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xeruborbactam isoboxil
- Development stage
- Phase 1
- Lead developer
- Shionogi
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Xeruborbactam isoboxil** is an orally bioavailable prodrug of xeruborbactam (formerly QPX7728), a cyclic boronate-based ultra-broad-spectrum beta-lactamase inhibitor that potently inhibits both serine (classes A, C, D) and metallo-beta-lactamases (class B). Developed by Qpex Biopharma (acquired by Shionogi in 2023), it is designed for combination with oral beta-lactam antibiotics like ceftibuten (as S-743229) to treat infections caused by multidrug-resistant Gram-negative bacteria, including carbapenem-resistant Enterobacterales (CRE), Acinetobacter baumannii, and Pseudomonas aeruginosa, in outpatient settings. Beyond beta-lactamase inhibition, xeruborbactam exhibits direct antibacterial activity at higher concentrations by binding to penicillin-binding proteins (PBPs), enhancing beta-lactam potency even in beta-lactamase-negative strains. It is currently in Phase 1 clinical development supported by BARDA.
- Other names
- xeruborbactam prodrug
02
Targets
NeuraminidasePBP1A (Penicillin-binding protein 1A)PBP2 (Penicillin-binding protein 2)PBP3 (Peptidoglycan D,D-transpeptidase FtsI)PBP1b (Penicillin-binding protein 1B)β-lactamase
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