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.

癌症的治疗一直是世界上的主要问题。有些癌症不能通过手术治疗，而只能用抗癌药物治疗。在许多抗癌药物中，小分子抑制剂起着不可替代的作用。HER2是HER家族之一，HER2抑制剂的开发为癌症的治疗做出了巨大贡献。一些HER2抑制剂已经在市场上，并且一些HER2抑制剂正在临床研究中。针对不同靶标的新型HER2抑制剂的设计，合成和开发也正在进行中，有些甚至还在临床研究中。市场上的HER2抑制剂已产生抗药性，这对未来HER2抑制剂的开发提出了巨大的挑战。本文概述了HER2抑制剂的发现和发展。