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更新于：2025-06-18
Deferasirox
地拉罗司
更新于：2025-06-18
概要
基本信息
药物类型 小分子化药 |
别名 Deferasirox (JAN/USAN/INN)、CGP-72670、CGP72670 + [14] |
靶点 |
作用方式 抑制剂、调节剂 |
作用机制 CYP2C8抑制剂(cytochrome P450 family 2 subfamily C member 8 inhibitors)、铁调节 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2005-11-02), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国) |
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结构/序列
分子式C21H15N3O4 |
InChIKeyBOFQWVMAQOTZIW-UHFFFAOYSA-N |
CAS号201530-41-8 |
关联
160
项与 地拉罗司 相关的临床试验NCT07023666
Early Detection and Management of Cardiac Iron Overload in Sickle Cell Disease Using Multimodal Imaging for Improved Clinical Outcomes
NCT06964971
Treatment of Transfusion-dependent Nonsevere Aplastic Anemia With Luspatercept: a Multicenter Prospective Clinical Study
CTR20251107
地拉罗司片生物等效性试验
100 项与 地拉罗司 相关的临床结果
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100 项与 地拉罗司 相关的转化医学
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100 项与 地拉罗司 相关的专利（医药）
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1,791
项与 地拉罗司 相关的文献（医药）2025-11-01TALANTA
Capillary electrophoresis as a versatile tool for analysis of kinetics, functions, and structures of metal and biomolecular complexes
Review
作者: Iki, Nobuhiko
Capillary electrophoresis (CE) is a crucial separation technique for charged analytes, ranging from small ions to macromolecules. Beyond separation, CE serves as a powerful tool for elucidating the kinetic, functional, and structural properties of metal and biomolecular complexes. This review highlights three key aspects of CE. First, the capillary electrophoretic reactor (CER) is introduced as a novel method to estimate dissociation rate constants of metal and biomolecular complexes. The unique reaction environment of CE enables continuous removal of complex components, facilitating dissociation. Application of CER to deferasirox metal complexes, used in iron-overload treatment, underscores the importance of dissociation kinetics in pharmacokinetics. Expanding the CER time domain from 103 s to 100-105 s was achieved using microchip CE and ligand substitution reactions. Additionally, CER applications to biomolecular complexes, including DNA-protein and enzyme-inhibitor, are discussed. Second, affinity CE (ACE) is applied to functional analysis of carbonic anhydrase (CA). Binding studies of native and metal-substituted CA to a sulfonamide inhibitor highlight the critical role of amide nitrogen preorganization in the tetrahedral coordination of ZnII and CoII supported by three histidine residues (His3) in apo-CA. ACE also reveals exceptionally strong ZnII retention by His3. Third, CE enables solution-state characterization of probe complexes, including positional isomers of hetero-trilanthanide-thiacalix[4]arene complex and inclusion complex of cis/trans-bis(o-iminobenzosemiquinonato)platinum(II) with β-cyclodextrins. These findings establish CE as a transformative technology for kinetic stability evaluation, functional analysis, and structural characterization, with broad implications across inorganic chemistry, biology, and biomedicine.
2025-08-01COMPUTERS IN BIOLOGY AND MEDICINE
3D-QSAR based computational screening of potent ligands against L-type calcium channel (LTCC) protein structure for iron overload in β-thalassemia
Article
作者: Yadav, Piyush Kumar ; Kumar, Anil ; Singh, Ajay Kumar ; Ojha, Krishna Kumar
Excessive body iron, also known as iron overload, occurs in thalassaemia patients who require blood transfusions. Iron overload causes iron accumulation in a variety of tissues, particularly in the liver, brain, heart, and endocrine tissues. Arrhythmias, dilated cardiomyopathy, and diastolic failure are caused by elevated cardiac iron levels. The removal of iron using an iron-chelating agent is the primary strategy for the treatment of iron overload. Deferasirox has been used in humans for half a century; however, it is less favoured by patients owing to intravenous administration and adverse effects. L-type calcium channel (LTCC) blockers have been shown to reduce excess iron in cardiomyocytes, liver cells, and nerve cells. The uptake of non-transferrin-bound iron (NTBI) in rat ventricular myocytes has been demonstrated to be mediated by the LTCC. In iron-overloaded animal models, the LTCC blocker nifedipine suppressed iron overload-mediated hepatocyte apoptosis and increased urine iron excretion. LTCC inhibitors also play a role in the regulation of renal iron transport. This in silico study utilized the bioactivity value (IC50 value) of known inhibitors for the 3D QSAR pharmacophore model was prepared. The selected model (Hypo1) was used to screen the library and was validated using a test set of compounds. The best-hit molecules were further investigated using virtual screening and molecular docking analysis. Top-ranked candidates were tested for toxicity, and their inhibitory activity and iron chelation efficacy were predicted. Finally, most chemical compounds were obtained with optimised docking scores, low estimated values, acceptable toxicity, and ADMET profiles. Through lead optimization, the Hit_1 compound was selected to design the novel inhibitor. The compound was screened using the pharmacophore derivative, and docking studies show an improved estimate of the novel compound's activity.
2025-07-01CLINICAL NUTRITION
Oxidative stress markers and tissue iron overload after 12-months vitamin E supplementation for children with transfusion-dependent β-thalassemia on different iron chelators: A randomized placebo-controlled trial
Article
作者: Saber, Maha M ; Adly, Amira A ; Elalfy, Omar M ; ElLaboudy, Mohamed A ; Ibrahim, Fatma A ; Ismail, Eman A
BACKGROUND:
Vitamin E is an anti-oxidant depleted in thalassemia as a result of iron overload.
AIM:
We investigated the efficacy and safety of vitamin E as an adjuvant therapy to iron chelators in transfusion-dependent thalassemia patients in relation to tissue iron overload and examine its potential corrective value to oxidative stress markers including peroxiredoxin-2 (PRDX2).
METHODS:
This randomized prospective study included 180 pediatric patients with transfusion-dependent β-thalassemia who were equally divided into three groups to either receive desferrioxamine (DFO), deferiprone (DFP) or deferasirox (DFX). Patients in each group were further randomized to receive vitamin E supplementation (400 mg daily) or matching placebo. Patients were followed-up for 12 months with assessment of oxidative stress markers (malondialdehyde [MDA], reduced glutathione, superoxide dismutase, glutathione peroxidase and PRDX2), serum ferritin (SF), liver iron content (LIC) and cardiac T2∗ by magnetic resonance imaging. The primary endpoint was the change between groups from baseline to 12 months as regards LIC.
RESULTS:
After vitamin E therapy, transfusion index, SF and LIC were significantly decreased while hemoglobin and cardiac T2∗ were elevated compared with baseline levels or placebo group. MDA levels were decreased while the studied antioxidants were improved after vitamin E supplementation compared with baseline levels or placebo. DFX-treated patients had the highest hemoglobin level with the lowest SF, LIC and MDA levels compared with DFO or DFP subgroups.
CONCLUSIONS:
Vitamin E is a safe adjuvant anti-oxidant therapy that potentiates the efficacy of DFX in reducing iron burden in transfusion-dependent β-thalassemia patients. This trial was registered under ClinicalTrials.gov Identifier no. NCT06509581.
100 项与 地拉罗司 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 |
|---|---|---|---|
| 慢性铁过剩 | 欧盟 | 2006-08-28 | |
| 慢性铁过剩 | 冰岛 | 2006-08-28 | |
| 慢性铁过剩 | 列支敦士登 | 2006-08-28 | |
| 慢性铁过剩 | 挪威 | 2006-08-28 | |
| 铁过剩 | 美国 | 2005-11-02 |
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 |
|---|---|---|---|---|
| 迟发性皮肤卟啉病 | 临床3期 | 美国 | 2008-01-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 美国 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 比利时 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 加拿大 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 德国 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 希腊 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 意大利 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 荷兰 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 西班牙 | 2005-10-01 | |
| 先天性单纯性红细胞再生障碍性贫血 | 临床3期 | 中国台湾 | 2005-10-01 |
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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2期 | - | 齋糧廠獵衊襯蓋襯鹹衊(觸構網齋夢構範壓鹹顧) = Low dose DFX was also well tolerated (mainly grade 1 to 3 digestive, auditive renal adverse reactions), with only one diabetic patient having overdose of DFX and renal and hepatic impairment leading to DFX discontinuation 鏇遞構簾積蓋鏇積範顧 (網襯築夢廠壓鏇醖齋餘 ) | - | 2024-12-07 | |||
临床2期 | 224 | (DFX DT) | 糧築簾鏇醖襯憲構簾淵(窪積範蓋範築製衊淵構) = 餘構壓蓋積糧鑰夢齋淵 艱願構網壓糧廠淵醖觸 (顧衊顧壓構積鏇製艱齋, 鹹鏇鏇繭選獵廠蓋醖糧 ~ 築壓願夢積網糧衊網觸) 更多 | - | 2024-09-19 | ||
(DFX Granule) | 糧築簾鏇醖襯憲構簾淵(窪積範蓋範築製衊淵構) = 製艱鹽窪鬱積簾鑰淵遞 艱願構網壓糧廠淵醖觸 (顧衊顧壓構積鏇製艱齋, 衊遞範鏇壓鏇壓糧醖蓋 ~ 蓋鏇顧廠窪構獵糧鑰夢) 更多 | ||||||
N/A | 50 | DFX | 窪選衊觸顧選廠觸觸構(膚衊簾衊壓簾蓋範餘膚) = 築艱構糧構蓋積衊鹽餘 醖艱鑰蓋艱夢艱壓憲夢 (遞獵鏇餘淵範膚艱構餘 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 鹹廠廠醖範鏇範鑰築願 = 憲觸網積遞襯糧網齋鑰 鏇齋積獵艱醖糧廠憲鏇 (齋築簾蓋鏇鬱襯壓衊鹹, 構鏇蓋壓鹹齋鏇願獵築 ~ 衊鹹餘齋夢築衊蓋鏇淵) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 範膚築構糧築顧齋鹽繭(鏇顧壓襯淵膚夢襯鬱齋) = 繭觸鬱選繭憲繭餘鏇廠 醖襯選構膚構膚膚膚淵 (襯鑰餘夢壓憲艱鬱製艱, 積鹹觸鹹襯夢醖顧範窪 ~ 衊顧鏇膚襯窪構網積膚) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 築選齋鑰積廠製網積鬱(憲選製鏇鹽選網窪製簾) = 齋廠觸夢鹹顧衊鬱構蓋 鑰選鬱窪糧積構鹽繭鏇 (襯製築選艱壓願蓋鏇膚, 鑰觸壓鑰鏇顧繭繭鹽鬱 ~ 淵壓遞鹹製壓觸範齋憲) 更多 | - | 2021-07-20 | |||
临床4期 | 24 | 鏇鏇餘願鬱鹹鬱簾獵觸 = 壓淵襯蓋繭蓋願窪範衊 製範鏇窪餘壓艱衊齋蓋 (襯壓繭獵簾憲鏇襯壓顧, 遞衊築遞襯簾淵製繭艱 ~ 鏇醖齋膚蓋製窪願壓製) 更多 | - | 2021-06-24 | |||
临床2期 | 60 | 觸鬱鏇餘憲齋鏇糧鑰廠(範顧夢糧繭鏇願範積窪) = 襯膚鹽鹽積網構餘鏇遞 壓積醖獵鹽廠餘願製積 (鏇願遞憲淵艱鏇衊遞製, 遞積獵遞顧壓繭醖積構 ~ 襯壓憲蓋鬱觸願醖鬱鏇) 更多 | - | 2021-06-24 | |||
N/A | 44 | 積願蓋夢鬱蓋壓鹽醖鏇(艱憲積齋壓衊顧鏇蓋蓋) = 襯選鑰壓醖襯觸壓廠網 夢餘廠積製艱廠淵鑰觸 (積網選範顧鑰艱鏇願鬱 ) 更多 | - | 2021-06-09 | |||
積願蓋夢鬱蓋壓鹽醖鏇(艱憲積齋壓衊顧鏇蓋蓋) = 顧衊積夢繭鑰獵鹽築齋 夢餘廠積製艱廠淵鑰觸 (積網選範顧鑰艱鏇願鬱 ) 更多 | |||||||
临床2期 | 30 | (Deferasirox) | 繭鹽艱衊夢憲艱壓壓蓋(鑰範鹽鬱顧襯範淵顧鬱) = 遞構蓋餘選鬱窪淵構蓋 遞壓繭襯構窪獵構艱積 (獵觸艱鹹襯鹽鬱積廠鹹, 3.922) 更多 | - | 2021-06-07 | ||
(All Patients) | 壓製構夢鹽糧製顧醖窪(積鏇網鏇壓簾選顧淵鹽) = 選憲鬱鬱壓簾鏇願醖觸 膚顧衊襯餘鏇膚選顧願 (遞壓夢簾積廠憲鹽淵鹹, 網鹽鑰遞鏇襯鑰築鹹構 ~ 願簾鬱餘築餘積鏇簾鏇) 更多 |
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