Drug intelligence / Profile preview

BLI-489

Development stage
Phase 1
Lead developer
Pfizer
Modality
Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

BLI‑489 is a novel bicyclic penem β-lactamase inhibitor developed by Wyeth for the treatment of bacterial infections and urinary tract infections. It acts by inhibiting class A and class C as well as some class D β-lactamases, thereby restoring the activity of partner β-lactam antibiotics against resistant bacteria. BLI‑489 has demonstrated synergistic effects in combination with antibiotics such as piperacillin, imipenem, and meropenem against carbapenem-resistant Enterobacterales (CRE) and other multidrug-resistant Gram-negative pathogens in both in vitro and in vivo models. Despite promising preclinical data showing improved efficacy over existing combinations like piperacillin-tazobact—especially against extended-spectrum beta-lactamase (ESBL)-producing strains—development was discontinued before approval[1][5][6][7][8].

Other names
6-methylidene-penem β-lactamase inhibitor6-[(5,6-Dihydro-8H-imidazo[2,1-c][1,4]oxazin-2-yl)methylene]-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid sodium salt hydrate
02

Targets

Neuraminidase

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