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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Monoclonal Antibodies, Small Molecule Inhibitors and Antibody-drug Conjugates as HER2 Inhibitors

Author(s): Xiu-Fang Li, Chen-Fu Liu and Guo-Wu Rao*

Volume 28 , Issue 17 , 2021

Published on: 08 September, 2020

Page: [3339 - 3360] Pages: 22

DOI: 10.2174/0929867327666200908112847

Price: $65


Overexpression of human epidermal growth factor receptor (HER)-2 is found in a variety of cancers, often portending poor clinical outcomes. Therefore, HER2 is an attractive target for treatment. This review describes the research progress of HER2 targeted inhibitors in recent years. Excellent reviews are available, so we focus on the development, mechanisms of action, and structure-activity relationships of different types of inhibitors, including monoclonal antibodies, small molecule inhibitors, and antibody-drug conjugates (ADCs). In addition, the differences among them are compared.

Keywords: HER2, ErbB2, tyrosine kinase, inhibitors, monoclonal antibody, antibody-drug conjugate.

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