Daiichi Sankyo and ArQule initiate enrollment in ARQ 197 Phase 3 trial in NSCLC

Daiichi Sankyo Company, Limited (TSE 4568) and ArQule, Inc. (Nasdaq: ARQL) today announced that the first patient has been enrolled in the Phase 3 trial of ARQ 197, an investigational selective inhibitor of the c-Met receptor tyrosine kinase, in combination with erlotinib, for patients diagnosed with non-squamous, non-small cell lung cancer (NSCLC) who have received one or two prior systemic anti-cancer therapies.

“It is our hope and expectation that this late-stage study will confirm the results we observed in patients with non-squamous cell histology in Phase 2, which showed promise toward extending overall survival and progression-free survival in this group when ARQ 197 was combined with erlotinib.”

The Phase 3 trial is a randomized, double-blinded, controlled study of previously treated patients with locally advanced or metastatic, non-squamous NSCLC who will receive ARQ 197 plus erlotinib or placebo plus erlotinib.

The primary objective is to evaluate the overall survival (OS) in the intent-to-treat (ITT) population. Secondary endpoints include OS in the subpopulation of patients with epidermal growth factor receptor (EGFR) wild type, progression-free survival (PFS) in the ITT population, and further assessment of the safety of ARQ 197 in combination with erlotinib.

According to the International Agency for Research on Cancer more than 1.6 million new cases of lung cancer were diagnosed in 2008 globally, and NSCLC accounted for 80 percent of those cases. According to the American Cancer Society more than 220,000 cases of lung cancer will have been diagnosed in 2010 in the U.S. Of patients diagnosed with lung cancer in Europe, almost 90 percent die of the disease.

"With lung cancer accounting for more deaths than colon, breast, and prostate cancers combined, we are very pleased to begin this Phase 3 trial to advance the knowledge about the role ARQ 197 might have in the treatment of patients with non-small cell lung cancer in combination with erlotinib," said Dr. Kazunori Hirokawa, global head of R&D Unit, Daiichi Sankyo. "It is our hope and expectation that this late-stage study will confirm the results we observed in patients with non-squamous cell histology in Phase 2, which showed promise toward extending overall survival and progression-free survival in this group when ARQ 197 was combined with erlotinib."

"The start of this Phase 3 trial marks a key milestone in the development of ARQ 197 and our partnership with Daiichi Sankyo," said Paolo Pucci, chief executive officer of ArQule. "Lung cancer is a devastating disease and our hope is that ARQ 197 will prove to be an effective treatment option that will help patients diagnosed with this disease."

In October 2010, agreement was reached with the U.S. Food and Drug Administration (FDA) on a Special Protocol Assessment (SPA) for the Phase 3 trial comparing ARQ 197 plus erlotinib against erlotinib plus placebo. The Phase 3 study of ARQ 197 plus erlotinib will enroll 988 patients in 150 sites in the U.S., Canada, Eastern and Western Europe, Australia and Latin America. Additional details are available on www.clinicaltrials.gov.

SOURCE Daiichi Sankyo Company, Limited and ArQule, Inc.