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Antibiotics, Industrial Chemicals and Herbicides
A Small Molecule Inhibitor of Staphylococcus aureus
George D. Markham, PhD, and Maxim Pimkin, MD

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Background

Staphylococcus aureus is a common bacterium that resides on skin and in nasal passages, but it can cause mild to serious infections if it enters the body through a cut in the skin. The methicillin-resistant Staphylococcus aureus (MRSA) is a bacteria strain resistant to the most common antibiotics (beta-lactam antibiotics, including methicillin, oxacillin, amoxicillin, and penicillin), and can cause life-threatening infections, such as bloodstream infections, surgical site infections, or pneumonia. MRSA infections occur most frequently among patients who undergo invasive medical procedures, who have weakened immune systems, and who are being treated in hospitals and healthcare facilities such as nursing homes and dialysis centers.

People infected with antibiotic-resistant organisms like MRSA are more likely to have longer and more expensive hospital stays, and may be more likely to die as a result of the infection. When the drug of choice for treating antibiotic-resistant infection does not eliminate the infection, these patients require treatment with second- or third-choice medicines that may be less effective, more toxic and more expensive.

Research published in 2007 highlighted that in 2005, there were about 368,600 hospital stays for infections with MRSA, a 30% increase from the previous year and a tenfold increase since 1995. On average, hospital stays for MRSA infections cost $14,000, compared with $7,600 for all other stays, and the length of hospitalization is more than double: 10.0 days for MRSA infections versus 4.6 days for all other stays (1)

It is estimated that in 2005 ~94,360 people developed a serious MRSA infection, and 18,650 persons (~20%) died of causes related to serious MRSA infections during a hospital stay (2).

Description

Screening more than 200,000 molecules by computational docking of a 3D library, Drs. Markham and Pimkin identified a lead compound that when tested in the lab showed inhibitory activity of growth of a clinical MRSA strain. They are now testing the MRSA domain that interacts with this compound to design similar small molecules with a higher inhibitory activity.

Applications

  • Development of new antibiotics against Staphylococcus aureus
  • Treatment of MRSA infections

Citations

  1. Elixhauser, A. et Steiner, C. "Infections with Methicillin-Resistant Staphylococcus Aureus (MRSA) in U.S. Hospitals, 1993–2005," Healthcare Cost and Utilization Project," Statistical Brief No. 35
  2. Center for Disease Control and Prevention, "MRSA: Methicillin-resistant Staphylococcus aureus in Healthcare Settings"

Patent Status:

  • U.S. Patent pending

For licensing information, contact

Clarissa Ceruti, PhD, MBA
Associate Director
Office of Corporate Alliances

Fox Chase Cancer Center
610 Old York Road, Room 407
Jenkintown, PA 19046
Tel.: 215-214-1546
Fax: 215-214-1440
clarissa.ceruti@fccc.edu