Antibiotic Resistance Blocker

Inventors: Tracy Mincer and Kristen E. Whalen
Publication No. US20160015686 A1

Overview: Prolific clinical use of antibiotics has led to the emergence of antibiotic resistant bacterial strains at near epidemic levels. Morbidity and mortality as a direct result of infection by antibiotic resistant bacteria has an estimated cost to the U.S. health care system in excess of $20 billion per year. Gonorrhea alone accounted for approximately 820,000 cases in 2008 at an estimated direct lifetime medical cost of $162 million.  Clinical strategies to treat antibiotic resistant infections include use of combinations of antibiotics as well as a search for new and more effective antibiotics. Another approach is to restore the effectiveness of commonly used antibiotics with molecules capable of impairing the resistance-generating machinery in bacteria, returning them to a condition of antibiotic susceptibility.

Technology: A pipeline of promising new chemicals which block antibiotic resistance in Gram-negative bacteria, has been established and the first of several therapeutic molecules isolated from marine microbial exudates has been characterized. This molecule significantly enhances the efficacy of co-administered antibiotics as well as increases the antibiotic susceptibility of resistant Gram-negative bacteria. The compound is water-soluble and acts in vitro at biologically relevant concentrations (IC50 of 0.79mM), and is expected to enhance efficacy in the treatment of pan/multidrug-resistant strains associated with disease targets such as:

• gonorrhea, the second most commonly reported infectious disease in the United States.(caused by: Neisseria gonorrhoeae)
• urinary tract infections  (caused by: Escherichia coli)
• hospital-acquired pneumonia, urinary tract infections, and bloodstream infections (caused by: Pseudomonas aeruginosa, Acinetobacter baumanii, Klebsiella pneumonia)