Table 1.
Comparison of three-generation EGFR-TKIs
| Representative drugs | Types of inhibitors | Targets of EGFR | ORR (%) |
PFS (months) | OS (months) | Ref |
|---|---|---|---|---|---|---|
| First-generation EGFR- TKIs | ||||||
| Gefitinib | Reversible | Ex19del, L858R | 67–74 | 9.2–11.9 | 30.5–38.8 | [5, 6] |
| Erlotinib | Reversible | Ex19del, L858R | 64 | 9.7–13.1 | 19.3 | [34, 35] |
| Icotinib | Reversible | Ex19del, L858R | / | 11.2 | 30.5 | [36, 37] |
| Second-generation EGFR-TKIs | ||||||
| Afatinib | Irreversible | Ex19del, L858R | 70 | 11.0–13.6 |
19.6–27.6* 30.7–33.3* |
[7, 39, 41, 42] |
| Dacomitinib | Irreversible | Ex19del, L858R | 75 | 14.7 | 34.1 | [8, 44] |
| Third-generation EGFR- TKIs | ||||||
| Osimertinib | Irreversible |
Ex19del, L858R T790M |
80 | 18.9 | 38.6 | [22, 46] |
| Aumolertinib | Irreversible |
Ex19del, L858R T790M |
74 | 19.3 | NR | [47] |
| Furmonertinib | Irreversible |
Ex19del, L858R T790M |
74 | 20.8 | NR | [48, 243] |
| Lazertinib | Irreversible |
Ex19del, L858R T790M |
55 | 11.1 | NR | [244, 245] |
EGFR-TKIs epidermal growth factor receptor tyrosine kinase inhibitors, wt wild type, ORR objective response rate, PFS progression-free survival, OS overall survival, NR not reached
*The upper data was derived from patients with L858R and the lower data was derived from patients with Ex19del. All exhibited data were derived from clinical trials in which drug as monotherapy in the first-line setting