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Table 1 Comparison of three-generation EGFR-TKIs

From: Therapeutic strategies for EGFR-mutated non-small cell lung cancer patients with osimertinib resistance

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]

  1. 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
  2. *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