Efflux Pump Inhibition by FDA-Approved Antifungals

Sertaconazole or Oxiconazole as EPI for Treating MDR S.Aureus Infections (Available for Licensing in Any Country) 

Sector: MEDICAL, Origin: INDIA

Multi-drug-resistant S. aureus(MDR-S. aureus) is a major clinical concern due to its resistance to multiple antibiotic classes, driven in part by the upregulation of efflux pumps such as NorA, NorB, and AbcA. These pumps reduce intracellular antibiotic concentrations, leading to treatment failure and the need for higher drug dosages

This invention demonstrates the novel repurposing of two FDA-approved antifungal agents, Sertaconazole and Oxiconazole, as Efflux Pump Inhibitors (EPIs) to enhance the antibacterial activity of frontline antibiotics against MDR-S. aureus. These drugs were found to effectively inhibit major bacterial efflux pumps such as norA, norB, and abcA, which are known to reduce intracellular antibiotic concentrations and contribute to resistance

Key Highlights:

  • Effectively inhibits key efflux pumps (norA, norB, abcA) in MDR-S. aureus strains.
  • Enhances the activity of existing antibiotics-especially norfloxacin, moxifloxacin, and cefotaxime, with over 4-fold MIC reduction.
  • Demonstrates>2-log reduction in bacterial load, indicating strong therapeutic potential.
  • Depolarises bacterial membrane potential to suppress drug efflux and improve antibiotic retention
  • Proven efficacy both in vitro and in vivo

Patent:

Indian Patent Filed ( 202431062787 )

Development Stage:

TRL – 4

Seeking:

Available for Licensing or for Collaboration in any BRICS+. Country

  1. Expansion to International market through collaboration with Government/Private hospitals

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