转染时重排(RET)是一种跨膜酪氨酸激酶受体。由于突变、基因融合或过度表达，RET信号异常可能导致癌症。已批准了6种抑制剂用于治疗RET驱动的癌症，包括:凡德他尼、卡博替尼、雷伐替尼、索拉非尼、塞博替尼和普西替尼。只有塞博替尼和普西替尼是专门为RET开发的，而其余则是多靶点激酶抑制剂。还有几个其他的RET靶向候选药物正在临床开发中。本综述涵盖了自2016年以来至今活性物质对抗RET相关的最新专利文献。由于RET的改变在几乎2%的所有癌症中都会发生，所以它代表了一个重要的治疗靶点。最近获得批准的RET靶向治疗是专门为靶向RET癌基因而开发的。这些批准代表了从上一个十年向现在重点关注开发选择性RET抑制剂的范式转变。这些新获批的RET抑制剂仍然存在药物抗性问题。下一代的RET抑制剂必须发展出来以阻断常见的耐药突变。为了实现这一目标，RET抑制剂应与基因组分析相结合，以确保针对最相关的临床突变。

Rearranged during transfection (RET) is a transmembrane receptor tyrosine kinase. Aberrations in RET signaling due to mutations, gene fusions, or overexpression can lead to carcinomas. Six inhibitors have been approved for the treatment of RET-driven cancers: vandetanib, cabozantinib, lenvatinib, sorafenib, selpercatinib, and pralsetinib. Only selpercatinib and pralsetinib have been developed specifically for RET, while the remaining are multikinase inhibitors. Several other RET targeted candidates are under clinical development.This review covers recent patent literature describing small molecules that are active against RET since 2016 till present.RET represents a major therapeutic target as its alterations occur in nearly 2% of all cancers. Recent approvals for RET targeted therapy have been developed specifically to target the RET oncogene. These approvals represent a paradigm shift from the last decade to now focus on the development of selective RET inhibitors rather than multikinase inhibitors. These newly approved RET inhibitors still have clinical issues with drug resistance. It is imperative that the next iteration of RET inhibitors are developed to block common treatment-resistant mutations. To accomplish this, RET inhibitors should be developed in concert with genomic profiling to ensure the most relevant clinical mutations are targeted.