PD-1/PD-L1小分子抑制剂临床进展  

Clinical Progress of PD-1/PD-L1 Small Molecule Inhibitors

作　　者：杨帆[1] 刘敦恺 王悦[1] 文博杰 赖宜生[1] 

机构地区：[1]中国药科大学新药研究中心,多靶标天然药物全国重点实验室,江苏 南京

出　　处：《药物化学》2024年第2期77-86,共10页Hans Journal of Medicinal Chemistry

摘　　要：PD-1/PD-L1是维持机体稳态的免疫检查点共抑制分子,与肿瘤免疫逃逸密切相关。目前全球已有22款PD-1/PD-L1单抗获批用于治疗各类恶性肿瘤,然而小分子抑制剂的研发却进展缓慢。自2015年百时美施贵宝公司公开第一份联苯类化合物专利以来,至今已有15款PD-1/PD-L1小分子抑制剂进入临床开发。本文从简介PD-1/PD-L1的结构和信号通路出发,分析部分PD-1/PD-L1小分子抑制剂的临床前研究,侧重综述该类小分子抑制剂临床研究的进展。PD-1/PD-L1 is an immune checkpoint co-suppressor molecule that maintains homeostasis in the body and is closely related to tumor immune escape. At present, 22 types of PD-1/PD-L1 monoclonal antibody have been approved globally for the treatment of various therioma, while the development of small molecule inhibitors is progressing slowly. Since the disclosure of the first patent for biphenyl compounds by Bristol Myers Squibb Company in 2015, 15 types of PD-1/PD-L1 small molecule inhibitor have been developed in clinical trials to date. This article starts with an introduction to the structure and signaling pathways of PD-1/PD-L1, analyzes the preclinical studies of some small molecule inhibitors of PD-1/PD-L1, and focuses on reviewing the progress of clinical research on this type of small molecule inhibitor.

关 键 词：免疫检查点疗法 PD-1/PD-L1 小分子抑制剂 临床进展 

分 类 号：R73[医药卫生—肿瘤]