Drug intelligence / Profile preview

ceftibuten + ledaborbactam etzadroxil

Development stage
Unknown
Lead developer
Basilea Pharmaceutica
Modality
Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Ceftibuten + ledaborbactam etzadroxil is an investigational fixed-dose oral combination of the third-generation cephalosporin antibiotic ceftibuten and the orally bioavailable prodrug beta-lactamase inhibitor ledaborbactam etzadroxil (formerly VNRX-7145). Ledaborbactam is a boronic acid-based inhibitor that, after conversion from its prodrug form, covalently and reversibly inhibits Ambler class A, C, and D serine beta-lactamases. This restores the activity of ceftibuten against multidrug-resistant Enterobacterales—including those producing extended-spectrum beta-lactamases (ESBLs), KPC carbapenemases, OXA-type enzymes, and AmpC enzymes—that are resistant to standard oral or intravenous antibiotics. The combination is being developed primarily for complicated urinary tract infections (cUTI), including acute pyelonephritis and infections caused by carbapenem-resistant Enterobacteriaceae. It is currently in Phase I clinical trials as an oral therapy option for drug-resistant Gram-negative bacterial infections[1][3][4][7].

Brand names
VNRX-7145 + ceftibuten
Other names
ceftibuten-ledaborbactam etzadroxilceftibuten + ledaborbactam etzadroxil
02

Targets

PBP (Penicillin-binding protein family)Neuraminidase

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