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題 名 | 新一類降血脂藥PCSK9抑制劑=PCSK9 Inhibitors--New Classification Antihyperlipidemia Medication |
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作 者 | 莊峻毅; 林旭志; 吳求珍; | 書刊名 | 藥學雜誌 |
卷 期 | 32:1=126 2016.03[民105.03] |
頁 次 | 頁25-30 |
分類號 | 418.227 |
關鍵詞 | PCSK9抑制劑; 降血脂藥; 高膽固醇血症; Alirocumab; Evolocumab; |
語 文 | 中文(Chinese) |
中文摘要 | PCSK9 (Proprotein convertase subilisin/kexin type 9) 為體內肝臟生合成之蛋白質, 於體內膽固醇的平衡扮演重要角色,它會與肝細胞表面低密度脂蛋白接受器 LDL Receptor (low density lipoprotein receptor; LDL-R) 鍵結,並一起於肝細胞內分解,使 LDL-R 無法再回收到肝細胞表面重新作用,進而影響血漿中膽固醇之清除,造成循 環系統低密度脂蛋白膽固醇 (low density lipoprotein cholesterol; LDL-C) 濃度過高,升 高了心血管疾病之風險。因此,若藥品能抑制 PCSK9對於肝細胞之作用,理論上, 將可降低血液中膽固醇指數,降低心血管疾病之風險。 美國 FDA 於2015年7月及8月各核准一個單株抗體 monoclonal antibodies (mAbs) PCSK9抑制劑-alirocumab 及 evolocumab 作為高膽固醇血症以及家族性高膽固醇血症之 治療,對於使用其他類降血脂藥療效不佳或耐受性不良時的病人,這是另一個選擇。 |
英文摘要 | PCSK9 (Proprotein convertase subilisin kexin type 9) is a protein produced by liver biosynthesis. It plays a crucial role in cholesterol homeostasis. PCSK9 binding to the specific region of LDL-R to induce intracellular degradation and prevent LDL-R from reaching the hepatocyte surface and further reaction to affect the eliminating cholesterol from serum. It results in great increasing LDL-C of serum level and the risk of cardiovascular diseases (CVD). Theoretically, medication which can inhibit PCSK9 will reduce LDL-C level and CVD risk. 2015, July and August the U.S. Food and Drug Administration have respectively approved alirocumab and evolocumab which are monoclonal antibodies (mAbs) PCSK9 inhibitors firstly approved as new class of cholesterol-lowering agents for treating hyperchlesterolemia and familial hypercholesterolemia. These are alternate choice for patients who suffered from intolerance of other cholesterol-lowering agents. |
本系統中英文摘要資訊取自各篇刊載內容。