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