Xeruborbactam
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| Clinical data | |
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| Synonyms | QPX7728 |
| Routes of administration | Intravenous (IV); Oral (as prodrug combination) |
| Drug class | β-lactamase inhibitor |
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| ChEMBL | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}} |
| Chemical and physical data | |
| Formula | C10H8BFO4 |
| Molar mass | 221.98 g·mol−1 |
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Xeruborbactam (research code QPX7728) is an investigational new drug that is being evaluated by Qpex Biopharma for the treatment of infections caused by multidrug-resistant gram-negative bacteria. It is a a bicyclic boronate β-lactamase inhibitor (BLI) that is active against both serine and metallo-β-lactamases (MBLs).[1]
Discovery
Xeruborbactam was first reported in 2020 as a cyclic boronic acid derivative with ultrabroad-spectrum inhibitory activity.[2]
Mechanism of action
Xeruborbactam acts as a transition state analog inhibitor, forming reversible covalent interactions with serine β-lactamases and coordinating with zinc ions in metallo-β-lactamases. This dual mechanism enables inhibition across all four Ambler classes (A–D), including KPC, OXA, and NDM enzymes.
Spectrum of activity
The compound restores β-lactam efficacy against Enterobacterales, Pseudomonas aeruginosa, and Acinetobacter baumannii producing extended-spectrum β-lactamases and carbapenemases. It is active in combination with β-lactams such as ceftibuten, cefepime, and meropenem.[3]
Clinical development
Xeruborbactam is being developed in both intravenous and oral formulations. The oral version is administered as a prodrug in combination with ceftibuten. Ongoing Phase 1 trials include:
| NCT Number | Trial Title/Description | Clinical Phase |
|---|---|---|
| NCT07083817 | Mass Balance Study of [14C]Xeruborbactam (QPX7728) in Healthy Adult Male Participants | Phase 1 |
| NCT06079775 | P1, DDI & MAD PK and Safety Study of Xeruborbactam Oral Prodrug in Combo With Ceftibuten in Healthy Participants | Phase 1 |
| NCT06547554 | DDI Study to Investigate PK and Safety of Cefiderocol/Xeruborbactam in Healthy Adults | Phase 1 |
| NCT07104162 | A Study to Investigate Safety and PK of IV Cefiderocol/Xeruborbactam Combination | Phase 1 |
| NCT04380207 | P1 SAD/MAD Study of QPX7728 (IV/oral xeruborbactam) alone or with QPX2014 in Healthy Volunteers | Phase 1 |
See also
References
- ↑ Lomovskaya O, Tsivkovski R, Sun D, Reddy R, Totrov M, Hecker S, Griffith D, Loutit J, Dudley M (2021). "QPX7728, An Ultra-Broad-Spectrum B-Lactamase Inhibitor for Intravenous and Oral Therapy: Overview of Biochemical and Microbiological Characteristics". Frontiers in Microbiology. 12. doi:10.3389/fmicb.2021.697180. PMC 8287861 Check
|pmc=value (help). PMID 34290688 Check|pmid=value (help). Unknown parameter|article-number=ignored (help) - ↑ Hecker SJ, Reddy KR, Lomovskaya O, Griffith DC, Rubio-Aparicio D, Nelson K, Tsivkovski R, Sun D, Sabet M, Tarazi Z, Parkinson J, Totrov M, Boyer SH, Glinka TW, Pemberton OA, Chen Y, Dudley MN (July 2020). "Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases". Journal of Medicinal Chemistry. 63 (14): 7491–7507. doi:10.1021/acs.jmedchem.9b01976. PMID 32150407 Check
|pmid=value (help). - ↑ Lomovskaya O, Castanheira M, Lindley J, Rubio-Aparicio D, Nelson K, Tsivkovski R, Sun D, Totrov M, Loutit J, Dudley M (November 2023). "In vitro potency of xeruborbactam in combination with multiple β-lactam antibiotics in comparison with other β-lactam/β-lactamase inhibitor (BLI) combinations against carbapenem-resistant and extended-spectrum β-lactamase-producing Enterobacterales". Antimicrobial Agents and Chemotherapy. 67 (11). doi:10.1128/aac.00440-23. PMC 10648875 Check
|pmc=value (help). PMID 37800963 Check|pmid=value (help). Unknown parameter|article-number=ignored (help)
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