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. 2017 Nov 30;8(69):114371–114392. doi: 10.18632/oncotarget.22825

Table 1. Selected ERBB family mutations found in patients.

ERBB mutation Principle tumor type (cBioPortal) Drug sensitivity Drug insensitivity Acquired resistance
EGFR R108G/K Glioma preclinical: erlotinib [143]
EGFR A289D/I/N/T/V Glioma preclinical: erlotinib [143]
EGFR E709A/K/Q NSCLC preclinical: afatinib, neratinib [144]
EGFR exon 18 insertions/deletions NSCLC preclinical, clinical: afatinib, neratinib [144]
EGFR G719A/C/D/S NSCLC clinical: erlotinib, gefitinib, afatinib [145], [35]
EGFR exon 19 insertions/deletions NSCLC clinical: erlotinib, gefitinib, afatinib [146]
EGFR exon 20 insertions/deletions NSCLC preclinical: EGF816, AP32788 [36, 37] clinical: afatinib, gefitinib, erlotinib [147],[148],[35]
EGFR S768G/I/T NSCLC clinical: afatinib, gefitinib, erlotinib [149], [35]
EGFR T790M NSCLC clinical: osimertinib [28]; preclinical: EA1045 and cetuximab [34] clinical: afatinib [26, 27] clinical: gefitinib, erlotinib, afatinib [18, 19]
EGFR C797S/Y NSCLC preclinical: EA1045 and cetuximab [34] clinical: osimertinib [32, 33]
EGFR L858R NSCLC clinical: gefitinib, erlotinib, afatinib [10],[11]
EGFR L861Q/R NSCLC, lung squamous clinical: gefitinib, erlotinib, afatinib [145], [35]
ERBB2 D277G/H/V/Y bladder preclinical: lapatinib, afatinib [80]
ERBB2 S310F/Y bladder, breast, esophagogastric, colorectal, lung, cervical preclinical: trastuzumab, lapatinib, neratinib, afatinib [77, 79, 80, 90]; clinical: neratinib [103, 105] preclinical: cetuximab, panitumumab [79]
ERBB2 R678Q esophagogastric, colorectal, bladder preclinical: lapatinib, afatinib, neratinib [77, 80]
ERBB2 L755S breast, bladder, colorectal preclinical: neratinib, afatinib [77, 112]; clinical: neratinib [98, 103, 105] preclinical: trastuzumab, lapatinib, cetuximab, panitumumab [77, 79, 85, 112] preclinical: lapatinib [112]
ERBB2 D769H/Y breast, bladder, esophagogastric, colorectal preclinical: trastuzumab, lapatinib, neratinib [77]; clinical: neratinib [103]
ERBB2 exon 20 insertions/deletions NSCLC preclinical: lapatinib, afatinib, neratinib, AP32788 [36, 73, 77, 82, 84, 93]; clinical: trastuzumab, afatinib, neratinib, dacomitinib [96, 100-103, 105] [150], [97] preclinical: erlotinib, gefitinib [73, 82, 93] clinical: osimertinib [29]
ERBB2 V777L breast, colorectal, esophagogastric preclinical: trastuzumab, lapatinib, neratinib [77, 79, 85] clinical: neratinib [91] preclinical: cetuximab, panitumumab [79]
ERBB2 T798I/M breast preclinical: afatinib [91] preclinical: trastuzumab, lapatinib, neratinib [85, 91, 111] clinical: neratinib [91]
ERBB2 V842I colorectal, breast, esophagogastric, endometrial preclinical: trastuzumab, lapatinib, neratinib [77, 79]; clinical: neratinib [103] preclinical: cetuximab, panitumumab [79]
ERBB2 L869R breast preclinical: neratinib, afatinib [91]; clinical: neratinib [92, 103, 105] preclinical: lapatinib [91]
ERBB3 V855A NSCLC preclinical: pertuzumab and afatinib [128]
ERBB3 mutations multiple tumor types clinical: neratinib [105]
ERBB4 KD mutations melanoma, esophagogastric, colorectal preclinical: lapatinib [132]