Relebactam is a compound used in combination wtih antibiotics to improve their efficiency. It is a β-lactamase inhibitor that has the 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 as imipenem/cilastatin/relebactam. Relebactam is soluble in water and DMSO. It is insoluble in ethanol.
|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.
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 infections caused by Enterobacteriaceae having complex β-lactamase backgrounds.
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