|ARIAD Presents New Preclinical Data Showing AP26113 Inhibits Clinically Relevant Mutants of ALK and ROS1|
The research conducted by ARIAD scientists was determined using cell lines harboring crizotinib-resistant mutant forms of ALK and oncogenic ROS1 fusions, tested in both in vitro studies and mouse-disease models.
“This preclinical research demonstrates that AP26113 inhibits all nine
clinically identified crizotinib-resistant ALK mutations, at plasma
concentrations we know to be clinically achievable,” said
AP26113 was also shown to inhibit ROS1 fusions as potently as it inhibits ALK, to retain activity against the gatekeeper mutation of ROS1, and to substantially suppress the outgrowth of resistant ROS1 cells in a mutation assay, all at clinically achievable plasma concentrations. These data suggest that AP26113 may be able to avoid the emergence of drug-resistant mutants in NSCLC patients with these oncogenic gene fusions.
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