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WOBURN, Mass.—Continuing progress in its preclinical and clinical programs has led ArQule, known in the past primarily for being a chemistry services business, to shift its focus to drug discovery efforts to develop innovative cancer therapeutics. As a result, the company will exit the chemistry services business altogether.
 
The decision to become an integrated research and development company draws heavily on ArQule's existing strengths in proprietary biology and validated chemistry, notes William B. Boni, VP of investor relations and corporate communications.  "We are retaining the core chemistry expertise that allowed us to succeed so well as a combinatorial chemistry company," he says.
 
ArQule will leverage its chemistry capabilities by continuing the discovery of compounds that act on its proprietary ACT targets—and other related biological targets—that are integral in the onset and spread of cancer. This chemistry aims to integrate drug-like qualities into new product candidates at the earliest stages of development.
 
"As we look toward the end of 2005, the company is solidly emerging as a cancer discovery company with programs that combine both an innovative approach to attacking cancer in the form of checkpoint activations, as well as a leveraging rather significant chemistry expertise in the pursuit of novel compounds that affect well-known biological targets."
 
ArQule has one clinical-stage compound, ARQ 501, an E2F modulator that has demonstrated  potency and selectivity in the activation of faulty cellular checkpoint machinery in cancer cells. It is partnered with Roche in this effort.
 
ArQule also plans to submit an IND application by the end of this year for ARQ 197, the lead compound of a series of proprietary compounds generated through the company's ARQ 650RP cancer survival pathway platform.
 
Boni says the company has an extensive portfolio of discovery-stage programs, but three particular preclinical-stage programs stand out as promising in the short run, in addition to AQR 197. They are a second-generation E2F activator along similar lines as ARQ 501, a selective BRAF kinase inhibitor and a novel checkpoint activator.

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