Evolocumab mechanism to reduce LDL cholesterol
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Evolocumab (Repatha) is an injectable monoclonal antibody that reduces LDL cholesterol levels. A limited quantity of LDL cholesterol is extracted from circulative blood when PCSK9-bound LDLR is degraded upon internalization in liver cells. Evolocumab competitively binds PCSK9 away from LDLR complexes, which allows LDLR to be recycled, returning to the surface and clearing additional molecules of LDL cholesterol.
依伏洛单抗(瑞派塔)是一种可注射的单克隆抗体,用于降低低密度脂蛋白胆固醇水平。在肝脏细胞内吞作用过程中,当PCSK9结合的低密度脂蛋白受体(LDLR)被降解时,从循环血液中提取出一定量的低密度脂蛋白胆固醇。依伏洛单抗通过与PCSK9竞争性结合,将PCSK9从LDLR复合物中移开,从而使LDLR得以循环利用,返回细胞表面,清除额外的低密度脂蛋白胆固醇分子。
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