Drug intelligence / Profile preview

ceftibuten + avibactam-tomilopil

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**Ceftibuten + avibactam-tomilopil** is an investigational oral combination of the third-generation cephalosporin ceftibuten and tomilopil, an orally absorbed prodrug of avibactam (ARX-1796/AV-006), a diazabicyclooctane β-lactamase inhibitor. Ceftibuten binds to penicillin-binding proteins to inhibit bacterial cell wall synthesis, while avibactam covalently inhibits class A (e.g., KPC, ESBLs), C (e.g., AmpC), and some class D (e.g., OXA-48) serine β-lactamases, restoring ceftibuten's activity against resistant Gram-negative Enterobacterales, including multidrug-resistant and carbapenem-resistant strains (CRE). Developed by Arixa Pharmaceuticals in partnership with Pfizer, it targets complicated urinary tract infections (cUTI) and other infections caused by β-lactam-resistant pathogens, offering a much-needed oral option where few alternatives exist, with potent in vitro activity (MIC50/90 often ≤0.03/0.06 mg/L at 1-4 mg/L avibactam) but inactivity against metallo-β-lactamases (e.g., NDM).[1][2][3][4][8]

Other names
ceftibuten-avibactamceftibuten/avibactam
02

Targets

AmpC (AmpC beta-lactamase)OXA (Class D beta-lactamase)Class A BL (Class A beta-lactamase)PBP (Penicillin-binding protein family)

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