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更新于：2026-09-24
Hyzetimibe
海博麦布
更新于：2026-09-24
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2021-06-25), |
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C25H21F2NO3 |
InChIKeyHEHHPZYUXSFAPV-GLGQCLCGSA-N |
CAS号1266548-75-7 |
关联
25
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100 项与 海博麦布 相关的临床结果
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100 项与 海博麦布 相关的转化医学
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100 项与 海博麦布 相关的专利（医药）
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4
项与 海博麦布 相关的文献（医药）2023-11-01European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Physiologically based pharmacokinetic modeling to characterize enterohepatic recirculation and predict food effect on the pharmacokinetics of hyzetimibe
Article
作者: Jiang, Bo ; Chen, Wenjun ; Shao, Rong ; Lou, Honggang ; Ruan, Zourong ; Chen, Jinliang ; Yang, Dandan
BACKGROUND AND OBJECTIVE:
Hyzetimibe is a cholesterol absorption inhibitor indicated for the treatment of hypercholesterolemia. This study aims to describe the multiple-peak pharmacokinetics (PK) of hyzetimibe and its active metabolite M1 through physiologically-based pharmacokinetic (PBPK) modeling, and to compare the model predictions of a virtual food effect study with the results of a clinical food effect study.
METHODS:
The plasma concentration data used for PBPK modeling were obtained from a single-dose, two-period crossover bioequivalence study in the fasted state. Advanced Compartmental Absorption and Transit model was used for absorption. Enterohepatic recirculation process was modeled by changing the gut physiological state from fasted to fed at meal time. Based on the established PBPK models, a virtual food effect study was simulated. A clinical food effect study was used for model external validation.
RESULTS:
PK profiles of hyzetimibe and M1 under fasting condition could be well described by the PBPK model, and the errors of Cmax, AUC0-∞, and AUC0-t were within the two-fold range. Simulated geometric mean ratios (GMRs, fed/fasted) showed that a high-fat breakfast slightly affected the PK of hyzetimibe, expressed as increased Cmax of hyzetimibe (130.6%). Simulated GMRs and 90% confidence intervals of AUC were within the preset bioequivalent range. The results of the simulated virtual food effect trial were consistent with those of the clinical food effect trial.
CONCLUSIONS:
The established PBPK model could describe the concentration-time profiles of hyzetimibe and M1 well with good prediction performance. A fully mechanistic model of enterohepatic recirculation warrants further investigation.
2015-08-01Bioanalysis4区 · 医学
Simultaneous Determination of Hyzetimibe and its Main Active Metabolite in Plasma by LC–MS/MS and its Application in PK Study
4区 · 医学
Article
作者: Shao, Rong ; Lou, Honggang ; Chen, Jinliang ; Jiang, Bo ; Wang, Jian’an ; Ruan, Zourong
BACKGROUND:
Hyzetimibe is a new compound belonging to a novel class of selective cholesterol absorption inhibitors. A simple, highly sensitive LC-MS/MS method has been developed for the quantification of hyzetimibe and its main active metabolite, hyzetimibe-glucuronide, in human plasma.
RESULTS:
Analytical samples were prepared using a protein precipitation method coupled with a concentration process. The linearity of this method was established for concentrations in the ranges of 0.05-50 and 0.5-500 ng/ml for hyzetimibe and hyzetimibe-glucuronide, respectively. The accuracy and precision of the method varied from 97.9 to 105% and 2.6 to 7.4%, respectively.
CONCLUSION:
This study represents the first reported example of an LC-MS/MS assay for the simultaneous quantification of hyzetimibe and its main active metabolite, hyzetimibe-glucuronide, in human plasma. Furthermore, this method has been successfully applied to a PK study.
2014-10-01Journal of clinical pharmacology3区 · 医学
Pharmacokinetics, pharmacodynamics, safety, and tolerability of hyzetimibe (HS-25) in healthy Chinese subjects
3区 · 医学
Article
作者: Wang, Jian'an ; Zhang, Xuehua ; Shao, Qingxiang ; Xiang, Meixiang ; Chen, Jinliang ; Ruan, Zhourong ; Lou, Honggang ; jiang, Bo
Hyzetimibe (HS-25) is a new cholesterol absorption inhibitor. We performed the first-in-human study to assess the safety, tolerability, and pharmacokinetics (including the effect of food) and pharmacodynamics (effect on blood lipid level) following single (1, 3, 5, 10, 20, and 30 mg) and multiple (5, 10, and 20 mg) ascending-dose of hyzetimibe in healthy subjects. An increase of exposure (area under the plasma concentration-time curve and maximum plasma concentration) to hyzetimibe and hyzetimibe-glucuronide (HS-25M1) was observed in an approximately dose-proportional manner. A terminal half-life of approximately 21 hours was observed with doses ranging between 5 and 30 mg. Steady state was achieved by day 8 of once-daily dosing with 1.6- and 1.2-fold accumulation for hyzetimibe and hyzetimibe-glucuronide, respectively. Food did not have any effect on hyzetimibe and hyzetimibe-glucuronide exposure. Administration of hyzetimibe once daily for 10 days reduced the levels of low-density lipoprotein cholesterol levels in healthy subjects and these recovered after discontinuation of this drug. All of the adverse events were mild or moderate in severity, and the majority of them were unrelated to hyzetimibe, with no dose-dependent trends. These findings suggest that hyzetimibe could be a potential treatment for hypercholesterolemia.
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 原发性高胆固醇血症 | 中国 | 2021-06-25 |
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 动脉粥样硬化 | 临床3期 | 中国 | 2016-06-07 | |
| 冠状动脉疾病 | 临床3期 | - | 2016-06-07 |
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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3期 | 255 | 襯艱齋繭願鹽艱願願觸(鹽遞醖築顧艱淵製夢遞) = 觸窪餘鹽築襯衊積鑰鹽 艱淵範窪範糧憲繭衊夢 (鹽鏇鬱選鹹鑰蓋夢積構 ) 更多 | 优效 | 2018-09-12 | |||
Atorvastatin strontium+Atorvastatin strontium | 襯艱齋繭願鹽艱願願觸(鹽遞醖築顧艱淵製夢遞) = 膚壓選衊淵鏇蓋壓網淵 艱淵範窪範糧憲繭衊夢 (鹽鏇鬱選鹹鑰蓋夢積構 ) 更多 | ||||||
临床3期 | 374 | 鏇繭餘蓋選繭淵齋艱遞(獵積積膚選蓋製艱醖簾) = 衊齋淵簾構觸壓鹹憲齋 獵鏇廠觸鏇餘鹹餘衊餘 (網製壓獵窪膚積遞鹽糧 ) | 积极 | 2018-09-12 | |||
Placebo | - |
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