Skip to McMaster Navigation Skip to Site Navigation Skip to main content
McMaster logo

Therapeutics & Diagnostics 22-079

New semi-synthetic glycopeptide analogs combat drug-resistant VRE infections

Tech ID



D. Wright
K. Koteva
M. Xu

Patent Status

US provisional patent filed

Stage of Research

Proof of principle data available


Leigh Wilson
Associate Director, New Ventures


Glycopeptide antibiotics (GPAs) are the ‘last-resort’ drugs reserved for the treatment of serious drug-resistant Gram-positive infections. Their beneficial efficacies are exhaustively challenged by the emergence and distribution of GPA-resistant pathogens, vancomycin resistant enterococcus (VRE), in healthcare settings, propelling the innovative discovery/development of more effective GPAs. Type V GPAs provide a unique mode of action that enables them to be very promising lead compounds for drug discovery and development to combat drug-resistant and particularly VRE infections.

A team of researchers from McMaster has identified a new Type V GPA, rimomycin, that is active against VRE and Mycobacteria strains. After running medicinal chemistry campaigns on rimomycin, a lead compound has been identified that shows 8- and 16- fold decrease in minimum inhibition concentration (MIC) against VRE and Mycobacteria strains.  The McMaster team has developed a synthetic biology platform to enable the synthesis of these compounds at gram scale.


  • The in vivo efficacy of the lead compound in the mouse systemic infection model demonstrates that it is a promising candidate to cure VRE A infections.


  • The lead compound contributes to a significant survival benefit against VRE A infection and prevents the invasive VRE A dissemination to blood and spleen.
  • The lead compound exhibited no cytotoxicity or hemolytic activity.
  • Compounds have a unique mechanism of action and negligible development of resistance.

Hamilton Health Sciences, St. Joseph's Healthcare Hamilton and McMaster University logos.