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更新于：2026-09-07
Ezetimibe/Rosuvastatin Calcium
依折麦布/瑞舒伐他汀钙
更新于：2026-09-07
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 + [18] |
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C44H56CaF2N6O12S2 |
InChIKeyGGPPBULYISSAKA-BGRFNVSISA-N |
CAS号147098-20-2 |
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关联
103
项与 依折麦布/瑞舒伐他汀钙 相关的临床试验CTR20260226
一项随机、开放、四周期、完全重复交叉、餐后状态下给药临床试验，评价瑞舒伐他汀依折麦布片(I)与旨立达在中国健康成年参与者中的生物等效性
CTR20261724
瑞舒伐他汀依折麦布片（10 mg/10 mg）在健康受试者中空腹及餐后状态下单次给药的生物等效性试验（预试验）
CTR20261592
瑞舒伐他汀依折麦布片（I）生物等效性研究
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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8
项与 依折麦布/瑞舒伐他汀钙 相关的文献（医药）2025-11-01BMJ Open
High-Intensity Statin versus Upfront Equivalent-Dose Combination of Moderate-Intensity Statin with Ezetimibe Following Acute Myocardial Infarction (ROSUZET-AMI): protocol of a multicentre, open-label, randomised non-inferiority trial
Article
作者: Lee, Kwan Yong ; Woo, Seong-Ill ; Park, Hun Sik ; Kim, Dong-Bin ; Kwon, O Sung ; Kim, Chan Joon ; Park, Mahn-Won ; Choi, Ik Jun ; Kim, Hee-Yeol ; Lee, Sunam ; Chang, Kiyuk ; Hwang, Byung-Hee ; Oh, Gyu Chul ; Kang, Tae Soo ; Sung, Joong Kyung ; Choo, Eun Ho ; Lim, Sungmin ; Yun, Kyeong Ho ; Lee, Han Cheol ; Choi, Yunseok ; Park, Chul-Soo
Introduction:
High-intensity statin therapy is recommended as a first-line strategy for lowering low-density lipoprotein cholesterol (LDL-C) levels in patients with acute myocardial infarction (AMI). A combination of moderate-intensity statin and ezetimibe at an equivalent dose to high-intensity statin may achieve similar LDL-C reduction with fewer side effects. This study evaluates the long-term efficacy and safety of this approach, initiated following AMI, compared with high-intensity statin monotherapy.
Methods and analysis:
The ROSUZET-AMI trial is a multicentre, prospective, open-label, randomised, non-inferiority trial. Patients with AMI who underwent percutaneous coronary intervention were randomised 1:1 to receive either moderate-intensity statin with ezetimibe (rosuvastatin 5 mg with ezetimibe 10 mg) or high-intensity statin monotherapy (rosuvastatin 20 mg). The primary endpoint is the composite of cardiovascular death, major coronary events (non-fatal myocardial infarction, documented unstable angina requiring hospitalisation and all coronary revascularisation events occurring at least 30 days after randomisation), or non-fatal stroke.
Ethics and dissemination:
Ethics approval for this study was obtained from the Institutional Review Board of Seoul St. Mary’s Hospital (No. 2020-0424-0003). Informed consent is obtained from every participant before randomisation. The results of this study will be submitted for publication in international peer-reviewed journals, and the key findings will be presented at international scientific conferences.
Trial registration number:
NCT04499859
.
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 ; Karpov, Yuri ; Catapano, Alberico L.
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 ; Won, Jong Chul ; Ahn, Kyu Jeung ; 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.
100 项与 依折麦布/瑞舒伐他汀钙 相关的药物交易
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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 | |
| 家族性高胆固醇血症 | 日本 | 2019-03-26 | |
| 原发性高胆固醇血症 | 韩国 | 2015-09-24 |
未上市
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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 | 製築鑰觸壓簾鏇糧衊觸(願鏇鏇網襯製襯蓋鹽齋) = 襯範鹹構鬱鬱蓋壓簾鏇 製齋鹽簾襯艱蓋衊積襯 (衊餘膚蓋廠選鹽鬱蓋鑰, 1.58) 更多 | 积极 | 2020-04-01 | |||
製築鑰觸壓簾鏇糧衊觸(願鏇鏇網襯製襯蓋鹽齋) = 餘觸願淵簾淵構齋獵鏇 製齋鹽簾襯艱蓋衊積襯 (衊餘膚蓋廠選鹽鬱蓋鑰, 1.58) 更多 | |||||||
临床3期 | 129 | (Rosuvastatin + Ezetimibe) | 醖築遞餘選艱廠積齋糧(選艱構壓壓構膚製膚憲) = 願壓觸鑰憲襯鏇構製網 築壓憲艱鹽餘鹹範糧顧 (蓋繭襯繭顧膚製膚鏇廠, 齋夢齋顧顧鏇齋製鹽窪 ~ 蓋鹹夢鏇顧遞製簾壓積) 更多 | - | 2020-01-22 | ||
(Simvastatin + Ezetimibe) | 醖築遞餘選艱廠積齋糧(選艱構壓壓構膚製膚憲) = 夢糧膚鑰壓廠糧襯壓襯 築壓憲艱鹽餘鹹範糧顧 (蓋繭襯繭顧膚製膚鏇廠, 壓願構窪築鏇製簾選鹽 ~ 鏇衊築淵蓋鹽齋簾獵製) 更多 |
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