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Table 1 Advances of EGFR-TKIs

From: Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

Drug

Brand name

Manufacturer

Targets

Applications of diseases

Approved years or current phases of clinical trials

Gefitinib

Iressa

AstraZeneca

EGFR-sensitizing mutations

Inoperable or recurrent NSCLC

2002§

1L metastatic EGFR-sensitizing mutant NSCLC

2015 [14, 15]

Erlotinib

Tarceva

OSI/Genentech

EGFR-sensitizing mutations

Locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen

2004 [16]

1L advanced EGFR-sensitizing mutant NSCLC

2016 [16]

Combined with ramucirumab for 1L advanced EGFR-sensitizing mutant NSCLC

2020 [191]

Icotinib

-

Shanghai Beta

EGFR-sensitizing mutations

Locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen

2011&

1L metastatic EGFR-sensitizing mutant NSCLC

2014& [17, 18

Afatinib

Gilotrif

Boehringer Ingelheim

EGFR, HER2

Metastatic EGFR-sensitizing mutant NSCLC

2013 [227,193,194]

Advanced SqCC of Lung whose disease has progressed after treatment with platinum-based chemotherapy

2016 [195]

1L metastatic NSCLC with non-resistant EGFR mutations (L861Q, G719X and S768I)

2018 [192, 196]

Dacomitinib

Vizimpro

Pfizer Inc

EGFR, HER2

1L metastatic EGFR-sensitizing mutant NSCLC

2018 [22, 23]

Osimertinib

Tagrisso

AstraZeneca

EGFR T790M, EGFR-sensitizing mutations

EGFR-T790M NSCLC

2015 [25]

1L metastatic EGFR-sensitizing mutant NSCLC

2018 [26, 27]

Metastatic or recurrent NSCLC with EGFR mutations other than the exon 19 deletion, L858R and T790M mutations, and exon 20 insertion

II [44]

Almonertinib

-

Jiangsu Hansoh

EGFR T790M, EGFR-sensitizing mutations

EGFR-T790M NSCLC

2020& [32]

1L locally advanced or metastatic pulmonary adenosquamous carcinoma

III (NCT04354961)

Investigational drugs

AST2818 (furmonertinib)

-

Shanghai Allist

EGFR T790M, EGFR-sensitizing mutations

Advanced EGFR-T790M NSCLC

II [33, 34]

1L locally advanced or metastatic EGFR-sensitizing mutant NSCLC

III (NCT03787992)

YH25448 (lazertinib)

-

Yuhan

EGFR T790M, EGFR-sensitizing mutations

Advanced EGFR-activating mutated NSCLC

I/II [35]

1L locally advanced or metastatic EGFR-sensitizing mutant NSCLC

III (NCT04248829)

BPI-7711

-

Shanghai Beta

EGFR T790M, EGFR-sensitizing mutations

EGFR-T790M advanced or recurrent NSCLC

I [36] IIb (NCT03812809)

1L locally advanced or recurrent/metastatic EGFR-sensitizing mutant NSCLC

III (NCT03866499)

EGF816 (nazartinib)

-

Novartis

EGFR T790M, EGFR-sensitizing mutations

Advanced EGFR-mutant NSCLC

I [37]

TAK-788 (mobocertinib)

-

Takeda

EGFR, HER2

Metastatic NSCLC with EGFR exon 20 insertions whose disease has progressed on or after platinum-based chemotherapy

2020/4/27 Breakthrough therapy recognition [45]

1L locally advanced or metastatic NSCLC with EGFR exon 20 insertions

III (NCT04129502)

Poziotinib

-

Hanmi

EGFR, HER2, HER4

 ≥ 2L advanced NSCLC with EGFR exon 20 insertions

II [46]

Tarloxotinib

-

Rain

EGFR, HER2, NRG fusion

2L NSCLC with EGFR exon 20 insertion or HER2-activating mutation, solid tumors With NRG1/ERBB family gene fusions

[197] II (NCT03805841)

TQB3804

-

Jiangsu ChiaTai Tianqing

EGFR T790M, C797S, EGFR-sensitizing mutations

Osimertinib-resistant EGFR T790M/C797S mutant NSCLC

[42] I (NCT04128085)

EAI045

-

CSN

L858R, EGFR T790M, C797S

Combined with cetuximab for osimertinib-resistant EGFR T790M/C797S mutant NSCLC

[41]

  1. In the last column of “Approved years or current phases of clinical trials”: if a drug has been approved, we provided data of the year of its approval by Food and Drug Administration (FDA) except gefitinib with a superscript “§” which means it was firstly approved by Ministry of Health, Labor and Welfare (MHLW), and almonertinib with a superscript “&” which means it was approved by National Medical Products Administration (NMPA); if a drug is under investigation, we provided current phases of its clinical trials
  2. EGFR epidermal growth factor receptor, TKIs tyrosine kinase inhibitors, EGFR-sensitizing mutations: EGFR exon 19 deletions or exon 21 L858R substitution mutations, SqCC squamous cell carcinoma
  3. Data source: www.fda.govwww.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)