ArQule and its partner Daiichi Sankyo have discontinued a Phase III trial evaluating the selective MET inhibitor tivantinib (ARQ 197) in patients with nonsquamous NSCLC, after an interim analysis by the Marquee study’s independent data monitoring committee concluded it wouldn’t meet its primary endpoint of improved overall survival. The 1,000 patient pivotal study was evaluating tivantinib in combination with erlotinib in previously treated patients with locally advanced or metastatic nonsquamous NSCLC.

Data from the interim analysis showed that, while adding tivantinib to erlotinib therapy resulted in statistically significant improvements in progression-free survival in the intent-to-treat population, the benefits didn’t extend to overall survival.

Cancer therapeutics firm ArQule and Daiichi Sankyo signed a global (excluding Japan and certain other Asian countries) license, co-development, and commercialization deal for tivantinib back in December 2008. The drug is being evaluated broadly as monotherapy and as part of combination therapy against a variety of cancers. The tivantinib clinical trial program currently includes non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, and gastric cancer, as well as earlier stage, signal generation studies in multiple tumor types.

The ArQule clinical pipeline also includes ARQ 736, a pan-RAF kinase inhibitor undergoing Phase I evaluation, together with ARQ 621, a Phase II-ready inhibitor of the Eg5 kinesin motor protein, and ARQ 092, an AKT inhibitor currently in Phase I clinical studies.

ArQule’s discovery engine is founded on a structure-based drug design technology, the ArQule Kinase Inhibitor Platform (AKIP™), which targets inactive forms of kinases that the firm says play key roles in cancer and other diseases. AKIP integrates in silico drug design with chemistry and assay development expertise to design and optimize non-ATP competitive inhibitors that interact with these kinase.

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