Precious Gene: The Application of RET-Altered Inhibitors

作者全名："Gou, Qitao; Gan, Xiaochuan; Li, Longhao; Gou, Qiheng; Zhang, Tao"

作者地址："[Gou, Qitao; Gan, Xiaochuan; Li, Longhao; Zhang, Tao] Chongqing Med Univ, Affiliated Hosp 1, Dept Oncol, 1 Youyi Rd, Chongqing 400016, Peoples R China; [Gou, Qiheng] Sichuan Univ, West China Hosp, Canc Ctr, Dept Radiotherapy, Chengdu 610041, Peoples R China"

通信作者："Zhang, T (通讯作者)，Chongqing Med Univ, Affiliated Hosp 1, Dept Oncol, 1 Youyi Rd, Chongqing 400016, Peoples R China.; Gou, QH (通讯作者)，Sichuan Univ, West China Hosp, Canc Ctr, Dept Radiotherapy, Chengdu 610041, Peoples R China."

来源：MOLECULES

ESI学科分类：CHEMISTRY

WOS号：WOS:000902800200001

JCR分区：Q2

影响因子：4.6

年份：2022

卷号：27

期号：24

开始页：　

结束页：　

文献类型：Review

关键词：molecular target therapy; small molecule inhibitor; tyrosine kinase inhibitor; RET-selective inhibitor; selpercatinib; pralsetinib; TPX-0046; zetletinib

摘要："The well-known proto-oncogene rearrangement during transfection (RET), also known as ret proto-oncogene Homo sapiens (human), is a rare gene that is involved in the physiological development of some organ systems and can activate various cancers, such as non-small cell lung cancer, thyroid cancer, and papillary thyroid cancer. In the past few years, cancers with RET alterations have been treated with multikinase inhibitors (MKIs). However, because of off-target effects, these MKIs have developed drug resistance and some unacceptable adverse effects. Therefore, these MKIs are limited in their clinical application. Thus, the novel highly potent and RET-specific inhibitors selpercatinib and pralsetinib have been accelerated for approval by the Food and Drug Administration (FDA), and clinical trials of TPX-0046 and zetletinib are underway. It is well tolerated and a potential therapeutic for RET-altered cancers. Thus, we will focus on current state-of-the-art therapeutics with these novel RET inhibitors and show their efficacy and safety in therapy."

基金机构：Chongqing medical University (CQMU) Program for Youth Innovation in Future Medicine; [W0089]

基金资助正文："This work was supported by the Chongqing medical University (CQMU) Program for Youth Innovation in Future Medicine (W0089), owner by L.L."