预约演示
更新于：2025-02-12
Enarodustat
恩那司他
更新于：2025-02-12
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2020-09-25), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C17H17ClN4O4 |
InChIKeyBPZAJOSLAXGKFI-UHFFFAOYSA-N |
CAS号1262131-60-1 |
关联
45
项与 恩那司他 相关的临床试验NCT06725810
A Prospective, Open-label, Randomized, Multicenter Study on the Rational Hemoglobin Target Value in Patients with Anemia of Non-dialysis Chronic Kidney Disease Treated with Enarodustat
NCT06737081
A Parallel, Open-label Phase II Clinical Study of Enarodustat (SAL-0951) Tablets in the Treatment of Chemotherapy-induced Anemia in Patients With Non-myeloid Malignancies
CTR20243024
恩那度司他（SAL-0951）片在非髓系恶性肿瘤患者中治疗化疗引起贫血的平行、开放Ⅱ期临床研究
100 项与 恩那司他 相关的临床结果
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100 项与 恩那司他 相关的转化医学
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100 项与 恩那司他 相关的专利（医药）
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60
项与 恩那司他 相关的文献（医药）2025-02-01Kidney Medicine
EPO-Mimetic Peptide Pegmolesatide Therapy for Pure Red Cell Aplasia in a Patient with Non-dialysis-dependent Type 1 Diabetic Nephropathy: A Case Report
Article
作者: Wang, Juan ; Chen, Qiong ; Liu, Xuan ; Yang, Man ; Fan, Qiu-Ling
Pure red cell aplasia (PRCA) is a rare complication of erythropoietin (EPO) therapy, characterized by a severe deficiency in red blood cell production. There is no guideline on the treatment for PRCA because there have been too few cases to perform prospective cohort studies. The main treatments for PRCA include immediate cessation of EPO, restrictive transfusion, and immunosuppressive therapies. A 35-year-old male patient with type 1 diabetic nephropathy was diagnosed with PRCA. Enarodustat and roxadustat were administered successively after discontinuation of EPO, but anemia did not improve, and the patient was maintained with weekly blood transfusions. Subsequently, the EPO-mimetic peptide pegmolesatide was administered, and the patient's hemoglobin started to increase after 1 week and increased from 50 g/L to 92 g/L over approximately 3 months. Based on these findings, we speculate that pegmolesatide can provide a safe, effective, and convenient therapeutic strategy for PRCA in Chinese patients with chronic kidney disease.
2025-01-08CURRENT TOPICS IN MEDICINAL CHEMISTRY
Bioanalysis, Analysis, Chemistry, and Pharmacological Aspects of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors
Article
作者: Sharma, Sanjay ; Patil, Roshani ; Jain, Sunidhi
Abstract::
The development of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIFPHIs),
such as Roxadustat (ROX), Enarodustat (ENA), Desidustat (DES), Vadadustat (VAD), Molidustat
(MOL), and Daprodustat (DAP), has significant effects on anemia in chronic kidney disease.
This review presents comprehensive information about the synthesis, pharmacology, and
analysis of HIF-PHIs across several matrices. The literature has presented several approaches for
quantifying HIF-PHIs in diverse sample matrices. Furthermore, HIF-PHIs exhibit similar modes of
action, demonstrating distinct pharmacokinetic parameters. The pharmacological insights encompass
their half-life, mechanism of action, absorption, distribution, metabolism, excretion, and therapeutic
uses. Research indicates that most studies concentrate on hyphenated methodologies for
drug estimation in various biological fluids. Consequently, this study assesses the biological efficacy
of HIF-PHIs and elucidates the analytical methodologies currently employed for measurement
across various matrices.
2024-12-16ChemMedChem
Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat
Article
作者: Brewitz, Lennart ; Tumber, Anthony ; Corner, Thomas P. ; Salah, Eidarus ; Nakashima, Yu ; Schnaubelt, Lara I. ; Kaur, Samanpreet ; Fiorini, Giorgia ; Schofield, Christopher J. ; Allen, Mark D.
Abstract:
Prolyl hydroxylase domain‐containing proteins 1–3 (PHD1–3) are 2‐oxoglutarate (2OG)‐dependent oxygenases catalysing C‐4 hydroxylation of prolyl residues in α‐subunits of the heterodimeric transcription factor hypoxia‐inducible factor (HIF), modifications that promote HIF‐α degradation via the ubiquitin‐proteasome pathway. Pharmacological inhibition of the PHDs induces HIF‐α stabilisation, so promoting HIF target gene transcription. PHD inhibitors are used to treat anaemia caused by chronic kidney disease (CKD) due to their ability to stimulate erythropoietin (EPO) production. We report studies on the effects of the approved PHD inhibitors Desidustat and Enarodustat, and the clinical candidate TP0463518, on activities of a representative set of isolated recombinant human 2OG oxygenases. The three molecules manifest selectivity for PHD inhibition over that of the other 2OG oxygenases evaluated. We obtained crystal structures of Desidustat and Enarodustat in complex with the human 2OG oxygenase factor inhibiting hypoxia‐inducible factor‐α (FIH), which, together with modelling studies, inform on the binding modes of Desidustat and Enarodustat to active site Fe(II) in 2OG oxygenases, including PHD1–3. The results will help in the design of selective inhibitors of both the PHDs and other 2OG oxygenases, which are of medicinal interest due to their involvement inter alia in metabolic regulation, epigenetic signalling, DNA‐damage repair, and agrochemical resistance.
100 项与 恩那司他 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 |
|---|---|---|---|
| 慢性肾衰竭贫血 | 韩国 | 2022-11-17 | |
| 肾性贫血 | 日本 | 2020-09-25 |
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 |
|---|---|---|---|---|
| 伴随慢性肾病的贫血 | 临床3期 | 中国 | 2020-12-08 | |
| 终末期肾脏病 | 临床1期 | 美国 | 2013-05-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | - | 衊鏇遞製鹽觸齋簾膚衊(夢鏇憲憲顧衊襯製夢獵) = 鬱窪淵衊鏇襯憲簾範遞 蓋壓壓鑰壓醖觸願夢壓 (築艱鑰糧鏇淵糧積觸廠 ) | 积极 | 2018-10-23 | |||
衊鏇遞製鹽觸齋簾膚衊(夢鏇憲憲顧衊襯製夢獵) = 廠淵壓艱襯獵膚遞淵夢 蓋壓壓鑰壓醖觸願夢壓 (築艱鑰糧鏇淵糧積觸廠 ) | |||||||
N/A | 40 | 糧壓衊襯蓋醖遞網鑰艱(願蓋壓鬱鹽衊醖鬱鏇衊) = The results of reticulocyte count, hematocrit level and red blood cells in terms of changes from baseline at week 8 were similar to that in hemoglobin 糧鏇窪製窪襯觸壓廠蓋 (齋夢夢餘餘網築選製選 ) 更多 | 积极 | 2015-05-21 | |||
JTZ-951 3 mg | |||||||
N/A | 伴随慢性肾病的贫血 hemoglobin | erythropoietin | 22 | 網顧顧鏇繭鹹廠窪觸艱(夢鬱製憲壓餘齋範蓋鑰) = The results of reticulocyte count, hematocrit level and red blood cells in terms of changes from baseline at Week 6 were similar to that in hemoglobin 醖築積窪鑰鹹淵範積鏇 (鹽簾範鑰齋壓鏇憲構膚 ) 更多 | 积极 | 2015-05-21 | ||
临床1期 | - | JTZ-951 2 mg | 繭鏇製艱窪憲衊餘鹹積(願鹽襯淵願鏇糧製獵築) = 窪築夢鹹夢觸衊醖蓋鏇 夢構鹽觸鬱製襯願遞構 (蓋鑰廠餘膚鹽壓鹹艱餘 ) | 积极 | 2015-05-21 | ||
JTZ-951 10 mg | 繭鏇製艱窪憲衊餘鹹積(願鹽襯淵願鏇糧製獵築) = 鏇餘鏇襯鏇願選廠窪鏇 夢構鹽觸鬱製襯願遞構 (蓋鑰廠餘膚鹽壓鹹艱餘, -0.7 ~ 2.3) |
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