2009-11-16 18:37:05 -
ArQule, Inc. (Nasdaq: ARQL) today presented data at the AACR-NCI-EORTC meeting in Boston demonstrating the capabilities of the Company’s proprietary drug discovery platform to generate a class of small molecules with significant therapeutic potential.
These data reflect the results of the application of the ArQule Kinase Inhibitor Platform (AKIP™) to discover and optimize a series of small molecule inhibitors of fibroblast growth factor receptor (FGFR) that are not ATP-competitive and show potent anti-tumor activity in FGFR-driven cancer models.
Several compounds from this program showed marked pharmacodynamic suppression of FGFR2 and corresponding growth inhibition in human gastric carcinoma cell lines. Growth of gastric carcinoma tumor xenografts in athymic mice was significantly inhibited after daily administration of a prototype compound for nine days, with
a number of animals being cured of their tumors with this regimen.
“The information presented today demonstrates the speed and efficiency of ArQule’s proprietary, structure-based drug discovery platform to identify chemically novel kinase inhibitors that are not classically ATP-competitive,” said Dr. Thomas C.K. Chan, chief scientific officer of ArQule.
“FGFR has been historically difficult to drug with small molecules, and its role in oncology and other diseases suggests that it may be a promising focal point for therapeutic intervention,” said Dr. Chan. “The opportunity now exists to expand the number of new chemotypes available for development against disease-relevant kinases in multiple therapeutic areas, since we believe that approximately half of the human kinome may be amenable to this novel mode of inhibition.”
ArQule is pursuing the development of its FGFR program independently.
The Company also maintains an oncology-focused AKIP™ drug discovery collaboration with Daiichi Sankyo Co., Ltd.
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 product, in Phase 2 clinical development, is ARQ 197, an inhibitor of the c-MET receptor tyrosine kinase. The Company has also initiated Phase 1 clinical testing with ARQ 621, designed to inhibit the Eg5 kinesin motor protein. An additional clinical-stage program includes compounds that activate the cell’s DNA damage response mechanism mediated by the E2F-1 transcription factor. The Company’s pre-clinical pipeline includes a compound designed to inhibit the BRAF kinase.
ArQule’s current discovery efforts, which are based on the ArQule Kinase Inhibitor Platform (AKIP™) are focused on the identification of novel kinase inhibitors that are potent, selective and do not compete with ATP for binding to the kinase.
This press release contains forward-looking statements regarding the Company's ArQule Kinase Inhibitor Platform (AKIP™) and its fibroblast growth factor receptor (FGFR) program that utilizes this technology.
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. As we learn more about the technology, our current expectations may not be met. Positive information about discovery activities and pre-clinical studies does not ensure that clinical trials will be successful. For example, compounds discovered through AKIP technology may not demonstrate promising therapeutic effect; in addition, they may not demonstrate an appropriate safety profile in clinical trials as a result of known or as yet unanticipated side effects. Furthermore, the results achieved in pre-clinical and clinical trials may not be sufficient to meet applicable regulatory standards. Problems or delays may arise during pre-clinical development, clinical trials or in the course of developing, testing or manufacturing these compounds that could lead the Company to discontinue development. 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 initiation and completion of clinical trials with compounds from the FGFR program are 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. Furthermore, ArQule may not have the financial or human resources to successfully pursue this or its other drug discovery programs in the future. Drug development involves a high degree of risk. Only a small number of research and development programs result in the commercialization of a product. 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, 781-994-0300VP, Investor
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