… specifically designed to target EGFRex20ins mutants. Preclinical data reported here
support … of mobocertinib in patients with NSCLC with EGFR exon 20 insertion mutations. …

… EGFR) inhibitor targeting EGFR gene mutations, including exon 20 insertions (EGFRex20ins),
in non–small … not reached) and median progression-free survival of 7.3 months (4.4–15.6). …

… to gain selectivity by targeting proteins in the vicinity of the alpha C-helix, a binding site
not exploited by … More specifically, mobocertinib inhibited all five variants of EGFR ex20ins …

… with EGFR exon 20 insertion (EGFR ex20ins) mutations, which … treated with immune checkpoint
inhibitors have shown modest … –targeted therapy, in a pooled population of 257 patients …

… mobocertinib target an uncommon NSCLC mutation that has historically marked a poor
prognosis because of innate resistance to previously approved EGFR tyrosine kinase inhibitors. …

… We sought to use commercially available mobocertinib (TAK-788) to characterize the …
EGFR mutations and to probe possible on-target mechanisms of resistance (including …

… small molecule TKIs [20,21,22] and therapeutic options were limited prior to the introduction
of mobocertinib (6, TAK-788, … ester side chain of mobocertinib targeted a selectivity pocket …

… inhibitors of EGFR exon 20 insertion mutations, including the V769_D770insASV and
D770_N771insSVD mutants. … S, Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon …

… (EGFR) tyrosine kinase inhibitor selective for EGFR exon 20 … tumors with EGFR exon 20
insertion (ex20ins) mutations are … oral exon 20–targeted therapy, PRO results with mobocertinib …

… Mobocertinib (TAK-788) is a potent irreversible tyrosine … ability of mobocertinib to inhibit
HER2 exon 20 insertions in vitro. … of HER2 exon 20 insertion mutations responded differently to …