Firms add third target and two more years to arrangement.

ArQule and Daiichi Sankyo expanded their research, development, and license agreement for the discovery of novel kinase inhibitors in oncology. The new deal establishes a third therapeutic target with an option for a fourth and includes a two-year extension based on the application of the ArQule Kinase Inhibitor Platform (AKIP™) technology.

“Our initial drug-discovery collaboration has identified a development candidate for one target, and we are optimizing advanced lead compounds for the other target,” reports Dr. Thomas C. K. Chan, Ph.D., CSO of ArQule. “The expansion of this collaboration will continue to deploy AKIP technology to discover inhibitors with novel modes of action for additional oncology targets over the next two years.”

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 binding mode that leads to inhibition of target kinases by small molecules that do not compete with adenosine triphosphate (ATP). ArQule says that it has identified binding sites in more than 200 kinases involved in multiple therapeutic areas that are amenable to such non-ATP competitive inhibition.

Consistent with the existing AKIP collaboration, the financial terms of the expanded agreement include research support, licensing fees for discovered compounds, milestone payments related to clinical development, regulatory review, and sales, as well as tiered royalties on net sales of each product.

Daiichi Sankyo will have an option to license compounds directed to the targets defined under the agreement following the completion of certain preclinical studies. ArQule retains the option to co-commercialize any licensed products in the U.S.

ArQule’s lead product, in Phase II development, is ARQ 197, an inhibitor of the c-Met receptor tyrosine kinase. It has also initiated Phase I testing with ARQ 621, designed to inhibit the Eg5 kinesin motor protein. The company’s preclinical pipeline includes a compound designed to inhibit the BRAF kinase.

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