ARIAD Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) has completed its review of the Company’s Investigational New Drug (IND) application for AP32788, a tyrosine kinase inhibitor (TKI) designed as a targeted therapy for patients with non-small cell lung cancer (NSCLC) with specific mutations in EGFR or HER2. ARIAD anticipates initiation of its Phase 1/2 clinical trial of AP32788 in patients with NSCLC in the second quarter of 2016.
AP32788 targets tumors driven by EGFR or HER2 kinases and was designed to achieve selective inhibition of exon 20 insertion mutations in these kinases. In preclinical studies, AP32788 potently inhibited EGFR mutations including exon 20 mutations, while remaining selective over native EGFR. It was also active against HER2 activating mutations including exon 20 mutations.
EGFR mutations represent the largest known, targetable subset of NSCLC. While the most common types of EGFR mutation are addressed by approved TKI therapies, there are no targeted treatment options available for the approximately 4 to 9 percent of EGFR-mutated lung tumors with exon 20 insertion mutations. In addition, patients with HER2 mutations, mostly exon 20 insertion mutations, comprise approximately 2 percent of NSCLC patients and also have no current targeted treatment options. ARIAD estimates that there are approximately 6,000 patients in the United States living with EGFR exon 20 or HER2 point mutations, based on a broader data set of 175,000 patients with stage IIIb or IV NSCLC living in the U.S. in 2015, according to Kantar Health.
