ARIAD Pharma Reports Positive Preclinical Data Of Brigatinib - Quick Facts

(RTTNews) - ARIAD Pharmaceuticals, Inc. (ARIA) announced Wednesday that in the preclinical data, brigatinib, its investigational oral tyrosine kinase inhibitor, was shown to be a highly potent and selective inhibitor of anaplastic lymphoma kinase or ALK, inhibiting ALK at lower concentrations than crizotinib, ceritinib, and alectinib.

Furthermore, in these studies, brigatinib was the only inhibitor that showed activity against all 17 tested ALK mutants that have been associated with preclinical or clinical resistance to existing ALK inhibitors, including G1202R. In addition, compared to crizotinib, brigatinib was shown to significantly prolong survival of mice with ALK+ tumors in the brain.

Brigatinib is an investigational, targeted cancer medicine discovered internally at ARIAD. It is in development for the treatment of patients with anaplastic lymphoma kinase positive (ALK+) non-small cell lung cancer (NSCLC).

The design and preclinical characterization of brigatinib are described in an article titled, "The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models," in the journal Clinical Cancer Research.

Victor Rivera, vice president of preclinical & translational research at ARIAD, said, "We believe that these preclinical findings support a molecular basis for the promising systemic and intracranial activity in ALK+, crizotinib-resistant NSCLC patients being treated with brigatinib in clinical trials and further validate our ongoing clinical research to understand the potential of brigatinib to address mutations associated with disease progression. In addition, we believe that these findings support testing brigatinib as initial therapy in ALK+ NSCLC patients, to see if the greater in vitro potency of brigatinib also manifests in human trials as deeper and more durable responses compared to crizotinib, and whether emergence of ALK resistance mutations can be delayed or even circumvented."

ARIAD has commenced the Phase 3 ALTA 1L clinical trial to compare brigatinib and crizotinib in ALK+ NSCLC patients who have not received prior ALK inhibitors.