NORWOOD, MA February 18, 2003 Cyclis Pharmaceuticals, Inc. today announced publication of laboratory studies demonstrating that an experimental anti-cancer agent, -lapachone, can selectively kill tumor cells while sparing healthy cells. The studies suggest a novel and fundamental therapeutic mechanism for potential cancer drugs that activate cellular pathways for selectively inducing death in cancer cells. Using this approach, called Activated Checkpoint TherapyTM (ACT), Cyclis is discovering and developing small molecule anti-cancer drugs, the most advanced of which is CO-501. This product, which is based on the new findings, is expected to enter clinical trials in mid-2003.

The findings are published in the on-line edition of the Proceedings of the National Academy of Sciences.

"When DNA damage occurs in normal cells, a checkpoint pathway is activated that triggers apoptosis when that damage cannot be repaired," said Cyclis Vice President of Research Dr. Chiang J. Li, senior author of the paper. "In cancer cells these pathways are defective, leading to uncontrolled growth. These studies strongly suggest that one such pathway, involving the E2F1 protein, can be turned on with small molecule drugs, leading to selective killing of cancer cells."

"This research details one example of how our ACTTM platform works at the molecular level," said Cyclis President and CEO, Dr. Samuel K. Ackerman. "We have applied this platform successfully with our initial drug candidates. This approach also opens the door to additional drug discovery for a wide range of cancers by applying knowledge of this unique mechanism of action to multiple drug targets of the checkpoint system."

In these studies, the researchers compared the effects of -lapachone on human cancer cell and normal cell survival. They demonstrated that the compound selectively induces apoptosis in the tumor cells, but not in normal cells. They furt
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Contact: Shannon Altimari
saltimari@fkhealth.com
617-761-6727
Feinstein Kean Healthcare
18-Feb-2003

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