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Review
. 2021;28(17):3339-3360.
doi: 10.2174/0929867327666200908112847.

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

Xiu-Fang Li  1 , Chen-Fu Liu  2 , Guo-Wu Rao  1
Affiliations
Review

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

Xiu-Fang Li et al. Curr Med Chem. 2021.

Abstract

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

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