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Study Shows Coronado Biosciences' Bcl-2 Inhibitor, Apogossypol, is More Efficacious, Less Toxic than Gossypol in Animal Models
Date:1/28/2008

Published Paper Provides Rationale for Continued Development of CNDO103 as

Cancer Treatment

SAN DIEGO, Jan. 28 /PRNewswire/ -- Coronado Biosciences Inc. today announced the publication of data demonstrating that the Bcl-2 inhibitor, Apogossypol, effectively killed a variety of cancer cells in vitro while demonstrating less toxicity than Gossypol in vivo in mice.

Published online in Blood (Jan. 17, DOI 10.1182/blood-2007-09-113647) by the Burnham Institute's president and CEO, John Reed, M.D., Ph.D., and collaborators, the paper summarized study findings demonstrating that mice treated with Apogossypol experienced less hepatotoxicity and gastrointestinal toxicity than those treated with Gossypol. The results support Coronado Biosciences' continued development of its lead candidate, CNDO103, as a cancer treatment.

"Apogossypol was rationally designed to eliminate the toxicities seen with Gossypol," said Reed. "This study provides strong evidence that Apogossypol is better tolerated by the animals without a compromise in potency in vitro. We hope these preclinical results translate to humans. If they do, Apogossypol can play a role in the treatment of many types of cancers."

Maurizio Pellecchia, Ph.D., a professor at the Burnham Institute of Medical Research, developed Apogossypol using NMR guided rational drug design. "Based on our molecular modeling, we predicted that Apogossypol would be equally potent in killing cancer cells but safer than the parent compound Gossypol," said Pellecchia. "It is gratifying that the exhaustive set of experiments reported in the paper support our predictions."

RJ Tesi, M.D., president and CEO of Coronado Biosciences, added: "The data reinforce our decision to push rapidly to the clinic with Apogossypol. We plan to perform IND-enabling preclinical studies for Apogossypol, CNDO103, in the first half of the year. If the toxicity profile in animals approximates what was
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SOURCE Coronado Biosciences Inc.
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