Relebactam Monohydrate is a β-lactamase inhibitor that has the diazbicyclooctane core. It has a similar structure to avibactam. It has activity against a wide spectrum of β-lactamases including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes. The R1 side chain of Relebactam includes a piperidine ring. It can be used to inhibit the breakdown of certain compounds, such as the broad spectrum beta-lactam carbapenem antibiotic imipenem. Relebactam targets, binds to and inhibits beta-lactamase. This reduces the breakdown of compounds like imipenem, and thereby increases the activity and effect of such compounds that would otherwise be inactivated by beta-lactamase. The compound can be used in combination with imipenem (ie imipenem/cilastin/relebactam).
Relebactam Monohydrate is soluble in DMSO.
| Molecular Formula | C12H20N4O6S x H2O |
| Mechanism of Action | Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases. |
| Microbiology Applications |
Relebactam is a non-β-lactam antimicrobial of the diazabicyclo[3.2.1]octanone (DBO) series. It inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. Relebactam inhibits 5 important class A serine B-lactamases (SBLs) representing both chromosomal and plasmid-borne enzymes (Tooke et al, 2019). Imipenem-Relebactam can be used against Enterobacteriaceae with complex β-lactamase backgrounds. Relebactam, when combined with imipenem, restores imipenem's activity against nonsusceptible isolates and enhances imipenem activity, specifically against susceptible Pseudomonas aeruginosa isolates. |
| References |
Hilbert DW, DeRyke CA, Motyl M(2023) Relebactam restores susceptibility of resistant Pseudomonas aeruginosa and Enterobacterales and enhances imipenem activity against chromosomal AmpC-producing species: Analysis of global SMART 2018–2020. BMC Microbiol. 23:165 Lang PA, Leissing TM, Page MGP, Schofield CJ, Brem J (2021) Structural investigations of the inhibition of Escherichia coli AmpC β-Lactamase by Diazabicyclooctanes. Antimicrob. Agents Chemother. 65(2):e02073-20 PMID 33199391 Papp-Wallace KM et al (2018) Relebactam is a potent inhibitor of the KPC-2 β-Lactamase and restores imipenem susceptibility in KPC-producing Enterobacteriaceae. Antimicrob. Agents Chemother. 62(6):e00174-18. PMID: 29610205 Tooke CL et al (2019) Molecular basis of class A β-lactamase inhibition by Relebactam. Antimicrobial Agents Chemother. 63(10):e00564-1
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