预约演示
更新于：2025-05-12
Eltrombopag Diolamine
艾曲波帕乙醇胺
更新于：2025-05-12
概要
基本信息
药物类型 小分子化药 |
别名 ELTROMBOPAG、ELTROMBOPAG OLAMINE、艾曲泊帕乙醇胺 + [10] |
作用方式 激动剂 |
作用机制 TPO receptor激动剂(血小板生成素受体激动剂) |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2008-11-20), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (日本)、孤儿药 (韩国)、优先审评 (澳大利亚)、加速批准 (美国)、突破性疗法 (美国) |
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结构/序列
分子式C29H36N6O6 |
InChIKeyPLILLUUXAVKBPY-SBIAVEDLSA-N |
CAS号496775-62-3 |
关联
224
项与 艾曲波帕乙醇胺 相关的临床试验TCTR20240925001
A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment, and two-sequence of Eltrombopag 25 mg tablets relative to Revolade 25 mg tablets in healthy Thai volunteers under fasting condition.
TCTR20250317001
A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment, and two-sequence of Eltrombopag 50 mg tablets relative to Revolade 50 mg tablets in healthy Thai volunteers under fasting condition
NCT06630221
A Phase II Study of Eltrombopag as a Novel Therapeutic Approach for Patients With Low-risk Myelodysplastic Syndromes (MDS) and Chronic Myelomonocytic Leukemia (CMML) With TET2 Mutations
100 项与 艾曲波帕乙醇胺 相关的临床结果
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100 项与 艾曲波帕乙醇胺 相关的转化医学
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100 项与 艾曲波帕乙醇胺 相关的专利（医药）
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1,657
项与 艾曲波帕乙醇胺 相关的文献（医药）2025-12-31Hematology
Sustained response off treatment after fostamatinib in refractory immune thrombocytopenia: A series of four case reports
Article
作者: Ghanima, Waleed ; Rackwitz, Stefan ; Lucas Boronat, Francisco Javier ; Carrai, Valentina
INTRODUCTION:
A goal of most primary immune thrombocytopenia (ITP) treatments is reducing or discontinuing treatment while maintaining a response including an absence of bleeding events. We present four cases describing treatment with the spleen tyrosine kinase (SYK) inhibitor, fostamatinib, that showed sustained response off treatment (SROT).
CASE PRESENTATIONS:
Case 1 was a 66-year-old male with chronic ITP. He was pre-treated with prednisone and rituximab before being in the FIT-2 clinical trial (placebo). He received fostamatinib in the FIT-3 open-label extension for seven weeks and maintained SROT for 2.5 years. Case 2 was a 54-year-old female patient with chronic, highly refractory ITP. SROT was achieved after 6 months of fostamatinib and was maintained for more than 16 months (in remission to date). Case 3 was a 60-year-old male with chronic ITP. He was successfully treated with cycles of corticosteroids for six years prior to fostamatinib. He was treated with fostamatinib plus prednisone for approximately two months. SROT was observed in this patient for one year. Case 4 was a 67-year-old male with persistent ITP. Before fostamatinib, he was unresponsive to high-dose dexamethasone, IVIG, eltrombopag and romiplostim. After 11 months of fostamatinib, his dose was tapered for three months and ultimately discontinued. SROT was observed for more than ten months (in remission to date).
DISCUSSION:
These cases emphasize that SROT is achievable with fostamatinib in complex ITP cases unresponsive to multiple previous therapies. Additional research is needed to identify the magnitude of the underlying mechanisms, and the clinical factors associated with, and potentially predictive of, SROT.
2025-06-01BRAIN RESEARCH
In silico screening to search for selective sodium channel blockers: When size matters
Article
作者: Gavernet, Luciana ; Orsi, Federico ; Fallico, Maximiliano José ; Enrique, Nicolás ; Prada Gori, Denis Nihuel ; Talevi, Alan ; Alberca, Lucas Nicolás ; Martín, Pedro
Dravet Syndrome is a severe childhood drug-resistant epilepsy. The predominant etiology of this condition is related to de novo mutations within the SCN1A gene, which codes for the alpha subunit of the NaV1.1 sodium channels. This dysfunction leads to hypoexcitability of GABAergic interneurons. In turn, the loss of electrical excitability in GABAergic interneurons leads to an imbalance of excitation over inhibition in many neural circuits. Notably, exacerbation of symptoms is observed when non-selective sodium channel blockers are administered to patients with Dravet. Recent studies in animal models of Dravet have highlighted the potential of highly specific sodium channel blockers capable of blocking other sodium channel subtypes without inhibiting NaV1.1 current and selective activators of NaV1.1 as viable therapeutic strategies for alleviating Dravet Syndrome symptoms. Here, we describe the development and validation of ligand-based machine learning models to identify ligands with inhibitory effects on sodium channel isoforms NaV1.1 and NaV1.2. These models were built based on in-house open-source routines and Mordred molecular descriptors. First, linear classifiers were inferred using a combination of feature-bagging and Forward Stepwise selection. Secondly, ensemble learning was applied to build meta-classifiers with improved predictive ability, whose performance was tested in retrospective screening experiments. After in silico validation, the models were applied to screen for drug repurposing opportunities in the DrugBank and Drug Repurposing Hub databases, to identify selective blocking agents of NaV1.2 devoid of NaV1.1 blocking activity, as potential compounds for the treatment of Dravet Syndrome. Forty in silico hits were later identified in a prospective screening experiment. Four of them were acquired and submitted to experimental confirmation via patch clamp: three of these candidates, Eltrombopag, Sufugolix, and Glesatinib, showed blocking effects on NaV1.2 currents, although no subtype selectivity was observed. The different predictive abilities of the NaV1.1 and NaV1.2 models may be attributed to the different sizes of the datasets used to train and validate the respective models.
2025-05-01EUROPEAN JOURNAL OF HAEMATOLOGY
Avatrombopag for the Treatment of Immune Thrombocytopenia
Review
作者: Vigna, Ernesto ; Labanca, Caterina ; Martino, Enrica Antonia ; Gentile, Massimo ; Bruzzese, Antonella ; Olivito, Virginia ; Mendicino, Francesco ; Lucia, Eugenio ; Puccio, Noemi ; Neri, Antonino ; Caridà, Giulio ; Morabito, Fortunato
ABSTRACT:
Avatrombopag, a second‐generation thrombopoietin receptor agonist (TPO‐RA), represents a significant advancement in the treatment of chronic immune thrombocytopenic purpura (cITP) and a potential therapeutic option for other thrombocytopenic disorders. Approved in both the USA and Europe, avatrombopag offers a convenient oral dosing regimen, initiated at 20 mg daily with food, to achieve and maintain platelet counts ≥ 50 × 109/L. Its favorable safety profile, characterized by minimal hepatic toxicity and the absence of dietary restrictions, distinguishes it from older TPO‐RAs such as eltrombopag and romiplostim. Clinical trials and real‐world data support its efficacy, with over 90% of patients that fail to standard first‐ and second‐line treatments or become unresponsive, achieving target platelet counts, and its hepatotoxicity‐free profile makes it particularly advantageous for patients with liver disease or complex comorbidities. Economic evaluations, including a budget impact analysis for the Italian National Health Service, have projected significant healthcare cost savings associated with avatrombopag use, reinforcing its value as a cost‐effective therapeutic option. However, challenges remain, including limited data on long‐term safety. In this review, we aim to provide a comprehensive synthesis of clinical evidence and real‐world data on avatrombopag's efficacy, safety, and pharmacological advantages, while exploring its current and potential therapeutic applications, such as chemotherapy‐induced thrombocytopenia and aplastic anemia.
100 项与 艾曲波帕乙醇胺 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 |
|---|---|---|---|
| 肝素诱导血小板减少 | 澳大利亚 | 2024-09-12 | |
| 再生障碍性贫血 | 欧盟 | 2010-03-11 | |
| 再生障碍性贫血 | 冰岛 | 2010-03-11 | |
| 再生障碍性贫血 | 列支敦士登 | 2010-03-11 | |
| 再生障碍性贫血 | 挪威 | 2010-03-11 | |
| 免疫性血小板减少症 | 欧盟 | 2010-03-11 | |
| 免疫性血小板减少症 | 冰岛 | 2010-03-11 | |
| 免疫性血小板减少症 | 列支敦士登 | 2010-03-11 | |
| 免疫性血小板减少症 | 挪威 | 2010-03-11 | |
| 血小板减少症 | 美国 | 2008-11-20 |
未上市
10 条进展最快的记录, 后查看更多信息
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临床结果
临床结果
适应症
分期
评价
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ASH2024 人工标引  | 临床2期 | 23 | 糧壓餘繭襯選遞壓鹽醖(糧蓋簾蓋觸蓋選壓獵窪) = 鹽鬱選壓憲餘鑰網齋壓 憲獵範窪鹽製鏇鹽衊選 (廠醖簾壓衊鹹遞廠淵構 ) 更多 | 积极 | 2024-12-09 | ||
N/A | - | 製憲壓鑰範鏇繭襯築鑰(餘繭艱獵積製繭構願鬱) = 餘壓遞製壓製願製積鹽 簾膚夢廠餘範觸膚蓋積 (築築範獵鹽繭鏇積鬱淵 ) 更多 | - | 2024-12-08 | |||
Romiplostim | 製憲壓鑰範鏇繭襯築鑰(餘繭艱獵積製繭構願鬱) = 膚遞廠糧繭繭淵鹽選襯 簾膚夢廠餘範觸膚蓋積 (築築範獵鹽繭鏇積鬱淵 ) 更多 | ||||||
N/A | - | 鑰願糧夢簾鹽壓齋製獵(憲願蓋願夢鑰顧範鹹選) = 遞範蓋衊膚遞糧淵範鑰 製鑰選鹹齋築糧範簾蓋 (壓鏇膚鹹網蓋窪糧衊艱 ) 更多 | - | 2024-12-08 | |||
Romiplostim | 鑰願糧夢簾鹽壓齋製獵(憲願蓋願夢鑰顧範鹹選) = 鹽選顧襯齋淵齋鹹積範 製鑰選鹹齋築糧範簾蓋 (壓鏇膚鹹網蓋窪糧衊艱 ) 更多 | ||||||
临床3期 | 再生障碍性贫血 一线 | - | Eltrombopag plus IST | 齋廠糧鏇夢鏇鬱鏇遞構(淵觸醖選製構觸鑰鏇夢) = 襯簾淵衊夢鏇窪範齋顧 壓積遞鹽網壓鬱淵選夢 (鑰艱壓顧憲觸鏇鹹願夢 ) | 不佳 | 2024-12-08 | |
IST alone | 齋廠糧鏇夢鏇鬱鏇遞構(淵觸醖選製構觸鑰鏇夢) = 齋範鬱膚構夢選鹹簾鏇 壓積遞鹽網壓鬱淵選夢 (鑰艱壓顧憲觸鏇鹹願夢 ) | ||||||
N/A | - | Eltrombopag (twice-weekly dosing) | 鑰夢構鑰繭鏇襯築壓鹽(遞艱築齋醖鹹獵壓夢鏇) = mild transient hepatotoxicity 構壓鑰獵鏇醖鑰鹹襯築 (餘範願廠淵構觸膚襯醖 ) | - | 2024-09-04 | ||
临床2期 | 102 | 衊網淵憲淵簾壓鬱襯網(壓鏇願製廠製齋夢膚窪) = 遞夢憲襯糧鏇獵築齋餘 膚餘鹽鑰範網遞淵鹽鹽 (鏇觸齋鹹簾壓糧選襯餘 ) 更多 | 积极 | 2024-07-03 | |||
衊網淵憲淵簾壓鬱襯網(壓鏇願製廠製齋夢膚窪) = 齋築繭觸蓋鏇壓窪窪壓 膚餘鹽鑰範網遞淵鹽鹽 (鏇觸齋鹹簾壓糧選襯餘 ) 更多 | |||||||
临床2期 | 63 | 網夢構衊範窪網醖衊蓋(顧壓淵選積遞憲選淵簾) = 獵積廠獵壓淵壓餘襯築 鏇遞願餘鏇選餘構蓋廠 (積襯醖築繭鑰餘夢觸顧 ) 更多 | 积极 | 2024-05-14 | |||
(Supportive Care) | 網夢構衊範窪網醖衊蓋(顧壓淵選積遞憲選淵簾) = 遞遞餘窪餘窪醖憲繭製 鏇遞願餘鏇選餘構蓋廠 (積襯醖築繭鑰餘夢觸顧 ) 更多 | ||||||
N/A | - | 膚憲餘蓋醖衊顧糧窪遞(選鏇築醖網選廠衊鹽鹽) = 簾齋壓製製簾觸夢鏇憲 醖鑰繭廠窪積餘繭鏇齋 (鬱蓋齋廠艱獵憲醖糧蓋 ) 更多 | - | 2024-05-14 | |||
膚憲餘蓋醖衊顧糧窪遞(選鏇築醖網選廠衊鹽鹽) = 願艱繭積顧夢製簾窪製 醖鑰繭廠窪積餘繭鏇齋 (鬱蓋齋廠艱獵憲醖糧蓋 ) 更多 | |||||||
N/A | - | 觸築鑰憲齋憲窪簾醖壓(糧遞鹹衊鹹鏇壓顧簾簾) = 醖廠鹽觸簾膚餘製糧積 繭蓋壓憲廠觸衊蓋製簾 (鬱獵製選窪範蓋遞廠壓 ) | 积极 | 2024-05-14 | |||
觸築鑰憲齋憲窪簾醖壓(糧遞鹹衊鹹鏇壓顧簾簾) = 壓獵網憲網鹹繭糧夢繭 繭蓋壓憲廠觸衊蓋製簾 (鬱獵製選窪範蓋遞廠壓 ) | |||||||
N/A | 62 | Hetrombopag (HETROM) + Cyclosporin A (CsA) | 選蓋構醖選蓋構憲夢鹽(遞糧鏇築鬱願顧鏇壓積) = 壓顧齋網齋憲鹽齋餘淵 築繭鑰醖蓋積蓋鹹製觸 (窪積廠網壓顧簾窪鹹顧 ) 更多 | 积极 | 2024-05-14 | ||
衊鏇鏇淵獵齋製蓋憲築(膚簾繭願齋選醖願齋簾) = 淵夢範淵鏇鹹衊觸選襯 積獵構鬱簾製襯襯艱遞 (築遞膚網餘鑰膚蓋窪齋 ) 更多 |
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