Liu Hui-Hui, Li Sha, Li Jian-Jun
State Key Laboratory of Cardiovascular Disease, Heart Failure Center, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 167 BeiLiShi Road, XiCheng District, Beijing, 100037, China.
State Key Laboratory of Cardiovascular Disease, Cardiometabolic Center, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 167 BeiLiShi Road, XiCheng District, Beijing, 100037, China.
Drugs. 2025 May;85(5):627-642. doi: 10.1007/s40265-025-02167-z. Epub 2025 Apr 1.
Tafolecimab, a fully human monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9), represents a significant therapeutic advancement in the management of hypercholesterolemia and has been approved for use in the Chinese population. Elevated low-density lipoprotein cholesterol (LDL-C) is a major risk factor for atherosclerotic cardiovascular disease, and traditional treatments often fall short due to challenges such as statin intolerance. Clinical trials have demonstrated that tafolecimab can effectively reduce LDL-C levels, achieving reductions of over 60% in many patients. It also improves other lipid parameters, including lipoprotein(a) [Lp(a)], non-high-density lipoprotein cholesterol (non-HDL-C), and apolipoprotein B (ApoB). It has a favorable safety profile, primarily characterized by mild to moderate adverse events. The long-acting formulation of tafolecimab enables less frequent dosing, thereby promoting compliance. As cardiovascular diseases continue to escalate globally, tafolecimab holds promise not only for patients in China but also for broader international applications, representing a critical advancement in the evolving landscape of lipid-lowering therapies.
塔伏西单抗是一种靶向前蛋白转化酶枯草溶菌素/克新9型(PCSK9)的全人源单克隆抗体,在高胆固醇血症的治疗方面代表了一项重大的治疗进展,并且已获批在中国人群中使用。低密度脂蛋白胆固醇(LDL-C)升高是动脉粥样硬化性心血管疾病的主要危险因素,而传统治疗方法由于诸如他汀类药物不耐受等挑战往往效果不佳。临床试验表明,塔伏西单抗可有效降低LDL-C水平,许多患者的降幅超过60%。它还能改善其他血脂参数,包括脂蛋白(a) [Lp(a)]、非高密度脂蛋白胆固醇(非HDL-C)和载脂蛋白B(ApoB)。其安全性良好,主要表现为轻度至中度不良事件。塔伏西单抗的长效制剂可减少给药频率,从而提高依从性。随着全球心血管疾病持续增加,塔伏西单抗不仅对中国患者有前景,在更广泛的国际应用中也有前景,代表了降脂治疗不断发展的格局中的一项关键进展。