Zheng H, Chen Z-S, Li J
The First Affiliated Hospital of China Medical University, Shenyang, China.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York City, New York, USA.
Drugs Today (Barc). 2021 Oct;57(10):621-629. doi: 10.1358/dot.2021.57.10.3313852.
Aberrations in oncogene RET (rearranged during transfection) have been found to be the cause of different kinds of malignancies, especially in lung and thyroid cancers. Targeted therapy of RET-altered cancers using multi-kinase inhibitors (MKIs) has demonstrated limited clinical efficacy due to off-target toxicity. In May 2020, the U.S. Food and Drug Administration (FDA) approved a novel specific RET inhibitor for use in some subtypes of lung and thyroid cancers with RET alterations. In this review, we summarize the mechanism of action, pharmaceutical properties and clinical data of selpercatinib, and share some of our perspectives.
致癌基因RET（转染过程中重排）的畸变已被发现是多种恶性肿瘤的病因，尤其是在肺癌和甲状腺癌中。由于脱靶毒性，使用多激酶抑制剂（MKIs）对RET改变的癌症进行靶向治疗已显示出有限的临床疗效。2020年5月，美国食品药品监督管理局（FDA）批准了一种新型特异性RET抑制剂，用于治疗某些RET改变的肺癌和甲状腺癌亚型。在本综述中，我们总结了塞尔帕替尼的作用机制、药学特性和临床数据，并分享了我们的一些观点。
