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Pharmacotherapy
IND Filed for CRA-024781, a Novel Histone Deacetylase Inhibitor
May 3, 2005 - 9:49:38 AM

Celera Genomics (NYSE:CRA), an Applera Corporation business, today announced that it has submitted an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA) for CRA-024781, a novel histone deacetylase (HDAC) inhibitor. Pending clearance by the FDA, Celera Genomics plans to initiate Phase 1 clinical trials.

HDAC inhibitors target HDAC enzymes and inhibit the proliferation of cancer cells and induce cancer cell death, or apoptosis(1).

Celera Genomics recently reported data at the American Association for Cancer Research (AACR) meeting in April 2005, showing the efficacy of CRA-024781 as an HDAC inhibitor in xenograft cancer models.

In addition, it was demonstrated that the measurement of tubulin and histone acetylation can be used to monitor the pharmacodynamic effects of CRA-024781 in vivo.

Histone deacetylation is carried out by a family of related HDAC enzymes. Inhibition of these enzymes causes changes to chromatin structure and to gene expression patterns, which results in the inhibition of proliferation of cancer cells, and induction of apoptosis. Celera Genomics published the first three-dimensional structure of an HDAC enzyme in July 2004, and this information has been used to aid the design of a series of novel HDAC inhibitors.

"We're pleased with the progress we've made in advancing CRA-024781 through its preclinical experiments to this point," said Robert Booth, Ph.D., Chief Scientific Officer of Celera Genomics. "We anticipate that we will utilize the insights we have gained from the identification of potential biomarkers of efficacy to design and implement our clinical trials, the first of which is planned to assess the safety and pharmacokinetics of CRA-024781 in a dose escalation study, at a projected cost of less than $3 million."

"Today's accomplishment reflects Celera's successful transition from sequencing the human genome and selling data to focusing on the realization of downstream value in therapeutics and diagnostics," said Kathy Ordonez, President of Celera Genomics. "While the Online/Information Business was important to Celera Genomics in its initial years, it is no longer strategically relevant and has been a source of cash consumption, estimated to be approximately $7 million for fiscal 2005, since many of the subscriptions were prepaid."

"Celera Genomics now has three important strategic assets. First, our proteomics platform continues to yield novel cancer targets that have been the focus of several partnerships for drug discovery and development, allowing us to advance them cost effectively. Secondly, and with today's achievement of filing for an IND with the FDA, our small molecule capability and pipeline of compounds is now sufficiently mature to look to partner and capitalize on this asset. Finally, Celera Diagnostics, a 50-50 joint venture with Applied Biosystems, is generating substantial product sales and making important discoveries for incorporation into future new products," Ms Ordonez added. "With the anticipated discontinuation of the Online/Information Business, Celera Genomics is now in a position to focus its efforts on its most substantial opportunities while managing its use of cash."

Celera Genomics has another compound, a Cathepsin K inhibitor, in a Phase I clinical trial as a potential treatment for osteoporosis. This compound is partnered with Merck, and has been in clinical trials since July 2004. This followed a multi-year collaboration with Merck to develop small molecule inhibitors of Cathepsin K, which was initiated in November 1996.

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