Drug intelligence / Profile preview

apatinib + trastuzumab

Development stage
Preclinical
Lead developer
Jiangsu Hengrui Medicine
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Apatinib + trastuzumab is a combination therapy consisting of two distinct agents used primarily in the treatment of HER2-positive cancers, particularly breast and gastric cancer that have become resistant to standard HER2-targeted therapies. Apatinib is a small molecule tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptor 2 (VEGFR-2), thereby blocking angiogenesis and reducing tumor blood supply. Trastuzumab is a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2/ERBB2), inhibiting downstream signaling pathways involved in cell proliferation and survival. The combination aims to overcome resistance mechanisms by simultaneously targeting tumor angiogenesis (via VEGFR-2) and HER2-driven signaling pathways. This regimen has been explored in clinical settings for patients with advanced or metastatic HER2-positive breast cancer with brain metastases, as well as for overcoming de novo or acquired resistance to trastuzumab in HER2-positive gastric cancer[1][2][4].

Other names
apatinib and trastuzumabapatinib plus trastuzumab
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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