Drug intelligence / Profile preview

bismuth subcitrate + esomeprazole + clarithromycin + amoxicillin + metronidazole

Development stage
Unknown
Lead developer
First Affiliated Hospital of Nanchang University
Modality
Small Molecules
Administration
Oral
01

Overview

This five-drug combination regimen is an intensive therapeutic approach designed for the eradication of *Helicobacter pylori* infection, particularly in regions with high antibiotic resistance. Developed and extensively studied by researchers at The First Affiliated Hospital of Nanchang University, the regimen consists of a proton pump inhibitor (esomeprazole), a bismuth salt (bismuth subcitrate), and three antibiotics: amoxicillin (a beta-lactam), clarithromycin (a macrolide), and metronidazole (a nitroimidazole). The mechanism of action is synergistic: esomeprazole inhibits the gastric H+/K+-ATPase to raise stomach pH, which optimizes the stability and activity of the antibiotics; bismuth subcitrate provides direct antimicrobial effects and mucosal protection; amoxicillin inhibits bacterial cell wall synthesis; clarithromycin blocks protein synthesis by binding to the 50S ribosomal subunit; and metronidazole induces DNA strand breakage. This regimen is often employed as a rescue therapy or in areas where dual resistance to clarithromycin and metronidazole is prevalent.

Other names
bismuth-containing concomitant therapymodified bismuth quadruple therapyconcomitant therapy with bismuth
02

Targets

UreaseATP4A (Potassium–transporting ATPase alpha chain 1)DNABacterial 50S ribosomal subunitPBP (Penicillin-binding protein family)

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