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Cornerstone Pharmaceuticals Announces The Journal of Molecular Medicine's Publication of Research Showing Selective Inhibition of Cancer Cell Energy Metabolism With Its Novel Lipoate Derivative Compounds
Date:7/25/2011

ism Directed (AEMD) platform.  Dr. Zachar's paper states that CPI-613 induces cancer-specific regulatory hyper-phosphorylation of the E1 subunits of the centrally important TCA enzyme complex, pyruvate dehydrogenase (PDH), resulting in the inhibition of PDH function.  These and related cancer-specific effects of the drug lead to catastrophic disruption of tumor mitochondrial metabolism. Tumor cells are thereby starved of energy and biosynthetic intermediates, culminating in cell death.  

The paper also reports that CPI-613 is a potent inhibitor of human tumor growth in pre-clinical animal models, producing apparent tumor clearance in some animals.  CPI-613 strongly inhibits tumor growth in a non-small cell human lung cancer and a human pancreatic cancer pre-clinical mouse tumor model.  In the pancreatic model, treated animals were further examined for long term survival after completion of a brief treatment regimen and a substantial fraction showed no tumor regrowth.

Robert Shorr, CEO, added "This research demonstrates that our active analogs of lipoic acid can act as potent anti-cancer agents that are highly selective in animal models by disrupting the activity of at least one key bioenergetic enzyme.  In view of the novel mechanism of action of these drugs and their potency in pre-clinical models, it is of great interest to assess their efficacy in human clinical trials and to be able to predict which patients will be most likely to benefit."

"Alterations in cancer cell metabolism are distinctive hallmarks of cancer and represent a new frontier in the development of novel and selective classes of chemotherapeutic interventions for use in the treatment of cancer.  Candidates for application of this new approach are so far, very few and lipoate analogs such as CPI-613 represent a promising new addition," said Dr. Bob Weinberg, a member of Cornerstone's scientific advisory board and a founder and member of the W
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SOURCE Cornerstone Pharmaceuticals, Inc.
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