Date: 2016-04-19
Type of information: Presentation of results at a congress
phase: preclinical
Announcement: presentation of results at the American Association for Cancer Research (AACR) Annual Meeting
Company: Ariad Pharmaceuticals (USA - MA)
Product: AP32788
Action
mechanism: tyrosine kinase inhibitor. 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.
Disease:
Therapeutic area: Cancer - Oncology
Country:
Trial details:
Latest
news: * On April 19, 2016, Ariad Pharmaceuticals announced the results of comprehensive preclinical studies on its investigational tyrosine kinase inhibitor (TKI), AP32788, at the American Association for Cancer Research (AACR) Annual Meeting 2016. AP32788 is a TKI designed to target specific mutations in EGFR or HER2 present in a subset of patients with non-small cell lung cancer (NSCLC), for whom there are currently no targeted therapies available. The research conducted by Ariad scientists showed that in a matched set of engineered cell lines, AP32788 inhibited all tested EGFR and HER2 mutants, including exon 20 insertion mutants, with selectivity over wild-type (WT) EGFR. Inhibition of WT EGFR in non-tumor cells has been associated with dose-limiting toxicities of EGFR inhibitors in patients. Enzymatic analysis confirmed that AP32788 irreversibly inactivated EGFR exon 20 with 20-fold selectivity over WT EGFR, in contrast to other tested EGFR TKIs. AP32788 also induced tumor regressions in a mouse EGFR exon 20 model at doses that were well tolerated.
