Relebactam is a compound used in combination with antibiotics to improve their efficiency. It is a β-lactamase inhibitor with a diazbicyclooctane core. It has activity against a wide spectram 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. The compound can be used in combination (imipenem/cilastatin/relebactam).
Relebactam is soluble in water and DMSO but insoluble in ethanol.
| Molecular Formula | C12H20N4O6S |
| Spectrum | Relebactam has activity against a wide spectrum of β-lactamases including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes |
| 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 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 clinically important class A serine B-lactamases (SBLs) representing both chromosomal and plasmid-borne enzymes (Tooke et al, 2019). Imipenem-Relebactam can be used for Enterobacteriaceae having complex β-lactamase backgrounds. |
| References |
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):e00564-19 |
