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更新于：2026-04-09
Evategrel
依福格雷
更新于：2026-04-09
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床1期 |
特殊审评- |
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结构/序列
分子式C21H26ClNO7S |
InChIKeyJIHSKBXKKCQDED-DIJKAEOVSA-N |
CAS号2760609-74-1 |
关联
3
项与 依福格雷 相关的临床试验CTR20250384
一项在中国健康成人受试者中评价多次口服苯磺酸CG-0255胶囊的药效动力学特征、药代动力学特征、安全性和耐受性的I期、开放性临床研究
CTR20244747
一项在中国健康成人受试者中评价单次给予注射用苯磺酸CG-0255（静脉注射）的药效动力学特征、药代动力学特征、安全性、和耐受性的I期、开放性临床研究
CTR20260630
一项评价苯磺酸CG-0255 胶囊在健康成年参与者中的食物影响的单中心、随机、开放、两周期、双交叉的I 期临床研究
100 项与 依福格雷 相关的临床结果
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100 项与 依福格雷 相关的转化医学
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100 项与 依福格雷 相关的专利（医药）
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3
项与 依福格雷 相关的文献（医药）2026-06-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Development and validation of a sensitive and rapid UHPLC-MS/MS method for the simultaneous quantification of CG-0255 and its active metabolite in human plasma and its application to Phase I studies
Article
作者: Li, Jiali ; Xu, Hongrong ; He, Gongxin ; Wu, Hao ; Yan, Hua ; Chen, Hanjing ; Sheng, Lei ; Li, Xuening ; Yuan, Fei ; Liu, Chao
CG-0255, a thiol prodrug of clopidogrel's active metabolite H4 (CG-0236), is a novel thienopyridine P2Y12 receptor antagonist under initial clinical development for the treatment of acute coronary syndromes. Unlike clopidogrel, CG-0255 is converted to the active thiol metabolite H4 (CG-0236) in a single hydrolytic step. Compared with clopidogrel, CG-0255 exhibits more efficient and consistent H4 formation in humans, which can be quantified in plasma following either intravenous or oral administration. In this study, we developed and validated a sensitive, rapid, and robust UHPLC-MS/MS method for the simultaneous quantification of CG-0255 and its derivatized active metabolite (MP-H4, CG-0261) in human plasma. After solid-phase extraction from 94.5 μL of plasma, analytes and isotope-labeled internal standards were separated on an ACQUITY UPLC BEH C18 column (2.1 mm × 50 mm, 1.7 μm) using isocratic elution with 0.1 % formic acid in water and acetonitrile (57:43, v/v) at a flow rate of 0.5 mL/min, followed by a 3.5 min column washing and re-equilibration, giving a total analytical run time of 7 min. Baseline separation of CG-0255, CG-0261, and their respective isomers was achieved. Detection was performed using positive electrospray ionization in multiple reaction monitoring mode on a Q-Trap 6500+ mass spectrometer. Calibration curves were linear over 0.05-25 ng/mL for both analytes, corresponding to 0.0353-17.65 ng/mL for H4 (CG-0236). Intra- and inter-day precision and accuracy were within ±15 % at all quality-control levels. The validated assay was successfully applied to two phase I clinical studies conducted at our center, characterizing the pharmacokinetics of CG-0255 following single-dose intravenous and multiple-dose oral administration. This UHPLC-MS/MS method provides a reliable platform for the quantitative evaluation of CG-0255 and its active metabolite in human plasma, and is well suited to support further global clinical development.
2025-12-01BIOCHEMICAL PHARMACOLOGY
Promising clopidogrel analogs may overcome clopidogrel resistance: 2025 update
Review
作者: Mi, Qiong-Yu ; Jia, Yu-Meng ; Ji, Jin-Zi ; Tai, Ting ; Jiang, Li-Ping ; Xie, Hong-Guang
Clopidogrel is one of the World Health Organization-recommended essential medicines used for antiplatelet therapy. However, its usage is limited by resistance of certain patients to clopidogrel. Herein, we systematically summarized promising novel analogs of clopidogrel and evaluated their preclinical and clinical properties as well as the science behind the study. The primary strategy of their design and synthesis is largely focused on how to enhance their metabolic activation, significantly increasing the systemic exposure of their active thiol metabolites (such as H4). Of these, DT-678 released H4 into the blood following exposure to GSH due to bypassing all cytochrome P450-mediated metabolic activation processes of clopidogrel; evategrel (formerly CG-0255) was converted to H4 by esterase-catalyzed hydrolysis. Vicagrel, acetate of clopidogrel, was completely hydrolyzed to 2-oxo-clopidogrel by intestinal hydrolases, thus bypassing the first-step oxidation of clopidogrel and consequently increasing the formation of H4. The same strategies as those for prasugrel and vicagrel were used to design new compounds, such as tipidogrel, compound 6b, PLD-301, and W-1. In addition, 2-oxo-clopidogrel, an intermediate metabolite shared by clopidogrel, vicagrel, PLD-301, and W-1, was used to determine whether it could exert the same antiplatelet effect as its parent drugs. Moreover, clopidogrel and vicagrel were also deuterated to further increase the formation of H4 in the liver. All these new compounds in the pipeline are promising antiplatelet drugs, and superior to clopidogrel. DT-678 and evategrel are considered the best clopidogrel analogs that may overcome clopidogrel resistance due to their superior efficacy and safety profiles over clopidogrel.
2025-11-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Discovery of a novel and potent antiplatelet thiol prodrug CG-0255
Article
作者: Tang, Xiubo ; Chen, Xiaowu ; He, Gongxin ; Wu, Hao ; Fan, Wenyuan ; Hou, Kai ; Zhang, Yuanchao ; Lu, Changliang ; Gu, Ziqiang
A series of novel thiol prodrugs based on clopidogrel active metabolite H4 were conceived and synthesized as a new generation of antiplatelet agents. The prodrugs are capable of being rapidly converted to H4 through fast one-step hydrolysis catalyzed by carboxylesterases, thus potentially overcoming clopidogrel resistance and many other issues caused by the reliance of clopidogrel on cytochrome P-450 (CYP)-mediated oxidative bioactivation. One of the thiol prodrugs, CG-0255, was selected for further development. CG-0255 exhibited excellent pharmacokinetic and pharmacodynamic properties suitable for being developed as a once daily oral antiplatelet drug. In addition, CG-0255 possessed adequate solubility and chemical stability capable of being formulated as an intravenous formulation, expanding its uses into surgical or emergency settings where intravenous administration is more desired. CG-0255 is the first P2Y12 inhibitor available in both intravenous and oral formulation, showing several advantages, such as rapid onset of action, low risk of drug-drug interaction, and an expected reduction in individual variation.
100 项与 依福格雷 相关的药物交易
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 急性冠状动脉综合征 | 临床3期 | - | - | |
| 缺血性卒中 | 临床3期 | - | - | |
| 动脉粥样硬化 | 临床1期 | 中国 | 2025-02-14 | |
| 冠状动脉疾病 | 临床1期 | 中国 | 2024-12-31 | |
| 脑梗塞 | 临床1期 | 美国 | - |
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