Daiichi Sankyo to License ARQ 092 From ArQule

ArQule, Inc. and Daiichi Sankyo, Co. Ltd. recently announced the execution of a license agreement for the development of a new AKT inhibitor called ARQ 092, the first compound to emerge from the companies’ November 2008 agreement to collaborate on research utilizing the AKIP (ArQule Kinase Inhibitor Platform) technology to generate novel, selective, and potent small molecule kinase inhibitors. Under the license agreement, Daiichi Sankyo will obtain exclusive rights for development, manufacturing, and marketing of ARQ 092 on a worldwide basis.

ARQ 092 will be studied in cancer patients to identify its utility in targeting the AKT-signaling pathway, which plays a role in regulating cell growth, survival, migration, and angiogenesis, and is frequently deregulated in cancer. Patient enrollment in the Phase I clinical trial with ARQ 092 is scheduled to open in the coming months.

“ARQ 092 is a potent, selective AKT inhibitor that has been optimized through a structure-based drug design methodology developed by ArQule scientists,” said Dr. Thomas C.K. Chan, Chief Scientific Officer of ArQule. “This clinical candidate is the result of close scientific collaboration between the two companies throughout the past two-and-a-half years.”

“The ARQ 092 collaboration builds on the success of our other partnerships with ArQule, including the co-development of our c-MET inhibitor, tivantinib, which is currently being studied in a Phase III trial as a treatment for non-squamous, non-small cell lung cancer,” said Dr. Kazunori Hirokawa, Global Head of the R&D Unit of Daiichi Sankyo. “In addition to our own internal R&D capabilities, our strategic alliance partnerships, such as our collaborations with ArQule, allow us to combine forces to move more programs into clinical trials toward our common goal of improving and extending lives.”

Kinases play pivotal roles in modulating diverse cellular activities and have been implicated as important mediators of certain forms of cancer and other diseases. The AKIP technology is based on a novel binding mode that leads to inhibition of target kinases by small molecules that do not compete with adenosine triphosphate (ATP) for binding. ArQule has identified more than 200 human kinases involved in multiple therapeutic areas that are amenable to such non-ATP competitive inhibition. ArQule’s ability to rationally design novel kinase inhibitors that encompass new chemical spaces allows for an expanding intellectual property estate. The company believes that non-ATP competitive small molecule inhibitors may have fewer off-target side effects and may have utility in treating a broad range of human diseases.