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A New Antibiotic’s Mechanism Of Action

The novel antibacterial drug gepotidacin is showing clinical promise for the treatment of skin infections and gonorrhea.

Gepotidacin was developed in response to the rising bacterial resistance to fluoroquinolone drugs such as ciprofloxacin. Like fluoroquinolones, gepotidacin acts on the bacterial enzymes gyrase and topoisomerase IV, but details of its interaction with these enzymes are unknown.

Neil Osheroff, PhD, and colleagues have now characterized the mechanism of action of gepotidacin against Staphylococcus aureus gyrase.

They found that gepotidacin is a potent inhibitor of the enzyme. Unlike fluoroquinolones, which induce double-stranded DNA breaks, gepotidacin induced only single-stranded breaks, even at high concentrations and extended times of exposure. Crystal structures of gepotidacin with gyrase and nicked or intact DNA revealed details of the compound’s interaction with the enzyme and DNA.

The findings, reported in ACS Infectious Diseases, provide important insights on a first-in-class antibacterial and will guide the development of additional compounds that overcome antibacterial resistance.

This research was supported by a Merit Review award from the U.S. Veterans Administration, and grants and fellowships from the National Institutes of Health (GM126363, GM007628), the PhRMA Foundation and the American Association of Pharmaceutical Scientists.

Original article by VUMC.

Pamela Clark, CRNI, is an Infusion Nurse Coordinator at Healix, a leader in the field of parenteral services.  She has more than 28 years of experience in infusion therapy and infusion education with both licensed nurses and patients. Her experience spans multiple infusion settings including: acute care, long-term care, home infusion, and ambulatory infusion care. She also has experience in oncology and oncology research.  

Pam has been active in the Infusion Nurses Society, both locally and nationally. She currently sits on the Journal of Infusion Nursing editorial review board, is secretary of the Greater Houston INS Chapter, and has experience as a presenter at national INS conferences on various infusion-related topics. Ms. Clark holds a Bachelor’s Degree in Nursing from The University of Texas System School of Nursing at Austin. She has been certified in Infusion Nursing by the Infusion Nurses Credentialing Corporation for more than 25 years.  

Pam has written several courses on intravenous antibiotics.  Click on the course name to learn more.

Intravenous Antibiotics: Where We Are and Where We’re Going – Additional Classifications

Intravenous Antibiotics: Where We Are and Where We're Going – Antivirals

Intravenous Antibiotics: Where We Are and Where We’re Going – Antifungals

Intravenous Antibiotics: Where We Are and Where We’re Going – ß-lactams

Intravenous Antibiotics: Where We Are and Where We’re Going – Glycopeptides

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