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WOBURN,Mass.—Instead of ending up at the wrong end of an April Fool's Day prank, ArQule Inc. started the month off with regaining worldwide rights for the development and commercialization ofcompounds covered under its AKT collaboration with Daiichi Sankyo Co.Ltd., including the lead compound emerging from this collaboration, ARQ092.
 
ARQ 092 is a selective AKT inhibitor that was discovered throughtechnology from the ArQule Kinase Inhibitor Platform (AKIP) andoptimized through a structure-based drug design methodology. The AKTsignaling pathway, which plays a role in regulating cell growth,survival, migration and angiogenesis, is frequently dysregulated incancer.
 
"Regaining worldwide rights to the AKT program, including the novel oralagent, ARQ 092, adds significant value for ArQule, as it expands ourproprietary pipeline in an exciting area of therapeutic development,"said Dr. Brian Schwartz, chief medical officer of ArQule, a biotech company focused on researching anddeveloping next-generation, small-molecule cancer therapeutics. "AKT, alsoknown as the serine/threonine kinase PKB, is believed to mediate anumber of signal transduction processes and represents a potentialtherapeutic target for several cancers and other diseases. We lookforward to the AACR data presentation from the ongoing Phase I trialwith ARQ 092."
 
That data will be presented at the American Association for Cancer Research (AACR) annual meeting onApril 9.
 
ArQule is regaining its rights to the AKT program and to ARQ 092pursuant to Daiichi Sankyo's decision to terminate a license andco-commercialization agreement with ArQule dated Nov. 8, 2011.
 
For Daiichi, the decision to exit this deal may have a lot to do with setbacks related to a previous deal that helped set the stage for teaming up on ARQ 092. In the previous work, both companies had been optimistic about ARQ 197 (tivantinib), ArQule's lead compound, but now recent months have seen some bumps in the road there, with tivantinib producing disappointing data in October 2012 in a Phase III trialinvolving patients with non-small cell lung cancer when the numbers suggested patients didn't livesignificantly longer than subjects in the control group. A few months later, in January, the drug fell short of hopes in a mid-stage study involving patients with colorectal cancer.
 
Tivantinib, which in Phase II and Phase III clinical development, is an oral, selective inhibitor of the c-MET receptortyrosine kinase. The company's pipeline consists of ARQ 092, designedto inhibit AKT; ARQ 087, designed to inhibit fibroblast growth factorreceptor (FGFR); ARQ 621, designed to inhibit the Eg5 kinesin motorprotein; and ARQ 736, designed to inhibit the RAF kinases. ArQule'sAKIP-based current discovery efforts are focused on the identification of novelkinase inhibitors that are potent, selective and do not compete with ATP(adenosine triphosphate) for binding to the kinase.
 

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