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更新于：2025-09-05
Ezetimibe/Rosuvastatin Calcium
依折麦布/瑞舒伐他汀钙
更新于：2025-09-05
概要
基本信息
药物类型 小分子化药 |
别名 Rosuvastatin Calcium/Ezetimibe、依折麦布瑞舒伐他汀钙、瑞舒伐他汀依折麦布 + [15] |
作用方式 抑制剂 |
作用机制 HMG-CoA reductase抑制剂(羟甲基戊二酰辅酶A合酶抑制剂)、NPC1L1抑制剂(尼曼-匹克C1型类似蛋白-1抑制剂)、胆固醇吸收抑制剂 |
在研适应症 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批日期 韩国 (2015-09-24), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C22H28CaFN3O6S |
InChIKeyAVDMILNVMOXCHF-DHMAKVBVSA-N |
CAS号147098-20-2 |
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关联
85
项与 依折麦布/瑞舒伐他汀钙 相关的临床试验CTR20252698
瑞舒伐他汀依折麦布片(Ⅰ)生物等效性试验
CTR20252300
瑞舒伐他汀依折麦布片（I）在中国健康人群中空腹和餐后状态下单次给药的人体生物等效性临床试验
CTR20251814
健康受试者餐后单次口服瑞舒伐他汀依折麦布片（I）的随机、开放、单剂量、两制剂、两序列、四周期、完全重复交叉设计的生物等效性试验
100 项与 依折麦布/瑞舒伐他汀钙 相关的临床结果
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100 项与 依折麦布/瑞舒伐他汀钙 相关的转化医学
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100 项与 依折麦布/瑞舒伐他汀钙 相关的专利（医药）
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7
项与 依折麦布/瑞舒伐他汀钙 相关的文献（医药）2022-01-01Journal of cardiovascular pharmacology and therapeutics
A Phase 3 Randomized Controlled Trial to Evaluate Efficacy and Safety of New-Formulation Zenon (Rosuvastatin/Ezetimibe Fixed-Dose Combination) in Primary Hypercholesterolemia Inadequately Controlled by Statins
Article
作者: Berthou, Baptiste ; Vrablik, Michal ; Baccara-Dinet, Marie ; Loy, Megan ; Catapano, Alberico L. ; Karpov, Yuri
Objective::
In primary hypercholesterolemia many people treated with statins do not reach their plasma LDL-C goals and are at increased risk of cardiovascular disease (CVD). This study aimed to evaluate efficacy and safety of a new fixed-dose combination (FDC) formulation of rosuvastatin/ezetimibe (R/E) in this population.
Methods::
This was a multicenter, multinational, randomized, double-blind, double-dummy, active-controlled, parallel-arm study of FDC R/E in people with primary hypercholesterolemia at very high risk (VHR) or high risk (HR) of CVD, inadequately controlled with 20 mg or 10 mg stable daily dose of rosuvastatin or equipotent dose of another statin. The primary objective was to demonstrate superiority of FDC R/E versus rosuvastatin monotherapy uptitrated to 40 mg (R40) or 20 mg (R20) in reduction of LDL-C after 6 weeks.
Results::
Randomized VHR participants (n = 244) were treated with R40, R40/E10, or R20/E10; randomized HR participants (n = 208) received R10/E10 or R20. In VHR participants, superiority of R40/E10 and R20/E10 versus R40 was demonstrated on LDL-C percent change from baseline to Week 6 with least squares mean differences (LSMD) of −19.66% (95% CI: −29.48% to −9.84%; P < .001) and −12.28% (95% CI: −22.12% to −2.44%; P = .015), respectively. In HR participants, superiority of R10/E10 over R20 was not demonstrated (LSMD −5.20%; 95% CI: −15.18% to 4.78%; P = .306), despite clinically relevant LDL-C reduction with R10/E10. No unexpected safety findings were reported.
Conclusions::
The results from this study suggest that R/E FDCs improve LDL-C reduction and goal achievement in people with primary hypercholesterolemia inadequately controlled with statins and at VHR/HR of CVD.
2020-04-01Diabetes therapy : research, treatment and education of diabetes and related disorders
Comparison of the Efficacy and Safety of Rosuvastatin/Ezetimibe Combination Therapy and Rosuvastatin Monotherapy on Lipoprotein in Patients With Type 2 Diabetes: Multicenter Randomized Controlled Study
Article
作者: Lee, Woo Je ; Lee, Jiwoo ; Park, Joong-Yeol ; Hwang, You-Cheol ; Ahn, Kyu Jeung ; Won, Jong Chul ; Song, Kee-Ho ; Park, Cheol-Young
INTRODUCTION:
Ezetimibe/statin combination therapy has been reported to provide additional cardioprotective effects compared to statin monotherapy. The apolipoprotein B/A1 (apoB/A1) ratio is an effective predictor of cardiovascular diseases. The aim of this study was to compare the efficacy and safety of rosuvastatin/ezetimibe combination therapy versus rosuvastatin monotherapy using the apoB/A1 ratio in patients with diabetes and hypercholesterolemia.
METHODS:
In this randomized, multicenter, open-label, parallel-group study, patients were randomly assigned to receive the combination therapy of rosuvastatin 5 mg/ezetimibe 10 mg once daily (n = 68) or monotherapy with rosuvastatin 10 mg once daily (n = 68), for 8 weeks.
RESULTS:
After the 8-week treatment, percentage change (least-square means ± standard error) in the apoB/A1 ratio in the rosuvastatin/ezetimibe group was significantly decreased compared to the rosuvastatin group (- 46.14 ± 1.58% vs. - 41.30 ± 1.58%, respectively; P = 0.03). In addition, the proportion of patients achieving > 50% reduction in low-density lipoprotein-cholesterol (LDL-C) and in the comprehensive lipid target (LDL-C < 70 mg/dL, non-HDL-cholesterol [non-HDL-C] < 100 mg/dL, and apoB < 80 mg/dL) was significantly different between the two groups (76.5 and 73.5% in the rosuvastatin/ezetimibe group and 47.1 and 45.6% in the rosuvastatin group, respectively; P < 0.001). The reduction in total cholesterol, non-HDL-C, LDL-C, and apoB were greater in the rosuvastatin/ezetimibe group than in the rosuvastatin group. Both treatments were well tolerated, and no between-group differences in drug-related adverse events were observed.
CONCLUSION:
The apoB/A1 ratio was significantly reduced in patients receiving combination therapy with ezetimibe and rosuvastatin compared to those receiving rosuvastatin monotherapy. Both treatments were well tolerated in patients with type 2 diabetes and hypercholesterolemia.
TRIAL REGISTRATION:
NCT03446261.
2019-11-01Clinical and translational science3区 · 医学
The Bioequivalence and Effect of Food on the Pharmacokinetics of a Fixed‐Dose Combination Tablet Containing Rosuvastatin and Ezetimibe in Healthy Japanese Subjects
3区 · 医学
ArticleOA
作者: Behm, Martin Otto ; Nishida, Chisato ; Matsumoto, Yuki ; Fujimoto, Katsukuni ; Wrishko, Rebecca Ellen ; Shirakawa, Masayoshi ; Furihata, Kenichi
Certain patient populations are unable to achieve the recommended low‐density lipoprotein cholesterol goals with statin monotherapy alone. Such patients may benefit from concomitant therapy with ezetimibe (EZE) 10 mg added on to a statin. To this end, fixed‐dose combination (FDC) tablets containing EZE 10 mg and rosuvastatin (ROS) 2.5 mg (EZE/ROS2.5) and EZE 10 mg and ROS 5 mg (EZE/ROS5) have been developed for treatment of hypercholesterolemia. The purpose of the series of clinical studies reported herein was to evaluate the potential food effect (MK‐0653H, protocol 836 (P836)) and the bioequivalence between FDC and co‐administration of EZE and ROS in healthy Japanese subjects under fasted and fed conditions (MK‐0653H, protocol 835 (P835) and MK‐0653H, protocol 846 (P846), respectively). These studies show there is no clinically relevant food effect on EZE exposure following single oral administration of the FDC EZE/ROS5 in healthy Japanese subjects; however, ROS exposure was decreased in the fed state under conditions used to evaluate the maximum food effect. Following single oral administration of individual ROS tablets under the same conditions, the magnitude of decrease in ROS exposure was comparable to that seen with FDC, suggesting that the effect of food on ROS exposure was similar between the FDC tablet and co‐administration of individual EZE and ROS tablets. The FDC EZE/ROS5 was generally well tolerated in healthy Japanese subjects under fasted and fed conditions.
100 项与 依折麦布/瑞舒伐他汀钙 相关的药物交易
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外链
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 纯合子家族性高胆固醇血症 | 美国 | 2021-03-23 | |
| 高脂血症 | 美国 | 2021-03-23 | |
| 杂合子家族性高胆固醇血症 | 巴西 | 2019-12-30 | |
| 高甘油三酯血症 | 巴西 | 2019-12-30 | |
| 高胆固醇血症 | 日本 | 2019-03-26 | |
| 高胆固醇血症 | 日本 | 2019-03-26 | |
| II型高脂蛋白血症 | 日本 | 2019-03-26 | |
| 原发性高胆固醇血症 | 韩国 | 2015-09-24 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 2型糖尿病 | 临床1期 | 韩国 | 2024-06-20 | |
| 血脂障碍 | 临床1期 | 韩国 | 2024-06-20 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 136 | 積願衊餘襯選艱襯簾淵(築淵築鬱繭簾鹽糧築鑰) = 繭淵窪積膚淵繭鹹範觸 構襯鏇鏇鑰壓齋淵顧積 (範積鑰憲網遞積鹽願鑰, 1.58) 更多 | 积极 | 2020-04-01 | |||
積願衊餘襯選艱襯簾淵(築淵築鬱繭簾鹽糧築鑰) = 廠壓網糧選醖獵衊選壓 構襯鏇鏇鑰壓齋淵顧積 (範積鑰憲網遞積鹽願鑰, 1.58) 更多 | |||||||
临床3期 | 129 | (Rosuvastatin + Ezetimibe) | 衊鏇選糧憲淵鹽醖製壓(選壓網淵製艱襯鹽襯觸) = 憲鏇築鬱醖獵鬱獵簾蓋 壓鹽獵鹽鬱獵淵築壓醖 (遞艱膚醖衊襯窪窪構艱, 遞齋衊衊憲遞積積構顧 ~ 壓範廠觸範顧願憲願簾) 更多 | - | 2020-01-22 | ||
(Simvastatin + Ezetimibe) | 衊鏇選糧憲淵鹽醖製壓(選壓網淵製艱襯鹽襯觸) = 網蓋鹽衊淵壓淵繭襯鹹 壓鹽獵鹽鬱獵淵築壓醖 (遞艱膚醖衊襯窪窪構艱, 積膚夢艱鏇範衊繭繭網 ~ 範獵廠築顧糧艱齋窪廠) 更多 |
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