塞尔帕替尼用于治疗局部晚期或转移性RET基因改变的实体瘤成年患者。
Selpercatinib for adult patients with locally advanced or metastatic RET-altered solid tumors.
作者信息
Le Dat, Konda Bhavana
机构信息
Department of Pharmacy, The Arthur G. James Cancer Hospital and Richard J. Solove Institute, The Ohio State University, Columbus, OH, USA.
Department of Internal Medicine, Division of Medical Oncology, Department of Internal Medicine, The Ohio State University Comprehensive Cancer Center, Columbus, OH, USA.
出版信息
Expert Rev Anticancer Ther. 2023 Jul-Dec;23(11):1117-1122. doi: 10.1080/14737140.2023.2267754. Epub 2023 Oct 27.
INTRODUCTION
The rearranged during transfection (RET) mutation is an oncogene driver for the development of cancer. Selpercatinib is a highly selective RET inhibitor that has demonstrated anti-tumor activity in RET-mutated cancers. Selpercatinib is approved for use in RET fusion-positive non-small-cell lung cancer (NSCLC), RET-mutated medullary thyroid cancer, RET fusion-positive thyroid cancer, and RET fusion-positive solid tumors.
AREAS COVERED
This review summarizes the pharmacology, efficacy, safety, and resistance mechanism of selpercatinib.
EXPERT OPINION
Selpercatinib has demonstrated durable responses with a favorable safety profile making it an excellent treatment option for RET-mutated cancers. Clinical trials are currently underway to determine the optimal sequencing of selpercatinib in RET fusion-positive lung and RET-mutated medullary thyroid cancer in the first-line setting compared to the current standard of care. Selpercatinib has shown promising anti-tumor activity in various RET-altered solid tumors opening a new treatment option for these patients.
引言
转染期间重排（RET）突变是癌症发展的致癌基因驱动因素。塞尔帕替尼是一种高度选择性的RET抑制剂，已在RET突变的癌症中显示出抗肿瘤活性。塞尔帕替尼被批准用于RET融合阳性非小细胞肺癌（NSCLC）、RET突变的甲状腺髓样癌、RET融合阳性甲状腺癌和RET融合阳性实体瘤。
涵盖领域
本综述总结了塞尔帕替尼的药理学、疗效、安全性和耐药机制。
专家观点
塞尔帕替尼已显示出持久的反应，安全性良好，使其成为RET突变癌症的优秀治疗选择。目前正在进行临床试验，以确定与当前标准治疗相比，塞尔帕替尼在一线治疗RET融合阳性肺癌和RET突变甲状腺髓样癌中的最佳用药顺序。塞尔帕替尼在各种RET改变的实体瘤中显示出有前景的抗肿瘤活性，为这些患者开辟了新的治疗选择。
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