Meropenem Vaborbactam (1:1 mixture) is a mixture of Meropenem (a carbapenem antibiotic) and Vaborbactam (a cyclic, boronic acid-based, non-suicidal, reversible beta-lactamase inhibitor). It is active against the bacteria causing complicated urinary tract infections including acute pyelonephritis. It was developed by Rempex.
|Mechanism of Action|| |
Meropenem penetrates the bacterial cell wall and binds penicillin-binding protein (PBP) and inhibits the cross-linking of peptidoglycan chains leading to cell lysis and death. It is stable in the presence of many beta-lactamases due to its 6-trans-hydroxyethylgroup. Vaborbactam alone has no antibacterial activity . The addition of the boronate ester improves substrate activity against beta-lactamases. Vaborbactam protects Meropenem from degradation by certain serine beta-lactamases such as Klebsiella pneumoniae carbapenemase (KPC). When in combination, the antimicrobial activity is similar to meropenem.
Resistance may involve porin mutations combined with overexpression of efflux pumps, but research has shown variable results.
|Spectrum||Meropenem Vaborbactam is active against Gram-positive and Gram-negative bacteria including carbapenem-resistant Enterobacteriaceae (CRE). It is also effective against E. coli, Klebsiella pneumoniae, and Enterobacter cloacae species complex.|
|Microbiology Applications|| |
Meropenem Vaborbactam is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips), specifically Oxoid discs, Sensititre, and ETEST. Medical microbiologists use AST results to recommend antibiotic treatment options.
Cho JC, Zmarlicka MT, Shaeer KM, and Pardo J (2018) Meropenem/Vaborbactam, the first Carbapenem/β-Lactamase inhibitor combination. Ann Pharmacother. 52(8):769-779 PMID 29514462
Petty LA, Henig O, Patel TS, Pogue JM and Kaye KS (2018) Overview of meropenem-vaborbactam and newer antimicrobial agents for the treatment of carbapenem-resistant Enterobacteriaceae. Infect. Drug Resis. 11:1461-1472. PMID 30254477
Pfaller MA, Huband MD, Mendes RE, FLamm RK and Castanheira MA (2018) In vitro activity of meropenem/vaborbactam and characterisation of carbapenem resistance mechanisms among carbapenem-resistant Enterobacteriaceae from the 2015 meropenem/vaborbactam surveillance programme. Int. J. Antimicrob. Agents 52(2):144-150
Weiss WJ et al (2017) Activity of Meropenem-Vaborbactam against carbapenem-resistant Enterobacteriaceae in a murine model of pyelonephritis. Antimicrob. Agents. Chemother. 62 (1) e01439-17