Increasing Vancomycin's Potency with Simple Chemical Modifications

Researchers demonstrate that they can modify vancomycin in ways that greatly increase antibacterial potency and limit development of bacterial resistance.

Vancomycin is a commonly prescribed antibiotic because of methicillin-resistant Staphylococcus aureus (MRSA) emergence in the 1980s. With increased use of vancomycin, both high-level (vanA+ and vanB+) and low-level vancomycin-resistant organisms have emerged, particularly in Enterococcus faecium where 20% to 35% of isolates now show high-level vancomycin-resistance (VRE). Using the strategy of chemically modifying existing antibiotics, researchers now report successfully chemically modifying vancomycin into several more-potent derivatives, with some of these exhibiting 1000 times greater activity than vancomycin against gram-positive pathogens, including VRE.

The most potent derivative, 4-chlorobiphenyl (CBP) C1-aminomethylene vancomycin, di…

Reviewing Author

George Sakoulas, MD

Disclosures

Consultant/Advisory BoardParatek Pharmaceuticals; Nestle Corp.; AbbVie; Shionogi

Speaker’s BureauAllergan/AbbVie; Paratek Pharmaceuticals; Nestle Corp.

RoyaltiesUpToDate

Editorial BoardsAntimicrobial Agents and Chemotherapy; Open Forum Infectious Diseases