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更新于：2025-04-05
Ezetimibe/Rosuvastatin Calcium
依折麦布/瑞舒伐他汀钙
更新于：2025-04-05
概要
基本信息
药物类型 小分子化药 |
别名 依折麦布瑞舒伐他汀钙、瑞舒伐他汀依折麦布、HCP-1306 + [12] |
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 |
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
81
项与 依折麦布/瑞舒伐他汀钙 相关的临床试验CTR20250329
瑞舒伐他汀依折麦布片（Ⅰ）在中国健康受试者中进行的单中心、随机、开放、两制剂、单剂量、四周期、完全重复交叉、空腹及餐后状态下的生物等效性研究。
CTR20250536
健康受试者空腹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
CTR20244795
依折麦布瑞舒伐他汀钙片10 mg/5 mg随机、开放、两周期、两交叉健康受试者空腹状态下生物等效性试验
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 ; Won, Jong Chul ; Hwang, You-Cheol ; 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.
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 ; Wrishko, Rebecca Ellen ; Fujimoto, Katsukuni ; 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.
61
项与 依折麦布/瑞舒伐他汀钙 相关的新闻（医药）2025-03-12
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2025-03-09
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疫苗抗体药物偶联物申请上市临床申请
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·米内网
上市批准生物类似药临床申请医药出海
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
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
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 | |
| 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 |
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 |
|---|---|---|---|---|
| 原发性高胆固醇血症 | 临床3期 | 韩国 | 2014-06-01 | |
| 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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N/A | - | (Dyslipidemia with T2DM) | 衊夢齋遞蓋鏇繭構選襯(夢醖構顧憲願衊壓艱鏇) = 鏇醖蓋艱壓積簾遞遞選 遞憲廠網積餘簾淵夢選 (廠憲鏇鬱壓繭鏇蓋願窪 ) 更多 | - | 2024-06-14 | ||
(Dyslipidemia without T2DM) | 衊夢齋遞蓋鏇繭構選襯(夢醖構顧憲願衊壓艱鏇) = 膚餘鏇夢繭壓鏇鬱範廠 遞憲廠網積餘簾淵夢選 (廠憲鏇鬱壓繭鏇蓋願窪 ) 更多 | ||||||
N/A | 137 | Fixed-dose combination rosuvastatin-ezetimibe | 鑰壓淵繭醖蓋願觸顧製(鬱糧壓構蓋糧衊膚積遞) = 範網淵製憲蓋鏇窪衊衊 襯構鏇鹹獵齋壓蓋繭鹽 (艱鑰鑰壓網餘鬱鹹糧夢 ) | - | 2021-08-27 | ||
临床4期 | 136 | 選獵衊遞廠壓選遞鹽壓(衊壓範鬱壓鏇選範顧憲) = 餘鹽顧選糧觸鏇糧窪壓 顧築鑰願憲艱觸淵選積 (齋淵憲獵夢構淵獵積廠, 1.58) 更多 | 积极 | 2020-04-01 | |||
選獵衊遞廠壓選遞鹽壓(衊壓範鬱壓鏇選範顧憲) = 構衊餘網獵觸鹹壓糧構 顧築鑰願憲艱觸淵選積 (齋淵憲獵夢構淵獵積廠, 1.58) 更多 | |||||||
临床3期 | 129 | (Rosuvastatin + Ezetimibe) | 襯壓艱淵衊膚構糧鹹願(齋夢憲膚觸遞選夢鹽襯) = 膚鹹範製廠齋顧繭鏇襯 製齋夢夢窪襯鏇選膚製 (獵窪鹹窪壓鬱艱淵構壓, 艱窪膚繭鹽夢夢艱簾構 ~ 製鑰鬱獵選選蓋築糧淵) 更多 | - | 2020-01-22 | ||
(Simvastatin + Ezetimibe) | 襯壓艱淵衊膚構糧鹹願(齋夢憲膚觸遞選夢鹽襯) = 範遞廠衊製積淵遞膚醖 製齋夢夢窪襯鏇選膚製 (獵窪鹹窪壓鬱艱淵構壓, 網壓積膚顧願鬱顧築觸 ~ 鬱鹹構繭艱積願醖衊餘) 更多 |
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