Drug intelligence / Profile preview

esomeprazole + bismuth + amoxicillin + tetracycline + furazolidone

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of five agents—esomeprazole, bismuth, amoxicillin, tetracycline, and furazolidone—used primarily for the eradication of Helicobacter pylori infection. Each component has a distinct mechanism: - Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by inhibiting the H+/K+ ATPase in gastric parietal cells. - Bismuth compounds have antimicrobial activity against H. pylori and protect the gastric mucosa. - Amoxicillin is a broad-spectrum beta-lactam antibiotic that inhibits bacterial cell wall synthesis. - Tetracycline is a broad-spectrum antibiotic that inhibits protein synthesis by binding to the 30S ribosomal subunit. - Furazolidone is a nitrofuran antibacterial agent with additional monoamine oxidase inhibitor (MAOI) activity; it interferes with bacterial enzyme systems and has activity against both bacteria and protozoa. This multi-drug regimen targets H. pylori through multiple mechanisms to overcome resistance and improve eradication rates, especially in regions where standard therapies are less effective or resistance rates are high[6][8][10]. Furazolidone's inclusion provides an alternative for cases resistant to other antibiotics[6].

02

Targets

Hpn/HspA (Helicobacter pylori Hpn/HspA metal-binding proteins)Bacterial RibosomeNTR (Bacterial nitroreductase)MAOA (Monoamine oxidase A)ATP4A (Potassium–transporting ATPase alpha chain 1)UreasePBP (Penicillin-binding protein family)

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