β-lactamase inhibitor endowed with intrinsic PBP2-targeting activity. This commentary discusses the pharmacology, mechanism of action, and medicinal chemistry of zidebactam, focusing on its distinctive peculiarities. Complementary PBP2/PBP3 targeting, together with serine β-lactamase inhibition, provides a multifaceted strategy to restore and enhance β-lactam activity against resistant pathogens.
Zidebactam as a new approved β-Lactamase inhibitor with intrinsic antibacterial activity via PBP2 binding / Pieroni, M.. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - (2026). [10.1007/s00044-026-03636-0]
Zidebactam as a new approved β-Lactamase inhibitor with intrinsic antibacterial activity via PBP2 binding
Pieroni, Marco
2026-01-01
Abstract
Antimicrobial resistance continues to challenge the clinical efficacy of established antibiotics, highlighting the need for innovative therapeutic strategies. Cefepime/zidebactam combines a fourth-generation cephalosporin with a novel diazabicyclooctane β-lactamase inhibitor endowed with intrinsic PBP2-targeting activity. This commentary discusses the pharmacology, mechanism of action, and medicinal chemistry of zidebactam, focusing on its distinctive peculiarities. Complementary PBP2/PBP3 targeting, together with serine β-lactamase inhibition, provides a multifaceted strategy to restore and enhance β-lactam activity against resistant pathogens.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
