英文药名：Praluent(Alirocumab for Solution for Subcutaneous Injection) 中文药名：阿立单抗重组预充注射剂 生产厂家：赛诺菲有限公司 药品介绍 近日，赛诺菲（Sanofi）与再生元（Regeneron）合作开发的新一代降脂药PCSK9抑制剂获得日本卫生劳动福利部（MHLW）批准，用于低密度脂蛋白胆固醇（LDL-C）不受控的高胆固醇血症成人患者。该药适用人群为：接受他汀类药物治疗LDL-C控制不足的伴有心血管（CV）高风险的高胆固醇血症成人患者以及杂合子家族性高胆固醇血症（HeFH）成人患者。Praluent剂量规格包括75mg和150mg，在日本市场以单剂量预充式注射笔或注射器销售. プラルエント皮下注75mgペン／プラルエント皮下注150mgペン 药物分类名称 高胆固醇血症治疗剂/完全人抗PCSK 9抗体 批准日期：2016年9月 商標名 Praluent 一般名 アリロクマブ（遺伝子組換え） Alirocumab（Genetical Recombination） 本　質 Alilocumab是针对人前蛋白转化酶枯草杆菌蛋白酶/ kexin 9型（PCSK 9）的重组人IgG1单克隆抗体。 阿里卡单抗在中国仓鼠卵巢细胞中产生。 阿糖胞苷是由由448个氨基酸残基组成的2 H链（γ1链）和由220个氨基酸残基组成的2L链（κ链）组成的糖蛋白（分子量：约149,000）。 处理注意事项 对于遮光，本产品应存放在外箱中。 批准条件 制定药品风险管理计划，适当实施。 药效药理 1. 作用机序 阿里卡单抗以高亲和性和特异性结合前蛋白转化酶枯草杆菌蛋白酶/ 9型（KKK9），并通过抑制PCSK9与LDL受体（LDLR）的结合可以去除低密度脂蛋白胆固醇的LDLR数量， 结果，LDL胆固醇水平降低。 2. 与PCSK9的结合亲和力 在体外试验中，该试剂显示出在中性（pH 7.4）条件下（KD范围为0.52），以高亲和性结合来源于人，食蟹猴，大鼠，小鼠和仓鼠的遗传修饰的PCSK 9 〜14.5nmol/L）。 3. 血液LDL胆固醇降低作用 在体内试验中，当将该药物静脉内或皮下施用于食蟹猴时，血清LDL胆固醇和总胆固醇呈剂量依赖性降低，最高剂量为15mg/kg时，平均LDL胆固醇在基线时为最大值 约80％。 适应症 家族性高胆固醇血症，高胆固醇血症 然而，仅当发生心血管事件的风险高且HMG-CoA还原酶抑制剂的作用不足时，才受到限制。 用法与用量 成人；每两周一次皮下接受75mg。 如果效果不足，可以增加到150毫克。 包装规格 皮下注射 75毫克笔：75毫克/1毫升×1 150毫克笔：150毫克/1毫升×1 制造销售 赛诺菲有限公司 本品的完整说明书附件：http://www.info.pmda.go.jp/go/pack/2189402G3027_1_03/ New release of "Plalient®" for hypercholesterolemia treatment Sanofi Co., Ltd. (head office: Shinjuku-ku, Tokyo, President and CEO: Jack Naton, hereinafter "Sanofi") today announced that it has entered into an agreement for the treatment of hypercholesterolemia "Pralient® subcutaneous injection 75 mg pen, We announced that we released a subcutaneous injection 150 mg pen, subcutaneous injection 75 mg syringe, same subcutaneous injection 150 mg syringe "(generic name: alilocumab (genetical recombination), hereinafter" pralient ® ") Pralient ® is a fully human monoclonal antibody targeting PCSK 9 (proprotein convertase subtilisin / cystine type 9). Increasing the number of LDL receptors that eliminate low-density lipoprotein cholesterol (LDL cholesterol, so-called "bad" cholesterol) from the blood by binding Pralient ® to PCSK9 and inhibiting PCSK9 binding to LDL receptor, As a result, the LDL cholesterol level decreases. Pralient ® has a high risk of developing cardiovascular events, and has efficacy and effect as familial hypercholesterolemia, hypercholesterolemia, which is inadequate for HMG-CoA reductase inhibitor (statin). For ODYSSEY JAPAN trial i for Japanese, LDL-C change rate from baseline to after 24 weeks was -63% in the Pralient® group and 2% in the placebo group, and the Pralient® had significant LDL- C decrease (p <0.0001). The LDL-C value of the Pralient® group decreased from 141.1 mg / dL at baseline to 54.8 mg / dL after 4 weeks (initial examination time), and its effect was 52 (LDL-C value of the placebo group: baseline 141.9 mg / dL, after 52 weeks 143.6 mg / dL) was maintained up to the week (53.4 mg / dL). In addition, 138 of 143 patients in this study (ITT group) are maintained at 75 mg starting dose after 12 weeks, and it is also shown that 75 mg is the optimal dose for Japanese. This drug is provided with a pen and a syringe. In releasing this drug, Liar · Goodman, Japan General Manager, Diabetes and Cardiovascular Business Unit JPAC Region Head, says: "There are many high-risk patients who can not achieve LDL cholesterol management target despite existing lipid lowering therapy, and patients with familial hypercholesterolemia who are genetically high in serum LDL cholesterol level In this way, we are pleased to be able to provide new treatment options for lipid therapy to Japanese patients in the presence of unmet medical needs in lipid therapy. " that's all i: The ODYSSEY JAPAN study is aimed at Japanese patients with hypercholesterolemia who have familial hypercholesterolemia heterozygotes (heFH) or cardiovascular event risk who are not properly controlled by lipid lowering therapy including statins , Randomized, double-blind, placebo-controlled, parallel group, multi-center joint study to eva luate the efficacy and safety of Alilocumab. Pralient ® Product overview Sales name Pralient®subcutaneous injection 75 mg pen, Plalient ® subcutaneous injection 150 mg pen Pralient®subcutaneous injection 75 mg syringe, Plalient ® subcutaneous injection 150 mg syringe common name Alilocumab (Genetical recombination) Indication or effect Familial hypercholesterolemia, hypercholesterolemia However, it is limited only when the risk of developing cardiovascular events is high and the effect is insufficient with HMG-CoA reductase inhibitors. Dosage and dosage Usually, adults receive 75 mg of Alilocumab (genetical recombination) subcutaneously once every two weeks. If the effect is insufficient, it can be increased to 150 mg once.