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Table 1 Selected clinical efficacy reports of third-generation EGFR-TKIs

From: Update on recent preclinical and clinical studies of T790M mutant-specific irreversible epidermal growth factor receptor tyrosine kinase inhibitors

Drug name

Number

Patient group

Dose

ORR

PFS

AEs (% total, % ≥ grade 3)a

ILD (%)

Distinct AEs

Osimertinib

411

EGFR-TKI pretreated advanced EGFR T790M–positive NSCLC

80 mg/day

66% (95% CI, 61–71)

11.0 months (95% CI 9.6–12.4)

Skin rash (41, < 1), diarrhea (38, < 1), dry skin (30, 0), QTc prolongation (3, 1)

3

Neutropenia, lymphopenia, thrombocytopenia, hyponatremia, QTc prolongation

Rociletinib

548

EGFR-TKI pretreated advanced EGFR T790M–positive NSCLC

500–750 mg twice per day

33.9% (95% CI, 29.5–38.5)

5.7 months (95% CI 4.2–6.2) at 500 mg twice a day

Hyperglycemia (65.2, 35.2), skin rash (11.7, 0.4), diarrhea (57.5, 4.6), QTc prolongation (30.1, 10.2)

2.4

Hyperglycemia, cataract, QTc prolongation, pancreatitis

Olmutinib

76

EGFR-TKI pretreated advanced EGFR T790M–positive NSCLC

800 mg/day

54%

6.9 months(95% CI 5.36–9.49)

Diarrhea (59, 0), pruritus (42, 1), rash (41, 5), nausea (39, 0), Palmar-plantar erythrodysesthesia syndrome (30, 4)

1

Palmar-plantar erythrodysesthesia syndrome

EGF816

152

Advanced EGFR mutation-positive NSCLCb

75–350 mg/day

46.9% (95% CI, 38.7–55.3)

9.7 months (95% CI 7.3–11.1)

Skin rash (53.9, 16.4), diarrhea (36.8, 2), pruritus (34.2, NA), dry skin (25.0, NA), stomatitis (24.3, 2.0)

0.7

Distinct skin rash, hepatitis B virus reactivation, increased serum lipase level

ASP8273

63

Advanced EGFR mutation-positive NSCLC (92% harbored EGFR T790M)

300 mg/day

30% (95% CI, 19.2–43.0)

6.0 months (95% CI 4.1–9.8)

Diarrhea (48, 2), nausea (27, 0), paresthesia (14, 0), vomiting (13, 0), dizziness (11, 0), and hyponatremia (19, 13)

0

Hyponatremia, paresthesia

  1. Abbreviations: EGFR epidermal growth factor receptor, TKI tyrosine kinase inhibitor, ORR objective response rate, PFS progression-free survival, AE adverse event, ILD interstitial lung disease, NSCLC non-small cell lung cancer, CI confidence interval, QTc QT interval corrected for heart rate, NA not available
  2. aFor each AE, reported values in this column are (the percent of patients receiving the therapy who experience the AE, the percent of patients receiving the therapy who experienced the AE at grade ≥ 3)
  3. bIncluding patients harbored sensitizing EGFR mutations following EGFR-TKI therapy (regardless of EGFR T790M status), EGFR exon 20 insertion or deletion, de novo T790M mutation, and patients with treatment-naïve advanced EGFR mutation-positive NSCLC
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Journal of Biomedical Science

ISSN: 1423-0127