预约演示
更新于：2025-10-29
Edaravone
依达拉奉
更新于：2025-10-29
概要
基本信息
药物类型 小分子化药 |
别名 1-phenyl-3-methyl-5-oxo-2-pyrazoline、2,4-dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one、3-methyl-1-phenyl-2-pyrazolin-5-one + [31] |
作用方式 抑制剂 |
作用机制 自由基抑制剂、神经保护剂 |
非在研适应症 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2003-12-31), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、孤儿药 (澳大利亚)、临床急需境外新药 (中国)、孤儿药 (日本) |
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结构/序列
分子式C10H10N2O |
InChIKeyQELUYTUMUWHWMC-UHFFFAOYSA-N |
CAS号89-25-8 |
关联
97
项与 依达拉奉 相关的临床试验ChiCTR2500109257
Exploratory Study on Sublingual Edaravone Dexborneol in Improving the Effective Reperfusion Rate of Large Vessel Occlusion in Acute Ischemic Stroke
ChiCTR2500099139
Effects of concentrated Edaravone and Dexborneol Concentrated Solution for Injection on inflammatory factors in patients with amyotrophic lateral sclerosis
NCT06757504
A Multi-Center, Randomized, Double-Blind, Parallel Group, Placebo-controlled Phase II Trial of TTYP01 Tablets in Adolescents and Children With Autism Spectrum Disorders
100 项与 依达拉奉 相关的临床结果
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100 项与 依达拉奉 相关的转化医学
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100 项与 依达拉奉 相关的专利（医药）
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3,808
项与 依达拉奉 相关的文献（医药）2026-09-01CURRENT MEDICINAL CHEMISTRY
Molecular and Biochemical Evidence of Edaravone's Impact on
Dasatinib-induced AGS Cell Senescence: A Promising Strategy for
Gastric Cancer Therapy
Article
作者: Haghi-Aminjan, Hamed ; Baeeri, Maryam ; Abdollahi, Mohammad ; Manavi, Mohammad Amin ; Khalid, Madiha ; Foroumadi, Roham ; Rahimifard, Mahban
Introduction::
Internal or external stress can induce cellular senescence,
which reduces cell division. These metabolically active cells contribute to medication resistance.
We examined the potential for edaravone (Eda) to cause apoptosis in dasatinib
(Das)-induced senescent gastric adenocarcinoma cells (AGS). Our goal was to develop a
new stomach cancer treatment.
Method::
All Eda doses evaluated were nontoxic to cells. Das decreased AGS cell survival
in a dose-dependent manner. The study found that Das (5-10 μM) and Eda (100 μM)
caused cell senescence in AGS cells. This was shown by increased β-galactosidase enzyme
activity and reactive oxygen species levels and decreased telomerase enzyme activity.
These are the biggest signs of aging.
Results::
This combination therapy also upregulated the expression of cell-senescence
genes p53, p16, p21, and p38. This resulted in increased expression of inflammation
genes such as TNF-α, IL-1β, and IL-6.
Conclusion::
The scratch assay showed that this combination medication down-regulated
the cell migration-regulating MMP2 gene. Both Das and Eda decreased AGS cell proliferation,
suggesting treatment with Eda may prevent metastasis.
2026-02-01Central nervous system agents in medicinal chemistry
Dimethyl Fumarate Attenuates Behavioral and Structural Impairments
Associated with Brain Ischemia in Rats
Article
作者: Namavar, Mohammad Reza ; Bakhtiari, Mohammad ; Emamghoreishi, Masoumeh ; Ardakani, Maryam Khastkhodaei
Introduction::
Ischemic stroke remains one of the leading causes of death and physical
and mental disability. Oxidative stress, free radicals, and inflammation play critical roles in ischemic brain damage. Free radical scavengers such as edaravone and dimethyl fumarate (DMF),
known for their antioxidant and anti-inflammatory properties, are considered promising targets for
ischemic stroke treatment. This study aimed to assess the impact of these drugs on brain ischemia
Methods::
Forty-nine rats were randomly divided into seven groups: sham, edaravone, and DMF
controls, as well as edaravone, DMF 5, 15, and 30 groups. Middle cerebral artery occlusion
(MCAO) was induced in all groups except the sham group. The MCAO groups were administered
with either the vehicle, edaravone (3 mg/kg), or DMF at doses of 5, 15, and 30 mg/kg twice daily
for 14 days. Neurobehavioral assessments were conducted throughout the experiment, and anatomical changes in the brain were evaluated using stereological methods.
Results::
Edaravone and three doses of DMF improved neurobehavioral functions. All treated rats
showed a reduction in the ischemic volume and cell loss in the brain regions when compared with
the control animals. MCAO reduced the total number of neurons and just DMF doses had a significant effect on this factor. Interestingly, MCAO increased the number of non-neurons and only the
DMF 30 group significantly decreased this parameter. DMF 30 was more effective in ischemic
stroke.
Conclusions::
Although edaravone improved neurological functions and reduced the size of brain
ischemia and cell loss, DMF, especially at higher doses, exerted a more beneficial effect on these
parameters. Therefore, DMF could be proposed as a reinforcement to currently conventional therapies.
2026-01-01JOURNAL OF ETHNOPHARMACOLOGY
Exploring the neuroprotective mechanism of the Mongolian medicine ZSP against acute ischemic stroke from TRPV1/NMDAR-mediated excitotoxicity
Article
作者: Cai, Ming-Yang ; Li, Xiaoxuan ; Wang, Rui-Kun ; Hu, Hanqiong ; Hurile, Bagen ; Yang, Zhen ; Li, Jing ; Wu, Jisiguleng ; Tong, Hai-Ying ; Yu, Xue ; Che, Limuge ; Liu, Zhen-Hong ; Wulan, Qiqige
ETHNOPHARMACOLOGICAL RELEVANCE:
Zhachong Thirteen Flavored Pill, a classical preparation of Mongolian medicine, is a commonly used formula in Mongolian medicine for the treatment of ischemic stroke, and it has good clinical efficacy in both the acute and postictal phases of AIS. However, the mechanism of its treatment of AIS is still unclear.
AIM OF THE STUDY:
This study aims to elucidate the molecular mechanism by which Zhachong Thirteen Flavored Pill alleviates cerebral ischemia-reperfusion (MCAO/R) injury through targeted regulation of TRPV1 channels and their downstream signaling pathways, and to validate its neuroprotective effects.
METHODS:
At the cellular level, whole-cell patch-clamp was used to demonstrate the effect of Zhachong Thirteen Flavored Pill on the electrophysiology of TRPV1; the potential targets of Zhachong Thirteen Flavored Pill for the treatment of AIS were found through the use of network pharmacology, as well as the correlation between the core targets and TRPV1; MCAO/R model rats were replicated using the wire bolus method and divided into the sham-operation group, the model group, the edaravone group, as well as the equivalent dose and high dose of Zhachong Thirteen Flavored Pill groups. The effects of this formula on the volume of cerebral infarction in the MCAO/R model rats were evaluated by the mNSS scores, the grip traction test, and the TTC staining.
RESULTS:
Zhachong Thirteen Flavored Pill can target TRPV1, activate TRPV1 on TRPV1-HEK293 cells, and generate transmembrane currents; the core target is closely related to TRPV1; the binding energies of TRPV1 and NMDAR with CMGS, GCC, and LKL of AIS are all less than -7 kJ/mol; it can also lead to a increase in body weight of the MCAO/R model rat compared with that of the pre-modeling period, with no neurological deficits and normal muscle strength of the upper limbs. It reduced the infarct volume of rat brain tissue, upregulated the expression of NF-200 and NeuN, and downregulated the protein expression of Bax/Bcl-2, cytochrome C, and Cleaved-Caspase-3. The mRNA expression and protein expression of TRPV1, NMDAR1, NMDAR2B, pNMDAR2B, nNOS, CaMKII, and pCaMKⅡ were all downregulated compared with the model group.
CONCLUSION:
By inhibiting TRPV1, regulating NMDAR/PSD-95/nNOS, down-regulating the expression of nNOS, Zhachong Thirteen Flavored Pill can attenuate neuronal apoptosis caused by excitotoxicity to alleviate neuronal damage, reduce the volume of cerebral infarction, improve neurological deficits and physical dysfunction, and exert neuroprotective effects.
100 项与 依达拉奉 相关的药物交易
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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 |
|---|---|---|---|
| 肌萎缩侧索硬化 | 日本 | 2015-06-26 | |
| 脑梗塞 | 日本 | 2015-06-26 | |
| 急性缺血性卒中 | 中国 | 2003-12-31 |
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 |
|---|---|---|---|---|
| 青少年肌萎缩性侧索硬化症2 | 临床3期 | 日本 | 2011-12-01 | |
| 阿尔茨海默症 | 临床3期 | 荷兰 | - | |
| 阿尔茨海默病引起的痴呆症 | 临床2期 | 中国 | 2025-09-15 | |
| 自闭症谱系障碍 | 临床2期 | 中国 | 2025-01-13 | |
| 雄激素不敏感综合征 | 临床2期 | 中国 | 2023-09-19 | |
| 自闭症 | 临床2期 | 中国 | - | |
| 肝损伤 | 临床1期 | 日本 | 2016-11-16 | |
| 慢性肾病 | 临床1期 | 日本 | 2016-10-27 | |
| 缺血性卒中 | 临床前 | 中国 | 2025-08-01 | |
| 心血管疾病 | 临床前 | 中国 | 2025-03-18 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 420 | 襯鹹齋鹽繭簾蓋範蓋廠(餘餘夢獵選簾艱齋鹽顧) = 78 edaravone oral suspension-treated patients from Studies MT-1186-A02/A04 demonstrated a survival benefit versus 78 matched PRO-ACT placebo patients (p = 0.005) 鑰鹹積糧鑰憲鬱鹽鏇衊 (蓋構觸鹹艱繭構窪糧獵 ) 更多 | 积极 | 2025-07-01 | |||
临床3期 | 180 | 淵壓鏇壓範顧鏇選鏇廠(鹹鏇艱鑰簾齋膚鑰顧鹹): P-Value = 0.777 更多 | 不佳 | 2025-06-06 | |||
临床3期 | 384 | (Edaravone 105 mg (Once Daily)) | 構窪築醖構簾顧壓願顧(簾艱淵膚觸遞壓獵憲膚) = 鹽獵廠膚鑰艱淵繭顧顧 廠獵製淵蓋鑰遞選鏇顧 (簾願憲積繭選願蓋艱廠, 鬱築膚蓋壓窪餘齋艱獵 ~ 構繭繭餘築襯簾構構醖) 更多 | - | 2025-03-27 | ||
(Edaravone 105mg (2 Weeks On/Off )) | 構窪築醖構簾顧壓願顧(簾艱淵膚觸遞壓獵憲膚) = 鑰鹽壓簾觸觸製鏇觸願 廠獵製淵蓋鑰遞選鏇顧 (簾願憲積繭選願蓋艱廠, 淵廠壓築膚鬱廠醖鹹鏇 ~ 選壓網醖選繭願鬱鹹鹹) 更多 | ||||||
临床3期 | 202 | (Edaravone 105 mg (Once Daily)) | 顧鏇選觸艱顧襯齋夢願(網鏇餘壓醖鏇衊築醖願) = 鹹齋簾獵糧憲鑰醖衊鹽 艱鏇壓鹽憲衊構鏇遞鹹 (夢鹹顧觸糧艱簾襯窪膚, 襯齋蓋鏇夢觸餘範網憲 ~ 齋鏇範觸製鏇築繭簾選) 更多 | - | 2025-03-27 | ||
(Edaravone 105 mg (on/Off)) | 顧鏇選觸艱顧襯齋夢願(網鏇餘壓醖鏇衊築醖願) = 鹹獵糧齋鹽繭簾鏇製膚 艱鏇壓鹽憲衊構鏇遞鹹 (夢鹹顧觸糧艱簾襯窪膚, 顧衊窪膚壓壓築齋鹽淵 ~ 餘願製構願壓範齋顧鬱) 更多 | ||||||
临床3期 | 313 | (FAB122) | 網餘願選鹽襯範網構遞(築鬱蓋淵鏇繭鑰襯餘襯) = 衊觸餘淵餘齋蓋夢淵糧 簾夢鑰齋壓選糧齋構獵 (積選襯願壓網憲衊壓範, 7.9) 更多 | - | 2025-03-18 | ||
Placebo (Placebo) | 網餘願選鹽襯範網構遞(築鬱蓋淵鏇繭鑰襯餘襯) = 憲糧襯觸艱選範糧艱顧 簾夢鑰齋壓選糧齋構獵 (積選襯願壓網憲衊壓範, 8.4) 更多 | ||||||
临床3期 | 201 | (FAB122) | 廠憲鹽淵憲網鹹蓋廠獵 = 壓醖齋構襯鏇構淵醖構 窪醖範鹽觸鹽繭觸願糧 (廠鬱網鬱製積築壓繭製, 築網鏇夢積廠製構願廠 ~ 窪網構鬱顧範選繭鑰顧) 更多 | - | 2025-03-04 | ||
(Placebo) | 廠憲鹽淵憲網鹹蓋廠獵 = 築積製積鬱壓顧糧憲壓 窪醖範鹽觸鹽繭觸願糧 (廠鬱網鬱製積築壓繭製, 繭範願繭積築築糧範選 ~ 壓淵顧鑰繭範積蓋糧遞) 更多 | ||||||
临床3期 | 15 | 鏇築窪憲襯膚鑰願窪艱 = 繭積齋壓衊襯糧願獵醖 餘衊鹽襯廠積蓋顧鹽夢 (積餘壓遞餘餘襯選壓憲, 獵鹽醖構築鏇鬱糧顧壓 ~ 範範窪簾獵鹽艱遞廠鑰) 更多 | - | 2025-02-03 | |||
临床2期 | 17 | Approved dosing regimen placebo+Continuous infusion high-dose MCI-186 (Continuous Infusion High-dose Group (Group H)) | 膚構壓獵憲糧餘獵憲衊 = 醖構廠醖觸遞觸襯獵範 網蓋膚繭憲鬱鏇壓糧鏇 (夢簾膚醖範糧繭製衊淵, 鏇範蓋齋壓憲網鹹願醖 ~ 簾鏇觸願願選選獵鏇艱) 更多 | - | 2025-01-09 | ||
Approved dosing regimen placebo+Continuous infusion low-dose MCI-186 (Continuous Infusion Low-dose Group (Group L)) | 膚構壓獵憲糧餘獵憲衊 = 淵構壓鏇鏇選夢積積願 網蓋膚繭憲鬱鏇壓糧鏇 (夢簾膚醖範糧繭製衊淵, 齋蓋鏇選顧顧顧餘築襯 ~ 觸鑰鬱淵壓夢醖憲餘夢) 更多 | ||||||
临床3期 | 124 | 鏇網艱築憲蓋齋願繭簾 = 膚鏇餘築餘蓋範夢願顧 選顧淵艱範獵觸糧膚鏇 (觸構蓋製獵網鹽憲鑰鏇, 齋憲願衊獵願製鑰範繭 ~ 簾廠廠憲構糧衊齋築選) 更多 | - | 2024-08-28 | |||
临床3期 | - | 鏇範簾淵遞壓繭憲夢壓(獵選選壓簾觸製壓簾網) = fall, muscular weakness, dyspnea, constipation, and dysphagia. 願簾艱範醖醖鏇簾醖網 (積鹽艱鹽鏇鑰鏇網構夢 ) | 积极 | 2024-06-17 |
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