Biology:Pilabactam
From HandWiki
Pilabactam is an beta-lactamase inhibitor that is being evaluated by Antabio as an antiinfective.[1][2][3]
Chemistry
The first in class non-β-lactam β-lactamase inhibitor avibactam contains a strained urea functional group within the diazabicyclooctane (DBO) ring system. This strained urea acts as a warhead that reacts with the active site serine residue in β-lactamases. Other drugs in this class include relebactam, durlobactam, nacubactam and zidebactam.[2] However none of these are active against carbapenem-resistant Acinetobacter baumannii. (CRAB). Pilabactam contains a fluorine atom that replaces a carboxamide group in the other DBOs and restores CRAB sensitivity.[2]
See also
- Diazabicyclooctane β-lactamase inhibitor
References
- ↑ "MEM ANT 3310". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800058516.
- ↑ 2.0 2.1 2.2 "Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii". Journal of Medicinal Chemistry 63 (24): 15802–15820. December 2020. doi:10.1021/acs.jmedchem.0c01535. PMID 33306385.
- ↑ "Disarming carbapenemase-producing Acinetobacter baumannii: high potency of the novel therapeutic combination of meropenem and the innovative diazabicyclooctane β-lactamase inhibitor pilabactam (formerly ANT3310)". Antimicrobial Agents and Chemotherapy 70 (4). April 2026. doi:10.1128/aac.01691-25. PMID 41711564.
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