Phase 1 study of the safety, tolerability, and pharmacokinetics of the β-lactamase inhibitor vaborbactam (RPX7009) in healthy adult subjects

DC Griffith, JS Loutit, EE Morgan, S Durso… - Antimicrobial agents …, 2016 - Am Soc Microbiol
Vaborbactam (formerly RPX7009) is a member of a new class of β-lactamase inhibitor with
pharmacokinetic properties similar to those of many β-lactams, including carbapenems. The …

Class A β-lactamases—enzyme-inhibitor interactions and resistance

Y Yang, BA Rasmussen, DM Shlaes - Pharmacology & therapeutics, 1999 - Elsevier
β-Lactamases of Ambler's Class A are the most commonly encountered mechanism of
bacterial resistance to β-lactam antibiotics. In the face of selective pressure arising from use …

The discovery and development of modified penicillin-and cephalosporin-derived β-lactamase inhibitors

JD Buynak - Current medicinal chemistry, 2004 - ingentaconnect.com
While β-lactam antibiotics remain among the most commonly prescribed pharmaceutical
products, their effectiveness is currently threatened by the development of bacterial …

Molecular targets of β-lactam-based antimicrobials: beyond the usual suspects

MI Konaklieva - Antibiotics, 2014 - mdpi.com
The common practice in antibacterial drug development has been to rapidly make an
attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once …

Recent developments in β-lactamase research and their implications for the future

K Bush - Clinical Infectious Diseases, 1988 - academic.oup.com
Abstract β-Lactamases, major determinants of bacterial resistance to β-lactam antibiotics,
can be classified into specific molecular classes following identification of active-site amino …

Clinical role of β-lactam/β-lactamase inhibitor combinations

N Lee, KY Yuen, CR Kumana - Drugs, 2003 - Springer
The use of β-lactamase inhibitors in combination with β-lactam antibiotics is currently the
most successful strategy to combat a specific resistance mechanism. Their broad spectrum …

Discovery of cyclic boronic acid QPX7728, an ultrabroad-spectrum inhibitor of serine and metallo-β-lactamases

SJ Hecker, KR Reddy, O Lomovskaya… - Journal of medicinal …, 2020 - ACS Publications
Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory
to inhibition by agents recently introduced. Most important among these are the class B …

Extended‐spectrum β‐lactamases: epidemiology, detection, and treatment

S Nathisuwan, DS Burgess… - … : The Journal of Human …, 2001 - Wiley Online Library
Extended‐spectrum β‐lactamases (ESBLs) are extremely broad spectrum β‐lactamase
enzymes found in a variety of Enterobacteriaceae. Most strains producing these β …

[HTML][HTML] Version 2000: the new β-lactamases of Gram-negative bacteria at the dawn of the new millennium

KS Thomson, ES Moland - Microbes and infection, 2000 - Elsevier
β-lactamases of Gram-negative bacteria are evolving dynamically. New developments
include the production of enzymes with novel substrate profiles, reduced susceptibility to β …

Bicyclic boronate VNRX-5133 inhibits metallo-and serine-β-lactamases

A Krajnc, J Brem, P Hinchliffe, K Calvopiña… - Journal of Medicinal …, 2019 - ACS Publications
The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in
clinical development. We report that VNRX-5133 inhibits serine-β-lactamases (SBLs) and …