Su Jingjing, Fu Yiting, Cui Zitong, Abidin Zain, Yuan Jingsong, Zhang Xinmiao, Li Runmin, Zhao Chunzhen
Key Laboratory of Molecular Pharmacology and Translational Medicine and Department of Pharmacology, College of Pharmacy, Weifang Medical University, Weifang, China.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States.
Front Pharmacol. 2024 Jan 10;14:1349081. doi: 10.3389/fphar.2023.1349081. eCollection 2023.
Relatlimab is a type of human immunoglobulin G4 monoclonal blocking antibody. It is the world's first Lymphocyte-Activation Gene-3 (LAG-3) inhibitor and the third immune checkpoint inhibitor with clinical application, following PD-1 and CTLA-4. Relatlimab can bind to the LAG-3 receptor which blocks the interaction between LAG-3 and its ligand to reduce LAG-3 pathway-mediated immunosuppression and promote T-cell proliferation, inducing tumor cell death. On 18 March 2022, the U.S. FDA approved the fixed-dose combination of relatlimab developed by Bristol Myers Squibb with nivolumab, under the brand name Opdualag for the treatment of unresectable or metastatic melanoma in adult and pediatric patients aged 12 and older. This study comprehensively describes the mechanism of action and clinical trials of relatlimab and a brief overview of immune checkpoint drugs currently used for the treatment of melanoma.
瑞帕利单抗是一种人免疫球蛋白G4单克隆阻断抗体。它是全球首个淋巴细胞激活基因-3(LAG-3)抑制剂,也是继PD-1和CTLA-4之后第三个有临床应用的免疫检查点抑制剂。瑞帕利单抗可与LAG-3受体结合,阻断LAG-3与其配体之间的相互作用,以减少LAG-3通路介导的免疫抑制并促进T细胞增殖,从而诱导肿瘤细胞死亡。2022年3月18日,美国食品药品监督管理局(FDA)批准了百时美施贵宝公司研发的瑞帕利单抗与纳武利尤单抗的固定剂量组合,商品名为Opdualag,用于治疗12岁及以上成人和儿童不可切除或转移性黑色素瘤。本研究全面描述了瑞帕利单抗的作用机制和临床试验,并简要概述了目前用于治疗黑色素瘤的免疫检查点药物。