卡博替尼治疗 KIF5B-RET 融合的非小细胞肺癌。快速重新定位的一个例子。

Cabozantinib for the treatment of non-small cell lung cancer with KIF5B-RET fusion. An example of swift repositioning.

机构信息

New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), 80 Cheombok-ro, Dong-gu, Daegu, 701-310, Korea.

出版信息

Arch Pharm Res. 2015 Dec;38(12):2120-3. doi: 10.1007/s12272-015-0660-1. Epub 2015 Sep 16.

DOI:10.1007/s12272-015-0660-1

PMID:26377589

Abstract

A new chimeric fusion transcript of KIF5B (the kinesin family 5B gene) and the RET (Rearranged during Transcription) oncogene, KIF5B-RET, was found in 1-2% of lung adenocarcinomas (LADCs) in 2012. Several related clinical trials for non-small cell lung cancer (NSCLC) with KIF5B-RET rearrangements using existing RET inhibitors, such as cabozantinib, lenvatinib, vandetanib, sunitinib, ponatinib, and AUY922, have been swiftly initiated by the discovery of the KIF5B-RET fusion gene. Anti-RET activity and the status of clinical development of cabozantinib for KIF5B-RET fusion-positive NSCLC are discussed.

摘要

2012 年，发现 1%-2%的肺腺癌（LADCs）中存在 KIF5B（驱动蛋白家族 5B 基因）和 RET（转录过程中重排）癌基因的新型嵌合融合转录本 KIF5B-RET。发现 KIF5B-RET 融合基因后，迅速启动了几项针对 KIF5B-RET 重排的非小细胞肺癌（NSCLC）的相关临床试验，这些临床试验使用了现有的 RET 抑制剂，如卡博替尼、仑伐替尼、凡德他尼、舒尼替尼、波那替尼和 AUY922。本文讨论了卡博替尼对 KIF5B-RET 融合阳性 NSCLC 的抗 RET 活性和临床开发状况。