摘要
目的为新型程序性死亡受体-1(PD-1)/程序性死亡配体-1(PD-L1)小分子抑制剂的研发提供参考。方法检索PubMed、Embase、Web of Science、ClinicalTrails.gov、中国知网、万方数据库2010年至2023年的PD-1/PD-L1小分子抑制剂相关文献,汇总并分析该类制剂的研发现状。结果与结论有成药潜力的PD-1/PD-L1小分子抑制剂共20种,包括CA-170(口服小分子抑制剂)、INCB086550(特异性PD-L1抑制剂)、DPPA-1(特异性抑制PD-1/PD-L1相互作用的多肽类拮抗剂)等,其中前两者已进入临床试验阶段。PD-1/PD-L1小分子抑制剂具有特异性抑制免疫检查点的药效作用特点,以及可口服、稳定性较好、膜通透性较高等优点,但其治疗效果仍需临床试验验证。
Objective To provide a reference for the research and development(R&D)of novel small molecule inhibitors of programmed death-1(PD-1)/programmed death-ligand 1(PD-L1).Methods The studies related to small molecule inhibitors of PD-1/PD-L1 in the PubMed,Embase,Web of Science,ClinicalTrails.gov,CNKI and WanFang databases from 2010 to 2023 were searched to summarize and analyze the R&D status of these inhibitors.Results and Conclusion There are 20 small molecule inhibitors of PD-1/PD-L1 with the potential to develop into drugs,including CA-170(oral small molecule inhibitor),INCB086550(specific PD-L1 inhibitor),DPPA-1(peptide antagonists specifically inhibiting the interaction of PD-1/PD-L1)and so on.The first two are already in clinical trial stage.The small molecule inhibitors of PD-1/PD-L1 can specifically inhibit immune checkpoints,and they can be taken orally,have good stability and high membrane permeability,but their therapeutic effects still need to be verified through clinical trials.
作者
张大猛
陈美宇
徐静
杜沛龙
朱馨婷
韩冷
郭澄
杨全军
ZHANG Dameng;CHEN Meiyu;XU Jing;DU Peilong;ZHU Xinting;HAN Leng;GUO Cheng;YANG Quanjun(The Sixth People's Hospital Affiliated to Shanghai Jiao Tong University School of Medicine,Shanghai,China 200233;Shanghai University of Medicine&Health Sciences,Shanghai,China 201318)
出处
《中国药业》
CAS
2024年第12期1-6,共6页
China Pharmaceuticals
基金
国家自然科学基金[82272925]
上海市浦江人才计划项目[21PJ1411900]
上海市第六人民医院院级管理类科研基金[沪六院内科字〔2023〕第1号]
上海市第六人民医院医疗服务能级提升工程医政管理优化项目[20220201]。
