本文關(guān)鍵詞： evolocumab 前蛋白轉(zhuǎn)化酶類 抗體 單克隆 PCSK抑制劑 調(diào)脂藥 膽固醇 LDL　出處：《中國(guó)新藥與臨床雜志》2017年04期 　論文類型：期刊論文

【摘要】：evolocumab是首個(gè)用于調(diào)節(jié)血脂的前蛋白轉(zhuǎn)化酶枯草溶菌素9(PCSK9)型抑制劑,用于治療原發(fā)性高膽固醇血癥和12歲及以上青少年和成年患者的純合子家族性高膽固醇血癥(Ho FH)。evolocumab通過與PCSK9特異性結(jié)合,從而減緩低密度脂蛋白受體的降解,顯著降低體內(nèi)低密度脂蛋白膽固醇(LDL-C)的水平。單獨(dú)用藥或聯(lián)合他汀類藥物可以使患者LDL-C水平降低55%~65%,特別適合于對(duì)他汀類不耐受以及高劑量他汀類(如阿托伐他汀、瑞舒伐他汀)調(diào)脂不達(dá)標(biāo)的患者,為調(diào)脂治療帶來(lái)了新的選擇。本文對(duì)其藥理作用,在治療和改善膽固醇高血脂的臨床試驗(yàn)和安全性研究等方面的研究進(jìn)展進(jìn)行綜述。
[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.
【作者單位】： 山東大學(xué)藥學(xué)院藥物化學(xué)研究所教育部天然產(chǎn)物化學(xué)生物學(xué)重點(diǎn)實(shí)驗(yàn)室;
【分類號(hào)】：R972.6
【正文快照】： evolocumab(AMG145)是美國(guó)Amgen公司研LDL-C在核內(nèi)體中被降解,LDLR則重新循環(huán)至細(xì)發(fā)的一種人源免疫球蛋白G2,屬于人源單克隆抗胞表面,繼續(xù)維持血漿中LDL-C的正常水平[7]。酶體,商品名:RepathaTM,分子式:C6242H9648N1668O1996S56,原PCSK9在內(nèi)質(zhì)網(wǎng)中經(jīng)過自我催化裂解轉(zhuǎn)變?yōu)槌上?!--http://www.cnki.com.cn/Article/CJFDTOTAL-XYYL201704003.htm-->，

本文編號(hào)：1476853