Closthioamide- a new, unusual natural product with potent antibiotic activity against MRSA

Referenznummer TO 10-00080
 

The Challenge 

Resistance of gram-positive pathogens against antibiotics is an increasing problem. One of the most problematic gram-positive bacterium in public health is the methicillin-resistant Staphylococcus aureus (MRSA), because it can only be treated with vancomycin and teicoplanin as it is resistant to all other antibiotics in clinical use. Various strains, however, have developed resistance against vancomycin as well. In addition, vancomycin-resistant enterococci (VRE) are one of the most important causes of nosocomial infections. As vancomycin-resistance is often accompanied by multi-drug resistance, there are no antibiotics available to treat such VRE-infections to date.

Technology

The invention discloses closthioamide, a novel type of antibiotics representing a fully unprecedented polythioamide natural product. Closthioamide is the first secondary metabolite isolated from strictly anaerobic bacteria, specifically Clostridium cellulolyticum. This unique compound is only moderately cytotoxic  (against HeLa cells), but is highly active against pathogenic, methicillin-resistant Staphylococcus aureus (MRSA) strains as well as against vancomycin-resistant enterococci (VRE) with MIC50 of 0.58 µM. Closthioamide is thus significantly more potent against these bacteria than ciprofloxacin, the standard drug used against VRE, with a remarkable strain selectivity. 

 

Commercial Opportunity

In-licensing or cooperation for further development of an antibiotic.

Developmental Status

In vitro assays with a panel of pathogens and cell lines conducted.

Patent Situation 

European Patent filed in October 2009.

Further Reading

Lincke et al. 2010. Closthioamide: An Unprecedented Polythioamide Antibiotic from the Strictly Anaerobic Bacterium Clostridium cellulolyticum. Angew. Chem. Int. DOI: 10.1002/anie.200906114.

 

 

 

 

 

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Kontakt:

Sabina Heim, Ph.D.
Technology Manager
Ascenion GmbH

T: +49 (0)531 6181-2090
F: +49 (0)531 6181-2098
heim@ascenion.de