EGFR-TKI | IC50 (nM) | |||||
---|---|---|---|---|---|---|
L858R | L858R/L747S | L858R/D761Y | L858R/T854A | L858R/T790Â M | ||
First-generation | gefitinib | 3.38 (1) | 15.1 (5.6) | 29.4 (8.7) | 222 (68) | 8568 (2535) |
erlotinib | 1.82 (1) | 8.68 (4.8) | 11.1 (6.2) | 85.9 (47) | 5377 (2955) | |
Second-generation | afatinib | 0.21 (1) | 0.24 (1.1) | 0.82 (3.9) | 2.13 (10) | 73.1 (116) |
dacomitinib | 0.27 (1) | 0.41 (1.5) | 1.16 (4.3) | 3.19 (12) | 38.1 (146) | |
neratinib | 6.44 (1) | 13.91 (2.2) | 23.8 (3.7) | 77.2 (12) | 707 (110) | |
Third-generation | osimertinib | 1.98 (1) | 1.74 (0.9) | 2.74 (1.4) | 1.98 (1) | 3.67 (1.3) |
rociletinib | 5.22 (1) | 4.69 (0.9) | 6.71 (1.3) | 6.94 (1.3) | 7.08 (1.4) |