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更新于：2025-11-06
Ezetimibe/Rosuvastatin Calcium
依折麦布/瑞舒伐他汀钙
更新于：2025-11-06
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 |
查看全部结构式(2)
关联
88
项与 依折麦布/瑞舒伐他汀钙 相关的临床试验CTR20253921
瑞舒伐他汀依折麦布片（I）在中国成年健康参与者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、四周期、完全重复交叉生物等效性试验
CTR20252698
瑞舒伐他汀依折麦布片(Ⅰ)生物等效性试验
CTR20252457
瑞舒伐他汀依折麦布片（I）在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、四周期、完全重复交叉生物等效性研究
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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5
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 ; 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 ; 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.
2017-12-21International journal of clinical pharmacology and therapeutics4区 · 医学
Pharmacokinetics and bioequivalence of a rosuvastatin/ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects
4区 · 医学
Article
作者: Kim, Hyun-Ju ; Na, Sookie ; Kim, Bo Kyung ; Ohk, Boram ; Yoon, Young-Ran ; Kang, Woo Youl ; Lee, Hae Won ; Seong, Sook Jin ; Gwon, Mi-Ri
OBJECTIVE:
The pharmacokinetic profiles and bioequivalence of a new rosuvastatin/ezetimibe fixed-dose combination (FDC; NVP-1205) vs. rosuvastatin and ezetimibe concomitantly administered as single agents were evaluated.
MATERIALS AND METHODS:
In this open-label, single-dose, crossover study (NCT02029625), eligible subjects were randomly assigned in a 1 : 1 ratio to receive a single dose of rosuvastatin (10 mg) with ezetimibe (10 mg) as either a FDC or as single agents concomitantly administered under fasted conditions, followed by a 2-week washout period and administration of the alternate formulation. Serial blood samples were collected predose and up to 96 hours postdose in each period for determination of plasma rosuvastatin and ezetimibe concentrations by liquid-chromatography tandem mass spectroscopy and calculation of pharmacokinetic parameters.
RESULTS:
The mean Cmax and AUC0-t values of rosuvastatin were 12.5 ng/mL and 115.6 ng×h/mL for the FDC, and 12.2 ng/mL and 115.1 ng×h/mL for the single agents concomitantly administered, respectively. The mean Cmax and AUC0-t values of ezetimibe were 4.7 ng/mL and 67.3 ng×h/mL for the FDC, and 4.5 ng/mL and 68.2 ng×h/mL for the single agents concomitantly administered, respectively. The geometric mean ratio (GMR) and 90% confidence interval (CI) for the rosuvastatin Cmax and AUC0-t were 106.20 (96.62 - 116.74) and 102.88 (96.32 - 109.90), respectively. The GMR and 90% CI for the ezetimibe Cmax and AUC0-t were 108.96 (98.56 - 120.51) and 98.13 (92.01 - 104.66), respectively. All treatments were well tolerated during this study, with no serious adverse events reported.
CONCLUSION:
The rosuvastatin/ezetimibe (10/10 mg) FDC was bioequivalent to single agents concomitantly administered. A single dose of rosuvastatin/ezetimibe as the FDC or as single agents was well tolerated.
.
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 | |
| 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
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 | 膚餘製鏇獵窪網衊齋網(鹹築鏇製糧艱簾蓋構願) = 構淵淵鑰衊網顧膚壓觸 構觸鬱遞鹽構鬱鏇醖夢 (齋壓衊鹹襯製廠蓋鏇鏇, 1.58) 更多 | 积极 | 2020-04-01 | |||
膚餘製鏇獵窪網衊齋網(鹹築鏇製糧艱簾蓋構願) = 衊鑰鹹廠構選積壓製廠 構觸鬱遞鹽構鬱鏇醖夢 (齋壓衊鹹襯製廠蓋鏇鏇, 1.58) 更多 | |||||||
临床3期 | 129 | (Rosuvastatin + Ezetimibe) | 鑰鑰艱構鑰觸範製願齋(衊鑰憲網蓋淵壓鬱壓蓋) = 積觸鬱簾鬱淵顧鹽憲鬱 糧選繭窪醖鹹構鹹製鹹 (鑰繭繭衊膚網積膚繭蓋, 壓簾糧醖壓壓淵窪餘簾 ~ 鹽鹹蓋製齋繭壓蓋醖襯) 更多 | - | 2020-01-22 | ||
(Simvastatin + Ezetimibe) | 鑰鑰艱構鑰觸範製願齋(衊鑰憲網蓋淵壓鬱壓蓋) = 遞衊膚觸鏇醖鹽廠夢願 糧選繭窪醖鹹構鹹製鹹 (鑰繭繭衊膚網積膚繭蓋, 鏇積淵鹹鏇窪蓋積積壓 ~ 廠鑰淵簾獵繭鑰壓鑰築) 更多 |
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