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. 2020 Jan 9;20:19. doi: 10.1186/s12886-019-1285-9

Table 2.

EGFR and FGFR inhibitors and the incidence of corneal subepithelial changes

Classification Drug Description Total prescribed patients patients referred to OPH (%) Patients With corneal epithelial changes
EGFR inhibitor 1st Generation Erlotinib EGFR TKI which binds in a reversible fashion to the ATP binding site of the receptor 2296 314 (13.68) 0
Gefitinib EGFR TKI which binds to ATP binding site of the receptor 2772 453 (16.34) 0
2nd Generation Afatinib selectively and irreversibly binds to and inhibits the EGFR 1, 2, and 4, and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. 302 26 (8.61) 0
3rd Generation Osimertinib a third generation EGFR inhibitor which shows 200-fold selectivity for T790 M/L858R protein over wild-type EGFR 202 158 (78.22) 1 (0.50%)
Olmutinib EGFR mutation-specific tyrosine kinase inhibitor 79 28 (35.44) 0
YH25448 a Highly Selective third Generation EGFR TKI 10 10 (100.00) 0
Naquotinib binds to and inhibits the activity of mutant forms of EGFR, including the T790 M EGFR mutant 11 11 (100.00) 0
Rociletinib inhibits T790 M, a secondary acquired resistance mutation, as well as other mutant EGFRs 11 4 (36.36) 0
BBB penetrating AZD3759 a novel EGFR tyrosine kinase inhibitor with high capability to penetrate the BBB 12 12 (100.00) 0
EGFR mAb Cetuximab a chimeric monoclonal antibody which binds to and inhibits EGFR 974 89 (9.14) 0
JNJ-61186372 bispecific antibody that targets EGFR and cMet 9 5 (55.56) 0
Ab-ADC ABT-414 an investigational compound targeting a tumor-selective EGFR epitope 5 5 (100.00) 5 (100.0%)
multi TKI Vandetanib a selective inhibitor of EGFR and vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase 19 10 (52.63) 3 (15.79%)
FGFR inhibitor ASP5878 a novel drug which inhibits all FGFRs targeting FGF19-expressing HCC 2 2 (100.00) 1 (50.0%)
FGFR mAb FPA144 an enhanced Monoclonal Antibody against FGFR2b 11 11 (100.00) 2 (18.18%)
multi TKI Pazopanib a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis (inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-alpha, beta receptors, cytokine receptor) 2 1 (50.00) 0
Regorafenib Multikinase inhibitor (VEGFR 1–3, PDGFR-alpha, PDGFR-beta, etc) 154 22 (14.29) 0

EGFR epidermal growth factor receptor, ATP adenosine triphosphate, FGFR fibroblast growth factor receptor, OPH ophthalmology department, BBB blood-brain barrier, mAb monoclonal antibody, cMet tyrosine-protein kinase Met, Ab-ADC antibody-drug conjugate, TKI tyrosine kinase inhibitor, VEGFR Vascular Endothelial Growth Factors, PDGFR Platelet-derived growth factor receptor