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Table 2 EGFR and FGFR inhibitors and the incidence of corneal subepithelial changes

From: Markedly increased ocular side effect causing severe vision deterioration after chemotherapy using new or investigational epidermal or fibroblast growth factor receptor inhibitors

 ClassificationDrugDescriptionTotal prescribed patientspatients referred to OPH (%)Patients With corneal epithelial changes
EGFR inhibitor1st GenerationErlotinibEGFR TKI which binds in a reversible fashion to the ATP binding site of the receptor2296314 (13.68)0
GefitinibEGFR TKI which binds to ATP binding site of the receptor2772453 (16.34)0
2nd GenerationAfatinibselectively 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.30226 (8.61)0
3rd GenerationOsimertiniba third generation EGFR inhibitor which shows 200-fold selectivity for T790 M/L858R protein over wild-type EGFR202158 (78.22)1 (0.50%)
OlmutinibEGFR mutation-specific tyrosine kinase inhibitor7928 (35.44)0
YH25448a Highly Selective third Generation EGFR TKI1010 (100.00)0
Naquotinibbinds to and inhibits the activity of mutant forms of EGFR, including the T790 M EGFR mutant1111 (100.00)0
Rociletinibinhibits T790 M, a secondary acquired resistance mutation, as well as other mutant EGFRs114 (36.36)0
BBB penetratingAZD3759a novel EGFR tyrosine kinase inhibitor with high capability to penetrate the BBB1212 (100.00)0
EGFR mAbCetuximaba chimeric monoclonal antibody which binds to and inhibits EGFR97489 (9.14)0
JNJ-61186372bispecific antibody that targets EGFR and cMet95 (55.56)0
Ab-ADCABT-414an investigational compound targeting a tumor-selective EGFR epitope55 (100.00)5 (100.0%)
multi TKIVandetaniba selective inhibitor of EGFR and vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase1910 (52.63)3 (15.79%)
FGFR inhibitor ASP5878a novel drug which inhibits all FGFRs targeting FGF19-expressing HCC22 (100.00)1 (50.0%)
FGFR mAbFPA144an enhanced Monoclonal Antibody against FGFR2b1111 (100.00)2 (18.18%)
multi TKIPazopaniba 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)21 (50.00)0
RegorafenibMultikinase inhibitor (VEGFR 1–3, PDGFR-alpha, PDGFR-beta, etc)15422 (14.29)0
  1. 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