Drug intelligence / Profile preview

CPZEN-45

Development stage
Unknown
Lead developer
Institute of Microbial Chemistry
Modality
Small Molecules
Administration
Inhalation, Intramuscular
01

Overview

CPZEN-45 is a semi-synthetic nucleoside antibiotic and a derivative of caprazamycin, specifically developed for the treatment of tuberculosis (TB). It targets the bacterial enzyme MraY (phospho-MurNAc-pentapeptide translocase), which is essential for the biosynthesis of the peptidoglycan layer of the bacterial cell wall. By inhibiting MraY, CPZEN-45 prevents the formation of Lipid I, thereby disrupting cell wall assembly and leading to bacterial cell death. This mechanism is distinct from existing TB therapies, allowing CPZEN-45 to maintain efficacy against multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of *Mycobacterium tuberculosis*. Preclinical studies have demonstrated its effectiveness against both actively replicating and dormant mycobacteria. The compound was developed by the Institute of Microbial Chemistry (BIKAKEN) in Japan and has been evaluated for delivery via inhalation to target the primary site of infection in the lungs.

02

Targets

MraY (Phospho-N-acetylmuramoyl-pentapeptide-transferase)WecA (UDP-N-acetylglucosamine 1-phosphate transferase)

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