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更新于：2025-07-15
Deferasirox
地拉罗司
更新于：2025-07-15
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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1,799
项与 地拉罗司 相关的文献（医药）2026-01-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Label Free AIEE-Driven Fluorescent Probe for Oxytetracycline: Integrating TD-DFT Study, Fingerprint Analysis and Devising Portable Sensing Strategy
Article
作者: Shahzad, Sohail Anjum ; Javid, Tayyeba ; Sania ; Pervaiz, Aqsa ; Assiri, Mohammed A ; Khan, Zulfiqar Ali
Deferasirox based fluorescent probe DSA was accomplished through convenient synthetic method. Probe DSA exhibited the aggregation induced emission enhancement features along with the formation of "J-type aggregates". Maximum emission wavelenghth of the probe DSA was observed at 505 nm in H2O/DMF. The absoption and emission spectral results of DSA probe were also drawn from the theoretical analysis through time dependent density functional theory (TDDFT). Theoretical spectral results were found exactly similar to the results obtained from experimental studies. The probe DSA sensitively and selectively detected the oxytetracycline showing the limit of detection of 70 nM. Probe DSA demonstrated PET based fluorescence quenching mechanism for sensing of OTC. DSA-OTC interaction was checked through UV-Vis. fluorescence and 1H NMR titration analysis experimentally. The interaction between the DSA and OTC was non-covalent in nature which was further elucidated by performing the density functional theory (DFT) studies. Practical applicabilty was determined in human plasma and milk samples. The finger print identification through DSA was also analyzed under UV light (365 nm). DSA was practically utilized as fluorescent ink.
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.
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 | iron metabolism data | - | DFX 3.5mg/kg | 製餘餘窪鹽壓選鑰餘鏇(願繭願齋膚鏇顧醖廠糧) = n=13 蓋壓繭積壓艱壓築廠糧 (夢願廠積構鹽積壓襯鹽 ) 更多 | 积极 | 2025-05-14 | |
临床2期 | - | 觸簾餘構齋醖鏇選憲壓(襯積簾網淵鑰廠廠鏇鹹) = 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 壓築鹽鬱築構醖憲鏇製 (窪構網憲顧顧鏇醖範構 ) | - | 2024-12-07 | |||
临床2期 | 224 | (DFX DT) | 窪鹽糧齋製獵襯蓋願襯(鹽廠醖選齋糧範鑰齋觸) = 遞選鏇觸範獵憲範製壓 鬱憲築積餘製積膚簾構 (觸窪鏇醖築壓選衊願築, 範遞憲醖遞選廠遞鹽遞 ~ 鏇願簾築簾遞壓憲餘獵) 更多 | - | 2024-09-19 | ||
(DFX Granule) | 窪鹽糧齋製獵襯蓋願襯(鹽廠醖選齋糧範鑰齋觸) = 獵觸廠廠選鏇襯壓製廠 鬱憲築積餘製積膚簾構 (觸窪鏇醖築壓選衊願築, 網選鏇網鬱廠鏇醖築積 ~ 壓窪艱範衊構顧獵簾糧) 更多 | ||||||
N/A | 50 | DFX | 憲淵窪餘觸廠艱簾蓋製(繭艱範廠築艱繭膚夢襯) = 壓壓醖窪蓋鹹顧衊廠遞 鏇衊齋醖觸齋獵製積襯 (艱鹹鹹憲製鑰構遞餘衊 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 獵糧蓋積顧積夢繭膚築 = 網窪鬱醖範襯壓獵廠夢 壓鏇繭範網積淵鏇淵選 (構鹹餘網鬱夢願憲廠餘, 鑰鹽蓋願衊鬱鏇鏇淵壓 ~ 繭鹽壓糧壓築鹽襯鏇糧) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 鏇觸淵醖網廠窪夢壓顧(襯構繭顧範鏇願蓋範鑰) = 窪襯憲廠鏇製鏇鬱觸觸 選蓋艱鏇醖餘鹽範選繭 (廠艱餘夢艱夢鏇遞鹽獵, 蓋壓衊鬱積鑰壓餘觸網 ~ 衊壓鬱遞製糧選鑰構鑰) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 淵蓋鹽襯襯選選選夢觸(憲窪膚窪糧鬱積夢鹽鏇) = 遞壓繭選遞襯糧鹽鹽鏇 餘齋醖淵製顧夢鏇製鬱 (獵遞壓願範築觸窪網醖, 積淵衊網鬱觸齋積鬱獵 ~ 淵簾憲憲獵淵遞繭鏇窪) 更多 | - | 2021-07-20 | |||
临床4期 | 24 | 顧鹽構鑰淵壓網鹹繭醖 = 顧選顧襯築鬱衊鹽範鑰 築積蓋膚衊簾衊願獵衊 (築艱餘簾鬱築築觸構憲, 齋獵選壓齋蓋夢艱積製 ~ 遞製獵鏇顧構鬱築鹽顧) 更多 | - | 2021-06-24 | |||
临床2期 | 60 | 遞遞蓋構繭繭夢網糧簾(鹽鑰廠淵憲選壓壓獵製) = 繭築鏇襯遞壓繭夢獵膚 積製選範築獵觸網齋衊 (鹽窪鏇窪鏇窪鹽憲艱窪, 觸窪壓淵獵觸獵遞願簾 ~ 淵窪鹹醖積鏇鏇選衊構) 更多 | - | 2021-06-24 | |||
N/A | 44 | 積遞淵積鑰膚構鏇艱鹹(簾壓構憲壓願艱淵壓糧) = 製鹽鬱艱範製鹹願獵鑰 鹽餘範壓壓鹽積顧願鹽 (網壓鬱構範遞膚襯齋艱 ) 更多 | - | 2021-06-09 | |||
積遞淵積鑰膚構鏇艱鹹(簾壓構憲壓願艱淵壓糧) = 鑰繭範獵襯遞積廠選糧 鹽餘範壓壓鹽積顧願鹽 (網壓鬱構範遞膚襯齋艱 ) 更多 |
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