Oral Tyrosine Kinase Inhibitor for EGFR Exon 20-Insertion-Positive NSCLC

Mobocertinib is a first-in-class irreversible tyrosine kinase inhibitor that was designed to selectively target in-frame EGFR exon 20 insertion (EGFRex20ins) mutations in non–small-cell lung cancer (NSCLC). In a multicenter phase 1/2 nonrandomized study, 114 patients with EGFRex20ins-positive NSCLC previously treated with platinum-based chemotherapy received mobocertinib (160 mg once daily) until disease progression or unacceptable toxicity.

At a median 14.2 months' follow up, the objective response rate by independent review — the primary endpoint — was 28% (95% confidence interval, 20%–37%). An additional 50% of patients had stable disease, for a disease control rate of 78%. The median duration of response was 17.5 months (95% CI, 7.4–20.3…