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A New Class of Metallo-β-lactamases inhibitors Against Antibacterial Resistance

A New Class of Metallo-β-lactamases inhibitors Against Antibacterial Resistance

Bismuth compounds can be administered in combination with β-lactam antibiotics to treat MBL-producing bacterial infection

领域
Therapeutic Chemicals
Reference No.
IP00603

Background

  • Due to widespread antibiotics use, bacterial resistance is increasing and now become a serious threat. Each year, over 2 million people are estimated to be infected by antibiotic-resistant bacteria, where at least 23,000 people died each year as a consequence.
  • β-lactam antibiotics are a class of broad-spectrum antibiotics used widely. The most prominent resistant mechanisms are the expression of β-lactamase enzymes, for which no clinically available wide-spectrum inhibitors are available. 
  • According to Grand View Research, the antibiotics market is expected to reach USD 57.0 billion by 2024. 

Technology Overview

  • Figure 1. In vitro test (Bacteria density upon treatment)
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  • Figure 2. In vivo test (Bacteria challenge in mice)
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  • This invention disclosed the use of some bismuth (III) compounds as metallo-β-lactamases (MBLs) inhibitors. They can be administered in combination with β-lactam antibiotics to treat MBL-producing bacterial infection. 
  • In vitro and in vivo data showed that such bismuth compounds were able to inhibit the MBLs, rendering the effectiveness of the beta-lactam antibiotics (including amoxicillin, ampicillin and meropenem) against multiple resistant strains. 
  • The bismuth compounds include but not limited to Colloidal bismuth subcitriate (CBS), Bismuth subsalicylate (BSS), Bismuth subgallate (BSG) and Ranitidine bismuth citriate (RBC) which are FDA-approved bismuth drugs and are safe to be used in humans.

Benefits & Applications

Benefits

This invention offers a solution to treat infections caused by bacteria resistant to beta‑lactam antibiotics.

Applications

Pharmaceutical composition for prevention or treatment of infection caused by metallo-β-lactamases (MBLs) producing bacteria. 

Patents

  • US Application No. 15/278,916
  • PCT Application No. PCT/CN2017/102077

IP Status

  • Patent application submitted

Seeking

  • Development partner
  • Commercial partner
  • Licensing

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