Drug intelligence / Profile preview

vaborbactam

Development stage
Phase 3
Lead developer
Rempex Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

Vaborbactam is a small molecule, non-β-lactam β-lactamase inhibitor based on a cyclic boronic acid pharmacophore. It was discovered by Rempex Pharmaceuticals (a subsidiary of The Medicines Company) and is used in combination with meropenem for the treatment of complicated urinary tract infections (cUTI), including kidney infections. Vaborbactam itself has no antibacterial activity but restores the efficacy of meropenem by inhibiting serine β-lactamases, particularly Klebsiella pneumoniae carbapenemase (KPC) and other class A and C β-lactamases. Its mechanism involves forming a covalent adduct with the catalytic serine residue in these enzymes, mimicking the tetrahedral transition state of hydrolysis and thereby preventing antibiotic degradation[2][5][6]. The combination product is marketed as Vabomere.

Brand names
Vabomere
02

Targets

SHV-12 (SHV-12 serine beta-lactamase)AmpC (AmpC beta-lactamase)KPC-2 (Klebsiella pneumoniae carbapenemase-2)OXA-48 (OXA-48 beta-lactamase)VIM-1 (VIM-1 metallo-beta-lactamase)CMY-2 (Beta-lactamase CMY-2)KPC-3 (KPC-3 beta-lactamase)CTX-M-15 (CTX-M-15 beta-lactamase)IGF2BP1NDM-1 (NDM-1 beta-lactamase)

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