一种调血脂的新型单抗药物evolocumab

发布时间：2018-01-30 17:46

  本文关键词： evolocumab 前蛋白转化酶类 抗体 单克隆 PCSK抑制剂 调脂药 胆固醇 LDL　出处：《中国新药与临床杂志》2017年04期 　论文类型：期刊论文

【摘要】：evolocumab是首个用于调节血脂的前蛋白转化酶枯草溶菌素9(PCSK9)型抑制剂,用于治疗原发性高胆固醇血症和12岁及以上青少年和成年患者的纯合子家族性高胆固醇血症(Ho FH)。evolocumab通过与PCSK9特异性结合,从而减缓低密度脂蛋白受体的降解,显著降低体内低密度脂蛋白胆固醇(LDL-C)的水平。单独用药或联合他汀类药物可以使患者LDL-C水平降低55%~65%,特别适合于对他汀类不耐受以及高剂量他汀类(如阿托伐他汀、瑞舒伐他汀)调脂不达标的患者,为调脂治疗带来了新的选择。本文对其药理作用,在治疗和改善胆固醇高血脂的临床试验和安全性研究等方面的研究进展进行综述。
[Abstract]:Evolocumab is the first protein-converting enzyme lysogenin 9 (SKPC9) inhibitor for regulating blood lipids. Homozygous familial hypercholesterolemia for treatment of primary hypercholesterolemia and homozygous hypercholesterolemia in adolescents and adults aged 12 years and over. Evolocumab binds specifically to PCSK9. In order to slow down the degradation of low-density lipoprotein receptor. Low density lipoprotein cholesterol (LDL-C) levels were significantly reduced by 55% or 65% in patients treated alone or in combination with statins. It is especially suitable for patients with intolerance to statins and high doses of statins (such as Atto vastatin, resuvastatin), which brings a new choice for lipid regulation therapy. Advances in clinical trials and safety studies in the treatment and improvement of cholesterol hyperlipidemia are reviewed.
【作者单位】： 山东大学药学院药物化学研究所教育部天然产物化学生物学重点实验室;
【分类号】：R972.6
【正文快照】： evolocumab(AMG145)是美国Amgen公司研LDL-C在核内体中被降解,LDLR则重新循环至细发的一种人源免疫球蛋白G2,属于人源单克隆抗胞表面,继续维持血浆中LDL-C的正常水平[7]。酶体,商品名:RepathaTM,分子式:C6242H9648N1668O1996S56,原PCSK9在内质网中经过自我催化裂解转变为成相，

本文编号：1476853