ImportanceCefepime/enmetazobactam is a novel β-lactam/β-lactamase inhibitor combination and a potential empirical therapy for resistant gram-negative infections.ObjectiveTo evaluate whether cefepime/enmetazobactam was noninferior to piperacillin/tazobactam for the primary outcome of treatment efficacy in patients with complicated urinary tract ...
Philipp Knechtle
exaly +5 more sources
Mechanistic basis for inhibition of the extended-spectrum β-lactamase GES-1 by enmetazobactam and tazobactam. [PDF]
β‐Lactamase‐catalysed hydrolysis is the primary form of β‐lactam antibiotic resistance in Gram‐negative bacteria. The penicillanic acid sulfone (PAS) enmetazobactam is thought to inhibit extended‐spectrum β‐lactamases (ESBLs) by fragmentation of an initial acyl‐enzyme to form an active‐site lysinoalanine cross link.
Beer M +10 more
europepmc +4 more sources
Bicyclic Boronate β‐Lactamase Inhibitors: The Present Hope against Deadly Bacterial Pathogens [PDF]
This article highlights the therapeutic potential of recently developed bicyclic boronate inhibitors, such as taniborbactam (VNRX‐5133), VNRX‐7145, and QPX‐7728, for restoring the efficacy of β‐lactam antibiotics against multi‐drug resistant bacteria having distinct resistance mechanisms.
Emilio Lence +1 more
wiley +3 more sources
Cefepime/Enmetazobactam. [PDF]
Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing
Staten AR, Baker DE.
europepmc +5 more sources
P59 Focus on enmetazobactam chemical stability in association with cefepime for prolonged infusions, in syringe and elastomeric diffusers [PDF]
Abstract Background Enmetazobactam, a N-methylated tazobactam derivative is a novel extended-spectrum β-lactamase inhibitor with a unique mechanism that overcomes tazobactam-resistant variants of class A β-lactamases, and is the first β-lactamase inhibitor approved in combination with cefepime in both
Jon Ward +4 more
europepmc +4 more sources
In vitro activity of cefepime-enmetazobactam on carbapenem-resistant Gram negatives
Cefepime-enmetazobactam is a new β-lactam/βlactamase inhibitor combination with broad-spectrum activity against multidrug-resistant Enterobacterales, including extended-spectrum β-lactamase producers. This study evaluated the in vitro activity of cefepime-enmetazobactam towards a collection of carbapenem-resistant Enterobacterales (CRE), Pseudomonas ...
Laurent Dortet
exaly +4 more sources
How Clavulanic Acid Inhibits Serine β‐Lactamases [PDF]
Inhibition of serine β‐lactamases by clavulanic acid occurs via a bifurcating mechanism. The formation of an acyl‐enzyme complex may be followed by hydrolysis, or oxazolidine ring opening and subsequent decarboxylation to give more stable species. Further fragmentation is slow and is less likely to be biologically relevant in inhibition.
Pauline A. Lang +6 more
wiley +3 more sources
β-Lactam/β-Lactamase Inhibitor Combinations in Sepsis-Associated Acute Kidney Injury and Renal Replacement Therapy [PDF]
Sepsis-associated acute kidney injury (SA-AKI) often requires renal replacement therapy (RRT), which markedly alters antimicrobial pharmacokinetics (PK) and pharmacodynamics (PD). Novel β-lactam/β-lactamase inhibitor (BL/BLI) combinations broaden options
Antonio Lacquaniti +10 more
doaj +2 more sources
Real-World Evidence and Multidrug Resistant Infections: How Can We Leverage RWE to Improve Patient Outcome with the Novel Beta-Lactam and Beta-Lactam/Beta-Lactamase Inhibitor Combinations [PDF]
Milo Gatti,1,2 Federico Pea1,2 1Department of Medical and Surgical Sciences, Alma Mater Studiorum University of Bologna, Bologna, Italy; 2Clinical Pharmacology Unit, IRCCS Azienda Ospedaliero-Universitaria Di Bologna, Bologna, ItalyCorrespondence ...
Gatti M, Pea F
doaj +2 more sources
Mechanistic Basis for Inhibition of the Extended Spectrum Class A β-Lactamase GES-1 by Tazobactam and Enmetazobactam [PDF]
AbstractExpression of β-lactamases is the primary form of β-lactam antibiotic resistance in Gram-negative bacteria. Enmetazobactam is a penicillanic acid sulfone (PAS) that inhibits extended spectrum β-lactamases (ESBLs) by forming an acyl-enzyme complex that eventually breaks down to an irreversible lysinoalanine crosslink. In contrast, enmetazobactam
Beer M +10 more
europepmc +3 more sources

