Song Minsoo
New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), 80 Cheombok-ro, Dong-gu, Daegu 701-310, South Korea.
Eur J Med Chem. 2017 Dec 15;142:383-392. doi: 10.1016/j.ejmech.2017.08.007. Epub 2017 Aug 9.
Renal cell carcinoma (RCC) is the most common type of kidney cancer in adults and is known to be the 10th most common type of cancer in the world. Most of the currently available RCC drugs are tyrosine kinase inhibitors (TKIs). However, combination therapies of TKIs and immune checkpoint inhibitors such as programmed cell death protein 1 (PD-1) and programmed cell death protein 1 ligand 1 (PD-L1) inhibitors are the focus of most of the final stage clinical trials. Meanwhile, other small molecule therapies for RCC that target indoleamine-2,3-dioxygenase (IDO1), glutaminase, C-X-C chemokine receptor 4 (CXCR4), and transglutaminase 2 (TG2) are emerging as the next generation of therapeutics. In this review, these three major streams for the development of small molecule drugs for RCC are described.
肾细胞癌（RCC）是成人中最常见的肾癌类型，也是全球第10大常见癌症类型。目前大多数可用的RCC药物是酪氨酸激酶抑制剂（TKIs）。然而，TKIs与免疫检查点抑制剂（如程序性细胞死亡蛋白1（PD-1）和程序性细胞死亡蛋白1配体1（PD-L1）抑制剂）的联合疗法是大多数晚期临床试验的重点。与此同时，其他针对吲哚胺-2,3-双加氧酶（IDO1）、谷氨酰胺酶、C-X-C趋化因子受体4（CXCR4）和转谷氨酰胺酶2（TG2）的RCC小分子疗法正在成为下一代治疗方法。在这篇综述中，描述了RCC小分子药物开发的这三大主要方向。
