ARQ 092 is first AKT inhibitor to emerge from collaboration that includes Phase III-stage tivantinib.
Daiichi Sankyo licensed exclusive worldwide rights to develop and commercialize ARQ 092, the first AKT inhibitor candidate to emerge from an ongoing collaboration with ArQule to develop small molecule kinase inhibitors. The anticancer candidate is expected to start in Phase I development within a few months.
Signed in 2008, the kinase inhibitor collaboration between Daiichi Sankyo and ArQule is leveraging the ArQule Kinase Inhibitor Platform (AKIP™), a drug discovery engine that targets inactive forms of kinases that play pivotal roles in cancer and other diseases. AKIP integrates in silico drug design with assay development expertise to design non-ATP competitive inhibitors that interact with these kinases in novel binding modes. ArQule says it has already used the platform to identify over 200 human kinases involved in multiple therapeutic areas that are amenable to non-ATP competitive inhibition.
The Daiichi Sankyo-ArQule collaboration also covers development of the small molecule c-Met receptor tyrosine kinase inhibitor, ARQ 197 (tivantinib), which is currently undergoing Phase III evaluation as a treatment for non-squamous, non-small cell lung cancer. Under terms of this deal Daiichi Sankyo has rights to the compound worldwide, except Japan and certain other Asian countries, where commercial rights have been licensed to Kyowa Hakko Kirin.
ArQule’s in-house pipeline includes two Phase I-stage compounds. ARQ 736 is a pan-RAF kinase inhibitor, and ARQ 621 is an inhibitor of the Eg5 kinesin motor protein.