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Table 3 Advances of HER2-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

Lapatinib

Tykerb

GlaxoSmithKline

EGFR, HER2

Combined with capecitabine for HER2-overexpressed metastatic breast cancer who has received prior therapy including an anthracycline, a taxane, and trastuzumab

2007 [76]

Combined with letrozole for 1L postmenopausal HER2-overexpressed and HR + metastatic breast cancer

2010 [78]

Neratinib

Nerlynx

Puma Biotechnology Inc

EGFR, HER2, HER4

Extended adjuvant treatment for patients with early-stage HER2 + breast cancer

2017 [79]

Combined with capecitabine for HER2 + metastatic breast cancer who has received two or more prior anti-HER2 based regimens in the metastatic setting

2020 [80]

Pyrotinib

-

Jiangsu Hengrui

EGFR, HER2, HER4

Combination with capecitabine for HER2-positive metastatic breast cancer 

2018& [81, 82]

HER2 exon 20 mutant advanced NSCLC

NCT02535507 [202]

Tucatinib

Tukysa

Seattle Genetics

HER2

Combination with trastuzumab and capecitabine for unresectable or metastatic HER2-Positive breast cancer

2020 [84]

  1. In the last column of “Approved years or current phases of clinical trials”, we provided data of the approved years by Food and Drug Administration (FDA), except pyrotinib with a superscript “&” which means it was approved by National Medical Products Administration (NMPA)
  2. Data source: www.fda.govwww.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)