Activity and Safety of Mobocertinib (TAK-788) in Previously Treated Non-Small Cell Lung Cancer With EGFR Exon 20 Insertion Mutations From a Phase 1/2 Trial. Cancer discovery Riely, G. J., Neal, J. W., Camidge, D. R., Spira, A. I., Piotrowska, Z. n., Costa, D. B., Tsao, A. S., Patel, J. D., Gadgeel, S. M., Bazhenova, L. n., Zhu, V. W., West, H. L., Mekhail, T. n., Gentzler, R. D., Nguyen, D. n., Vincent, S. n., Zhang, S. n., Lin, J. n., Bunn, V. n., Jin, S. n., Li, S. n., Janne, P. A. 2021


Mobocertinib, an oral epidermal growth factor receptor (EGFR) inhibitor targeting EGFR gene mutations including exon 20 insertions (EGFRex20ins) in non-small cell lung cancer, was evaluated in a phase 1/2 dose-escalation/expansion trial ( NCT02716116). Dose escalation identified 160 mg daily as the recommended phase 2 dose and maximum tolerated dose. Among 136 patients treated with 160 mg daily, the most common any grade treatment-related adverse events (TRAEs; >25%) were diarrhea (83%), nausea (43%), rash (33%), and vomiting (26%), with diarrhea (21%) the only grade {greater than or equal to}3 TRAE >5%. Among 28 EGFRex20ins patients treated at 160 mg daily, the investigator-assessed confirmed response rate was 43% (12/28; 95% confidence interval (CI): 24-63%) with median duration of response of 14 months (5.0-not reached), and median progression-free survival of 7.3 months (4.4-15.6). Mobocertinib demonstrated antitumor activity in patients with diverse EGFRex20ins variants with a safety profile consistent with other EGFR inhibitors.

View details for DOI 10.1158/2159-8290.CD-20-1598

View details for PubMedID 33632775