ArQule Regains Worldwide Rights to AKT Program

ArQule

today announced it has regained worldwide rights for the development and commercialization of compounds covered under its AKT collaboration with Daiichi Sankyo Co., Ltd., including the lead compound emerging from this collaboration, ARQ 092. Data from an ongoing Phase 1 trial with ARQ 092 will be presented at the AACR (American Association for Cancer Research) Annual Meeting on April 9, 2013. “Regaining worldwide rights to the AKT program, including the novel oral agent, ARQ 092, adds significant value for ArQule, as it expands our proprietary pipeline in an exciting area of therapeutic development,” said Brian Schwartz, M.D., chief medical officer of ArQule. “AKT, also known as the serine/threonine kinase PKB, is believed to mediate a number of signal transduction processes and represents a potential therapeutic target for several cancers and other diseases. We look forward to the AACR data presentation from the ongoing Phase 1 trial with ARQ 092.” ARQ 092 is a selective AKT inhibitor that was discovered through technology from the ArQule Kinase Inhibitor Platform (AKIP™) and optimized through a structure-based drug design methodology. The AKT signaling pathway, which plays a role in regulating cell growth, survival, migration and angiogenesis, is frequently dysregulated in cancer. ArQule is regaining its rights to the AKT program and to ARQ 092 pursuant to Daiichi Sankyo's decision to terminate a license and co-commercialization agreement with ArQule dated November 8, 2011. 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 oral, selective inhibitor of the c-MET receptor tyrosine kinase. The Company's pipeline consists of ARQ 092, designed to inhibit AKT, ARQ 087, designed to inhibit fibroblast growth factor receptor (FGFR), ARQ 621, designed to inhibit the Eg5 kinesin motor protein, and ARQ 736, designed to inhibit the RAF kinases. 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 (adenosine triphosphate) for binding to the kinase.