Zidebactam

China [CN]

Mechanism of Action

Dual Mechanism of Action

It binds with high affinity to penicillin-binding protein 2 (PBP2) in Gram-negative bacteria, inhibiting bacterial cell wall synthesis, inducing spheroplast formation, and leading to bacterial death.

It inhibits Ambler class A and C β-lactamases, protecting cefepime from hydrolysis. It is stable against class B metallo-β-lactamases and class D carbapenemases, and can exert its effect without relying on β-lactamase inhibitors.

Clinical Applications and Development Progress

Combination preparation: WCK5222, a combination of cefepime and this drug in a 1:1 ratio, is used to treat complex urinary tract infections (including acute pyelonephritis) and hospital-acquired pneumonia in adults.

Progress in China: Received NMPA clinical approval in 2022 for the treatment of complex urinary tract infections (including acute pyelonephritis) in adults.

Global progress: Currently in Phase III clinical trials, showing broad-spectrum in vitro activity against multidrug-resistant strains producing ESBL, KPC, MBL, etc. (such as Pseudomonas aeruginosa and Acinetobacter baumannii) (NCBI).