Drug intelligence / Profile preview

tigemonam

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Tigemonam is an orally active monocyclic β-lactam antibiotic, specifically a monobactam, developed by E. R. Squibb and Sons (now Bristol Myers Squibb). It was designed to target gram-negative aerobic bacterial pathogens, including members of the Enterobacteriaceae family, *Haemophilus influenzae*, and *Neisseria gonorrhoeae*. Its mechanism of action involves the inhibition of bacterial penicillin-binding proteins (PBPs), which disrupts cell wall synthesis. Tigemonam demonstrates significant stability against hydrolysis by many beta-lactamases and exhibits an antibacterial spectrum similar to aztreonam but with the advantage of oral bioavailability when formulated as its dicholine salt (SQ 30836). Despite showing excellent in vitro and in vivo activity against gram-negative bacteria in preclinical studies, the drug's development was discontinued before reaching clinical use.

Other names
tigemonam dicholine
02

Targets

PBP1A (Penicillin-binding protein 1A)

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