Table 6.
List of IC50 values (nano-molar) among first-generation (gefitinib, erlotinib), second-generation (afatinib, dacomitinib), and third-generation (AZD9291, CO-1686, HM781-36B, ASP8273) EGFR TKIs against various EGFR genotypes
| First-generation EGFR TKIs
|
Second-generation EGFR TKIs
|
Third-generation EGFR TKIs
|
References | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Gefitinib | Erlotinib | Afatinib | Dacomitinib | AZD9291 | CO-1686 | HM61713 | ASP8273 | ||
| EGFR WT cell line | |||||||||
| Calu3 | 1,933 | 4,101 | 71 | 65 | 650 | NA | NA | NA | 44 |
| NCI-H2073 | 200 | 692 | 30 | 54 | 461 | NA | NA | NA | 44 |
| NCI-H1666 | 46 | 48 | 2.8 | 8.1 | 110 | 770 | NA | 230 | 45 |
| H358 | NA | 449 | 31 | NA | NA | NA | 2,225 | NA | 46 |
| EGFR exon 19-deletion cell line | |||||||||
| PC-9 | 23 | 28 | 0.8 | 0.4 | 8 | NA | NA | NA | 44 |
| PC-9 | 34 | 46 | 3.0 | 17 | 62 | 350 | NA | 19 | 45 |
| NCI-H1650 | 5,100 | 9,900 | 77 | 76 | 340 | 840 | NA | 70 | 45 |
| HCC827 | 7.5 | 9.8 | 0.76 | 0.55 | 4.3 | 45 | NA | 9.9 | 45 |
| HCC827 | NA | 3.2 | 1.8 | NA | NA | NA | 9.2 | NA | 46 |
| EGFR del19/T790M cell line | |||||||||
| PC-9 VanR | 4,232 | 5,778 | 679 | 531 | 40 | NA | NA | NA | 44 |
| PC-9ER | 2,000 | 1,500 | 23 | 27 | 14 | 100 | NA | 14 | 45 |
| EGFR L858R/T790M cell line | |||||||||
| NCI-H1975 | 6,962 | 6,165 | 483 | 335 | 11 | NA | NA | NA | 44 |
| NCI-H1975 | 9,700 | 10,000 | 230 | 110 | 28 | 140 | 26 | NA | 45 |
| NCI-H1975 | NA | 2,253 | 53 | NA | NA | NA | 10 | NA | 46 |
Abbreviations: IC50, half-maximal inhibitory concentration; TKIs, tyrosine-kinase inhibitors; NA, not available.