ARIAD Pharmaceuticals (NASDAQ:ARIA) has initiated a Phase 1/2 clinical trial of AP32788, an investigational 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.
AP32788 targets tumors driven by EGFR or HER2 kinases and was designed to achieve selective inhibition of these kinases with exon 20 mutations. There are currently no approved targeted treatment options available for the approximately 4% to 9% of EGFR-mutated lung tumors with exon 20 insertion mutations in NSCLC patients.
The trial will be conducted in two parts: a dose escalation phase, followed by an expansion phase.
The initial Phase 1 dose-escalation trial segment will include 20-to-30 patients with advanced NSCLC, who are refractory to standard available therapies. The primary objective of the Phase 1 segment of the trial is to determine the safety, tolerability, pharmacokinetic profile, and recommended Phase 2 dose of orally administered AP32788.
The Phase 2 segment of the trial will enroll approximately 80 patients and will evaluate anti-tumor activity of AP32788 in these molecularly defined patient populations.
“While there are approved TKIs for use in NSCLC patients with common EGFR activating mutations, there is a need for targeted treatment options to address the subset of patients with EGFR exon 20, HER2, and other uncommon EGFR mutations,” Dr. Robert Doebele, associate professor, division of medical oncology, University of Colorado, said in a statement.