Development and Challenges of the Discovery of HER2 Inhibitors

Mini Rev Med Chem. 2020;20(20):2123-2134. doi: 10.2174/1389557520666200729162118.

Abstract

The treatment of cancer has always been a major problem in the world. Some cancers cannot be treated with surgery, but only with cancer drugs. Among many cancer drugs, small molecule inhibitors play an irreplaceable role. HER2 is one of the HER families, and the development of HER2 inhibitors has made a huge contribution to the treatment of cancer. Some HER2 inhibitors are already on the market, and some HER2 inhibitors are undergoing clinical research. The design, synthesis and development of new HER2 inhibitors targeting different targets are also ongoing, and some are even under clinical research. The HER2 inhibitors that are on the market have developed resistance, which brings great challenges to the HER2 inhibitor development in the future. This article reviews the development and challenges of the discovery of HER2 inhibitors.

Keywords: Cancer; HER2; challenges; discovery; drug resistance; inhibitors.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Drug Development*
  • Female
  • Humans
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Receptor, ErbB-2 / antagonists & inhibitors*
  • Receptor, ErbB-2 / metabolism

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • ERBB2 protein, human
  • Receptor, ErbB-2