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Table 1 The cardiotoxicity of EGFR-TKIs

From: Cardiotoxicity of small-molecule kinase inhibitors in cancer therapy

Generation

Name

Chemical structure

Targets

Approved for indications on

Cardiotoxicity

Corporation

EGFR

 First-

Gefitinib (Iressa)

EGFR

NSCLC

05/05/2003

MI, myocarditis, cardiac hypertrophy, AF, left bundle branch block

AstraZeneca

Erlotinib (Tarceva)

EGFR

NSCLC (2004) Pancreatic

cancer (2005)

Myocardial ischemic, MI, HF, venous thromboembolism

Roche/Astellas

Icotinib (Conmana)

EGFR

NSCLC

06/07/2011

ND

BettaPharma

 Second-

Afatinib (Gilotrif)

EGFR

NSCLC

07/2013

diastolic dysfunction, left ventricle enlargement, pericardial effusion

Boehringer

Ingelheim

Dacomitinib

(Vizimpro)

EGFR

NSCLC

10/2018

ND

Pfizer

 Third-

Osimertinib (Tagrisso)

EGFR

NSCLC

11/2015

Acute coronary syndrome, QT interval prolongation, MI, HF, mitral or tricuspid valve regurgitation, AF, pericardial effusion, decreased LVEF, supraven-tricular tachycardia

AstraZeneca

Aumonertinib (Ameile)

EGFR

NSCLC

2020

QT interval prolongation

Hansoh

Furmonertinib (Alflutinib)

EGFR

NSCLC

03/2021

QT interval prolongation, AF

Allist Pharmaceuticals

HER

 HER2

Lapatinib (Tykerb)

EGFR/HER2

Breast cancer

03/2007

Cardiomyopathy, hypotension, arrhythmia, ischemic heart disease, QT prolongation, decreased LVEF, HF

Novartis

 

Neratinib (Nerlynx)

EGFR/HER2/HER4

Breast cancer

07/2017

Arrhythmia, ischemic heart disease, QT interval prolongation, decreased LVEF, HF

Puma Biotech

 

Tucatinib (Tukysa)

HER2

HER2-positive breast cancer

04/2020

ND

Seagen

 

Mobocertinib

(Exkivity)

EGFR/HER2

NSCLC

09/2021

QT interval prolongation, HF

Takeda Pharmaceutical Company

 

Pyrotinib

pan-HER

HER2-positive breast cancer

08/2018

QT interval prolongation

Hengrui Medicine

  1. All data statistics from the FDA (https://www.accessdata.fda.gov)
  2. EGFR: epidermal growth factor receptor; NSCLC: non-small cell lung cancer; MI: myocardial infarction; AF: arial fibrillation; HF: heart failure; HER2: human epidermal growth factor receptor 2; LVEF: left ventricular ejection fraction; ND: No data