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ArQule, Inc. (ARQL) Provides Clinical Update on E2F-1 Program; Company Plans to Stop Further Clinical Testing

4/10/2008 9:07:21 AM

WOBURN, Mass.--(BUSINESS WIRE)--ArQule, Inc. (NASDAQ: ARQL - News) today announced the completion of its previously disclosed analysis of QTc prolongation data related to a Phase 1 dose escalation trial with ARQ 171, a second generation product in its E2F-1 DNA damage response cancer therapy program. Based on the confirmation of QTc prolongation associated with ARQ 171, the Company does not plan to pursue further clinical testing with this compound.

The Company’s E2F-1 program is under development pursuant to a collaboration with Roche. Roche has an option to license worldwide rights to products under this program based on data from completed Phase 2 clinical trials with ARQ 501, the first-generation E2F-1 compound, as well as a recommended Phase 2 dose and other information defined in the collaboration agreement for a second-generation E2F-1 product. As a result of ArQule’s decision to forego further development of ARQ 171, a new chemical entity designated ARQ 761 has become the second-generation E2F-1 product behind ARQ 501.

ArQule is currently conducting GLP toxicology studies with ARQ 761, a pro-drug that reverts to ARQ 501 following exposure to plasma. Pending the successful completion of these studies, an IND (Investigational New Drug application) for ARQ 761 would be filed in the second half of 2008.

“On an ongoing basis, ArQule and Roche are evaluating clinical and pre-clinical data from our E2F-1 compounds to inform Roche’s decision regarding further participation in this program,” said Peter S. Lawrence, chief operating officer of ArQule. “Pending the successful pre-clinical and Phase 1 clinical development of ARQ 761, we expect to have a recommended Phase 2 dose for this compound in 2009. Roche’s option to the E2F-1 program runs through December 31, 2008, and they have the right to extend the option period through December 31, 2009 in exchange for financial support of further program deliverables.”

About the E2F-1 Program

ARQ 501 and ARQ 761 are designed to kill cancer cells selectively while sparing normal cells through the activation of DNA damage response pathways believed to be regulated by the E2F-1 regulatory protein, thereby restoring the ability of the cell to recognize DNA damage and initiating the process of apoptosis, or programmed cell death, in these cells. ARQ 501 is the first product generated in this program, while ARQ 761 is a second-generation compound.

About ArQule

ArQule is a biotechnology company engaged in the research and development of next-generation, small-molecule cancer therapeutics. The Company’s targeted, broad-spectrum products and research programs are focused on key biological processes that are central to cancer. ArQule’s lead products, which are in clinical-stage development, consist of ARQ 197, an inhibitor of the c-Met receptor tyrosine kinase, and ARQ 501, an activator of the cell’s DNA damage response mechanism mediated by the E2F-1 transcription factor. The Company’s most advanced pre-clinical development programs are focused on the inhibition of the Eg5 kinesin spindle protein and the B-RAF kinase. ArQule’s discovery efforts are focused on the identification of novel kinase inhibitors that are potent, selective and do not compete with ATP (adenosine triphosphate), an energy source for cells.

This press release contains forward-looking statements regarding the progress of the Company’s pre-clinical and clinical development of products in its E2F-1 program, including ARQ 501 and ARQ 761, as well as the Company’s collaboration with Hoffman-La Roche related to this program. These statements are based on the Company’s current beliefs and expectations, and are subject to risks and uncertainties that could cause actual results to differ materially. Even if a drug candidate such as ARQ 761 should successfully complete preclinical testing and Phase 1 clinical trials, such results do not ensure that later stage or larger scale clinical trials would be successful. For example, the E2F-1 compounds may not demonstrate promising therapeutic effect; in addition, they may not demonstrate an appropriate safety profile in pre-clinical testing or in clinical trials as a result of known or as yet unanticipated side effects. The results achieved in later stage trials may not be sufficient to meet applicable regulatory standards. Problems or delays may arise during clinical trials or pre-clinical development or in the course of developing, testing or manufacturing that could lead the Company to discontinue development of these compounds or cause its partner to discontinue its collaboration with the Company. Even if later stage clinical trials are successful, the risk exists that unexpected concerns may arise from analysis of data or from additional data or that obstacles may arise or issues be identified in connection with review of clinical data with regulatory authorities or that regulatory authorities may disagree with the Company’s view of the data or require additional data or information or additional studies. In addition, the planned timing of completion of pre-clinical development and Phase 1 clinical testing with ARQ 761 is subject to the ability of the Company to enroll patients, enter into agreements with clinical trial sites and investigators, and other technical hurdles and issues that may not be resolved. Moreover, the Company’s partner could choose not to pursue the collaboration for reasons unrelated to the progress of the program. Drug development involves a high degree of risk. Only a small number of research and development programs result in the commercialization of a product. Furthermore, ArQule may not have the financial or human resources to successfully pursue drug discovery in the future. For more detailed information on the risks and uncertainties associated with the Company’s drug development and other activities see the Company’s periodic reports filed with the Securities and Exchange Commission. The Company does not undertake any obligation to publicly update any forward-looking statements.


ArQule, Inc. William B. Boni, 781-994-0300 VP, Investor Relations/Corp. Communications

Source: ArQule, Inc.

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