预约演示
更新于：2026-07-30
Hyzetimibe
海博麦布
更新于：2026-07-30
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- |
登录后查看时间轴
结构/序列
分子式C25H21F2NO3 |
InChIKeyHEHHPZYUXSFAPV-GLGQCLCGSA-N |
CAS号1266548-75-7 |
关联
23
项与 海博麦布 相关的临床试验CTR20232183
评估海博麦布片在肾功能不全和健康受试者中的多中心、非随机、开放、平行对照的药代动力学研究
CTR20232181
评估海博麦布片在肝功能不全和健康受试者中的多中心、非随机、开放、平行对照的药代动力学研究
CTR20231842
海博麦布片和华法林钠片在健康受试者中的药物相互作用研究
100 项与 海博麦布 相关的临床结果
登录后查看更多信息
100 项与 海博麦布 相关的转化医学
登录后查看更多信息
100 项与 海博麦布 相关的专利（医药）
登录后查看更多信息
5
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 ; Yang, Dandan ; Chen, Jinliang
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: Zhang, Xuehua ; Wang, Jian'an ; 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.
100 项与 海博麦布 相关的药物交易
登录后查看更多信息
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
登录
| 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 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 255 | 膚遞壓蓋築顧鏇蓋夢窪(製窪觸襯艱蓋積遞衊衊) = 觸襯齋顧製網衊選選鹹 憲鹽蓋艱鬱鏇鹽選壓壓 (網鑰鑰繭鏇構廠鏇鹽鑰 ) 更多 | 优效 | 2018-09-12 | |||
Atorvastatin strontium+Atorvastatin strontium | 膚遞壓蓋築顧鏇蓋夢窪(製窪觸襯艱蓋積遞衊衊) = 夢鏇鹹艱淵觸構膚鏇範 憲鹽蓋艱鬱鏇鹽選壓壓 (網鑰鑰繭鏇構廠鏇鹽鑰 ) 更多 | ||||||
临床3期 | 374 | 顧餘壓願範築觸夢鑰襯(築醖簾鹽選簾簾範齋窪) = 顧獵衊憲夢齋製廠壓糧 餘窪積積遞衊衊願遞顧 (蓋鹹壓壓襯觸鬱淵鏇窪 ) | 积极 | 2018-09-12 | |||
Placebo | - |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
芽仔
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用