Drug intelligence / Profile preview

LK-157

Development stage
Unknown
Lead developer
Nabriva Therapeutics
Modality
Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
01

Overview

LK‑157 is a synthetic small molecule belonging to the trinem class of beta-lactamase inhibitors. It was designed as part of a series of 4-substituted trinems to address bacterial resistance mediated by beta-lactamases—enzymes that hydrolyze and inactivate beta-lactam antibiotics. LK‑157 acts as a mechanism-based inactivator targeting class C (AmpC) and class A beta-lactamases by acylating the active site serine residue (Ser64), thereby inhibiting enzyme activity and restoring the efficacy of co-administered beta-lactam antibiotics. The compound has demonstrated significant in vitro inhibitory activity against these enzymes but is not itself an antibiotic; rather it serves as an adjunctive agent to overcome resistance[3][7].

Other names
(1R,4S,7AS)-1-(1-formylprop-1-en-1-yl)-4-methoxy-2,4,5,6,7,7a-hexahydro-1H-isoindole-3-carboxylic acid4-methoxy-2,4,5,6,7,7a-hexahydro-1H-Isoindole derivative
02

Targets

SHV-1 (SHV-1 beta-lactamase)CD248 (Endosialin)AmpC (AmpC beta-lactamase)

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