ArQule Announces Presentations at AACR 102^nd Annual Meeting

WOBURN, Mass.--(BUSINESS WIRE)--ArQule, Inc. (Nasdaq: ARQL) today announced that four presentations of pre-clinical data for its product candidates will take place at the 102^nd Annual Meeting of the American Association for Cancer Research, which will be held from April 2-6, 2011 in Orlando, Florida.

These product candidates include: ARQ 736, a pan-RAF kinase inhibitor in Phase 1 clinical development; ARQ 680, the active moiety of ARQ 736; ARQ 087, a pan-FGFR kinase inhibitor in pre-clinical development; and tivantinib (ARQ 197), an oral c-Met inhibitor in Phase 3 and Phase 2 clinical development.

The titles and times of these presentations are as follows:

• Abrogation of the paradoxical activation of the MAPK pathway following RAF inhibition by ARQ 680, a potent inhibitor of the RAF family of serine/threonine kinases
  Poster Session
  PO.ET06.03. Kinase Inhibitors 1
  Tuesday, April 5, 2011, 8:00 AM – 12:00 PM

• In vitro cross species metabolism of a novel RAF kinase inhibitor phosphate prodrug, ARQ 736
  Poster Session
  PO.CH01.05. Drug Delivery and Drug Metabolism
  Tuesday, April 5, 2011, 8:00 AM – 12:00 PM

• Exploratory biomarker discovery for clinical development of ARQ 087, a potent pan-FGFR kinase inhibitor
  Poster Session
  PO.ET06.03. Kinase Inhibitors 1
  Tuesday, April 5, 2011, 8:00 AM – 12:00 PM

• Potentiation of the anti-proliferative and cytotoxic activity of ARQ 197 & gemcitabine with a pulsatile exposure regimen
  Poster Session
  PO.ET03.01. Enhancing Efficacy of Targeted Agents
  Wednesday, April 6, 2011, 8:00 AM – 12:00 PM

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 human cancers. ArQule’s lead product, in Phase 2 and Phase 3 clinical development, is tivantinib (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, and with ARQ 736, designed to inhibit the RAF kinases. ArQule’s current discovery efforts, which utilize 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 (adenosine triphosphate) for binding to the kinase.

This press release contains statements regarding the Company’s pre-clinical and clinical development of ARQ 736, ARQ 680, ARQ 087 and ARQ 197. 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. Positive information about pre-clinical and early stage clinical trial results does not ensure that later stage or larger scale clinical trials will be successful. For example, ARQ 736, ARQ 680, ARQ 087 and ARQ 197 may not demonstrate promising therapeutic effect; in addition, they may not demonstrate an appropriate safety profile in current or later stage or larger scale 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 in the course of developing, testing or manufacturing these compounds that could lead the Company or its partners 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. Obstacles may arise or issues may be identified in connection with review of clinical data with regulatory authorities, or 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 for ARQ 197 is subject to the ability of the Company or Daiichi Sankyo, Inc., its partner, and Kyowa Hakko Kirin, a licensee of ARQ 197, to enroll patients, enter into agreements with clinical trial sites and investigators, and overcome other technical hurdles and issues related to the conduct of the trials that may not be resolved. Drug development involves a high degree of risk. Only a small number of research and development programs result in the commercialization of a product. Positive pre-clinical data may not be supported in later stages of development. Furthermore, ArQule may not have the financial or human resources to successfully pursue drug discovery in the future. Moreover, Daiichi Sankyo has certain rights to unilaterally terminate its ARQ 197 license, co-development and co-commercialization agreement with the Company. If it were to do so, the Company might not be able to complete development and commercialization of ARQ 197 on its own. 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.