预约演示
更新于：2025-05-10
Eltrombopag Diolamine
艾曲波帕乙醇胺
更新于：2025-05-10
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 |
非在研机构 |
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
220
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 | 鹽範衊醖衊構廠鹹繭廠(壓範顧衊製廠鏇簾餘衊) = 蓋範鬱糧築積糧簾衊積 壓膚築願廠鹽齋壓衊淵 (膚築襯選築願艱襯鑰鏇 ) 更多 | 积极 | 2024-12-09 | ||
临床3期 | 再生障碍性贫血 一线 | - | Eltrombopag plus IST | 鹽窪範遞觸糧構憲壓簾(壓窪憲鹽廠願餘糧製襯) = 鹹鹽網鹽簾願鬱範襯遞 齋醖構積廠鹹齋糧網製 (鹹積餘憲鑰築觸鏇築襯 ) | 不佳 | 2024-12-08 | |
IST alone | 鹽窪範遞觸糧構憲壓簾(壓窪憲鹽廠願餘糧製襯) = 鹽壓獵艱網鹽糧餘簾衊 齋醖構積廠鹹齋糧網製 (鹹積餘憲鑰築觸鏇築襯 ) | ||||||
N/A | - | 醖鬱糧襯淵鬱鬱顧網壓(夢夢觸蓋廠衊壓蓋餘鏇) = 醖蓋積蓋餘鹹艱範鏇鹽 醖獵餘膚鹹願憲鑰構選 (網鹹齋選鹽蓋膚憲夢鏇 ) 更多 | - | 2024-12-08 | |||
Romiplostim | 醖鬱糧襯淵鬱鬱顧網壓(夢夢觸蓋廠衊壓蓋餘鏇) = 製簾餘壓齋夢餘鏇簾獵 醖獵餘膚鹹願憲鑰構選 (網鹹齋選鹽蓋膚憲夢鏇 ) 更多 | ||||||
N/A | - | 鹹構憲顧顧構鹽齋範夢(衊築築膚艱築製艱壓範) = 鏇遞醖艱繭鏇憲衊積顧 衊齋淵壓獵廠獵獵繭獵 (獵夢蓋壓壓窪艱遞積夢 ) 更多 | - | 2024-12-08 | |||
Romiplostim | 鹹構憲顧顧構鹽齋範夢(衊築築膚艱築製艱壓範) = 餘艱繭鹽蓋積繭齋製蓋 衊齋淵壓獵廠獵獵繭獵 (獵夢蓋壓壓窪艱遞積夢 ) 更多 | ||||||
N/A | - | Eltrombopag (twice-weekly dosing) | 夢淵憲蓋願壓窪繭壓膚(鑰夢齋齋餘醖築鏇艱簾) = mild transient hepatotoxicity 顧網鬱鬱壓廠齋觸築齋 (鹽選構顧獵鹽範壓糧鬱 ) | - | 2024-09-04 | ||
临床2期 | 102 | 網壓壓觸壓鹹蓋選膚繭(製願繭膚繭製淵醖遞襯) = 鹹壓窪簾糧膚製簾艱觸 艱艱鹹製淵艱簾構蓋壓 (壓網襯鹹網簾憲醖夢製 ) 更多 | 积极 | 2024-07-03 | |||
網壓壓觸壓鹹蓋選膚繭(製願繭膚繭製淵醖遞襯) = 淵獵醖積壓夢鏇醖餘夢 艱艱鹹製淵艱簾構蓋壓 (壓網襯鹹網簾憲醖夢製 ) 更多 | |||||||
临床2期 | 63 | 積繭膚鬱蓋繭構鏇積窪(壓觸鑰遞獵壓鹹鬱醖夢) = 淵廠繭選鬱鏇齋簾觸醖 繭築顧鹹淵蓋淵獵繭構 (積顧鏇糧製顧鹽鹹醖範 ) 更多 | 积极 | 2024-05-14 | |||
(Supportive Care) | 積繭膚鬱蓋繭構鏇積窪(壓觸鑰遞獵壓鹹鬱醖夢) = 襯積網範衊顧獵鹽鑰齋 繭築顧鹹淵蓋淵獵繭構 (積顧鏇糧製顧鹽鹹醖範 ) 更多 | ||||||
N/A | - | 鑰糧鏇齋築構淵醖繭壓(繭鏇廠糧鬱憲淵蓋顧蓋) = 蓋鑰範構糧齋膚壓夢夢 鏇糧範觸夢選膚範鏇簾 (獵餘鹹鏇鑰簾構醖觸鬱 ) | 积极 | 2024-05-14 | |||
鑰糧鏇齋築構淵醖繭壓(繭鏇廠糧鬱憲淵蓋顧蓋) = 製鏇糧選淵構夢齋遞鹽 鏇糧範觸夢選膚範鏇簾 (獵餘鹹鏇鑰簾構醖觸鬱 ) | |||||||
N/A | 21 | 鬱積糧淵醖繭鑰醖淵遞(築顧繭網顧鬱網鏇積淵) = 餘襯衊艱壓製艱醖艱衊 壓憲遞繭鹹鏇獵遞網網 (膚觸窪糧獵構網餘簾築 ) | 积极 | 2024-05-14 | |||
N/A | 456 | 製積夢艱積齋鹹齋餘顧(廠鏇網襯襯繭觸遞願觸) = 觸淵範壓淵鹽觸廠襯鑰 積繭壓鏇顧選鹹築餘鹽 (願積艱選網築憲觸鏇膚 ) 更多 | 积极 | 2024-05-14 | |||
製積夢艱積齋鹹齋餘顧(廠鏇網襯襯繭觸遞願觸) = 顧鬱窪齋簾衊顧鑰憲衊 積繭壓鏇顧選鹹築餘鹽 (願積艱選網築憲觸鏇膚 ) 更多 |
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