HER2 is a clinically proven receptor tyrosine kinase target that is over-expressed in breast cancer and other cancers such as gastric and ovarian cancer. Herceptin (trastuzumab), the intravenously-dosed protein inhibitor that modulates HER2, has been approved for HER2 positive metastatic breast cancer patients as well as an adjuvant to surgery in early stage breast cancer patients. The second indication has significantly expanded the number of breast cancer patients eligible for an HER2 inhibitor.
ARRY-380 is an orally active, reversible and selective HER2 inhibitor. In multiple preclinical tumor models, ARRY-380 was well tolerated and demonstrated significant dose-related tumor growth inhibition that was superior to Herceptin and Tykerb (lapatinib). Additionally, in these models, ARRY-380 was well tolerated and additive for tumor growth inhibition when dosed in combination with the standard of care therapeutics Herceptin or Taxotere (docetaxel).
Array continues dose escalation in a Phase 1 trial with ARRY‑380. The trial is designed to evaluate the safety, maximum tolerated dose and pharmacokinetics of ARRY‑380 in patients with advanced cancer. Array announced positive interim results of this trial at the 2009 San Antonio Breast Cancer Symposium. These results showed that ARRY-380 at doses greater than or equal to 200 mg BID demonstrated evidence of tumor regression in eight out of ten heavily pre-treated patients with HER2 expressing cancers. Of these eight patients, four had prolonged stable disease for 16 weeks or longer. ARRY-380 has been well-tolerated; the predominant adverse events have been Grade 1 and included nausea, rash and fatigue. In completed cohorts, no Grade 3 or 4 treatment-related adverse events and no cardiac adverse events have been observed.
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