Background

Gap between the burden of infections due to multidrug-resistant bacteria and thedevelopment of new antibiotics to tackle the problem.

More and more data on the role of antibiotics efflux in the multidrug resistant(MDR) bacteria emergence, but no efficient solution.

→ New molecules able to restore the sensitivity of MDR Bacteria toantibiotics (inhibitors of efflux pump). Already tested on 2 bacteria species andwith 3 antibiotics at different concentrations. At least 5 active moleculesincrease/restore in vitro antibiotics activity

Benefits

• Efficient, easy to synthesize; cheap; water soluble
• Activity higher than PAβN activity without cytotoxicity effect: restoration of MDR bacteria sensitivity to antibiotics
• Potentially active on a wide spectrum of antibiotics /macrolids and bacteriastrains

DEVELOPMENT STATUS & RESULTS

In vitro Assays on a large number of MDR strains of each bacterial species

In vitro Assays using different combinations of compounds/antibiotics

In vivo Assays to determine the efficiency of the compounds on infected mice by different MDR bacteria species

Results:
→ Our new molecules target efflux pump and restore the antibiotic activity on MDR bacteria.
→ Antibiotic dose needed to kill the MDR bacteria is at least 8 times lower than without molecule.
→ No cytotoxicity on CHO cell line

Applications

Infectiology/Pharmacology

• Restoring existing antibiotics activity on MDR bacteria
• Development of new applications for existing antibiotics (Macrolids on Gram negatives)