CAMBRIDGE, MA, USA I February 1, 2016 I ARIAD Pharmaceuticals, Inc. (NASDAQ:ARIA) today 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.
“ARIAD scientists designed AP32788 using our integrated drug discovery program to target cancer orphan subsets that are genetically defined but have no current targeted treatment options. This compound specifically addresses the needs of patients with NSCLC driven by EGFR exon 20 or HER2 mutations, who currently have a poor prognosis and limited treatment options,” stated Timothy P. Clackson, president of research and development and chief scientific officer of ARIAD. “Data on the preclinical characterization of AP32788 have been submitted for presentation at the American Association of Cancer Research annual meeting in April.”
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.1 In addition, patients with HER2 mutations, mostly exon 20 insertion mutations, comprise approximately 2 percent of NSCLC patients2 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.
About AP32788
AP32788 is an investigational oral tyrosine kinase inhibitor (TKI) of activating mutations in EGFR and HER2. The molecule was designed to address the unmet need in patients with non-small cell lung cancer (NSCLC) driven by exon 20 insertion mutations in EGFR and HER2, and is ARIAD’s fourth internally discovered oncology IND to be cleared for clinical development.
About ARIAD
ARIAD Pharmaceuticals, Inc., headquartered in Cambridge, Massachusetts and Lausanne, Switzerland, is an integrated global oncology company focused on transforming the lives of cancer patients with breakthrough medicines. ARIAD is working on new medicines to advance the treatment of various forms of chronic and acute leukemia, lung cancer and other difficult-to-treat cancers. ARIAD utilizes computational and structural approaches to design small-molecule drugs that overcome resistance to existing cancer medicines. For additional information, visit http://www.ariad.com or follow ARIAD on Twitter (@ARIADPharm).
1 Costa, D. 2015. EGFR Exon 20 Insertion in Non-Small Cell Lung Cancer. My Cancer Genome http://www.mycancergenome.org/content/disease/lung-cancer/egfr/64/ (Updated November 5, 2015).
2 JCO April 22, 2013 JCO.2012.45.6095
SOURCE: Ariad Pharmaceuticals
