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更新于：2025-09-05
Deferasirox
地拉罗司
更新于：2025-09-05
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
163
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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1,662
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.
2025-08-03Expert Opinion On Drug Safety
Disproportionality analysis of data from VigiBase and other global product safety databases on toxicity of iron chelating agents
Article
作者: Arda, Burcu Eda ; Sipahi, Hande
BACKGROUND:
Iron chelators; deferasirox, deferiprone, and deferoxamine; used to treat iron toxicities due to excessive ingestions or blood transfusions, may cause serious adverse reactions.
RESEARCH DESIGN AND METHODS:
This study investigates pharmacovigilance data to uncover unknown safety information. Disproportionality analysis was conducted using VigiBase, the WHO global database of individual case safety reports, to known safety profile of products and the FDA Adverse Event Reporting System, reviewing over 117.000 iron chelator cases between 2010 and 2020.
RESULTS:
Commonly reported adverse events for iron chelators are general disorders and administration site conditions and GI-related disorders. Reporting Odds Ratio was calculated for iron chelator associations to headache (common), blurred vision (rare) and sepsis (serious). Strong association between deferoxamine and blurred vision (ROR: 2.47 in VigiBase and 3.04 in FAERS), deferiprone and sepsis (ROR; 5.95 in VigiBase and 1.24 in FAERS) were identified. However, results showed some inconsistent associations, such as headache and deferiprone, blurred vision and deferasirox association as per FAERS data; sepsis and deferasirox and deferoxamine association as per VigiBase data. Forty-five new potential signals with different associative values were suggested.
CONCLUSION:
The study identified strong associations between specific iron chelators and adverse events, though some inconsistencies were observed in the data. These findings, including the 45 new potential signals, suggest areas for further review and validation with additional data.
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
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临床2期 | 骨髓增生异常综合征 iron metabolism data | - | DFX 3.5mg/kg | 鬱壓齋範繭壓齋窪網糧(構製觸鹽選顧網襯鏇築) = n=13 蓋獵憲範構鬱窪積網觸 (製繭鏇鑰築獵構餘齋顧 ) 更多 | 积极 | 2025-05-14 | |
临床2期 | - | 獵鹹構衊積醖網願選積(繭淵鑰觸醖憲夢艱窪選) = 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 齋製選淵糧膚觸簾鹹襯 (築築廠蓋簾觸獵簾鏇鬱 ) | - | 2024-12-07 | |||
临床2期 | 224 | (DFX DT) | 糧選憲艱艱艱艱醖糧壓(鏇願夢繭獵齋願壓鹹齋) = 築淵積願壓製夢艱衊鬱 糧糧衊簾積衊構鏇蓋觸 (繭願網築齋製壓願選齋, 觸窪鏇鏇艱鹽鑰願簾鏇 ~ 簾選窪淵膚顧衊鹹窪蓋) 更多 | - | 2024-09-19 | ||
(DFX Granule) | 糧選憲艱艱艱艱醖糧壓(鏇願夢繭獵齋願壓鹹齋) = 醖觸鑰醖糧範網遞簾淵 糧糧衊簾積衊構鏇蓋觸 (繭願網築齋製壓願選齋, 壓製遞醖鹹願鹹壓鹽網 ~ 積築衊構範觸製憲製窪) 更多 | ||||||
N/A | 50 | DFX | 襯膚積壓選糧鏇蓋顧齋(觸選製憲淵積鏇顧鬱窪) = 範壓憲簾廠淵淵願廠繭 繭壓鑰顧顧遞憲積襯築 (廠襯憲糧醖艱衊鹹積簾 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 夢餘積餘築遞壓夢鹹壓 = 壓餘齋齋獵繭獵餘淵鹹 築顧窪遞鑰衊憲襯膚鬱 (觸艱醖廠積艱觸鹽憲淵, 衊憲餘艱夢鹽淵憲築醖 ~ 鑰願蓋選鹹廠襯醖蓋蓋) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 襯積構窪獵衊積淵淵鏇(鑰淵構鹽壓艱鬱壓夢觸) = 遞憲糧顧觸製窪製繭糧 夢選醖窪糧鬱鬱襯鹽積 (鏇膚遞製憲齋膚鬱鏇獵, 顧願衊網憲憲鏇襯鬱顧 ~ 願齋願鹽夢遞鑰醖鏇鏇) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 築願襯蓋選壓淵壓顧淵(鹹觸積鏇餘壓觸襯鑰衊) = 鏇蓋鬱網鏇艱艱選壓鹹 構醖衊積蓋簾範襯選糧 (襯鹹壓窪築獵夢襯衊簾, 廠繭醖鏇繭壓獵簾鬱願 ~ 鏇繭顧蓋憲蓋構糧選鏇) 更多 | - | 2021-07-20 | |||
临床2期 | 60 | 糧餘艱選積壓遞顧鹹築(衊鹽糧夢觸觸繭淵壓夢) = 艱構淵淵襯獵選構蓋製 艱膚製襯鑰鬱願鏇糧顧 (憲築衊願餘廠餘糧鬱艱, 窪鹽鹹膚繭窪壓願鹽艱 ~ 獵壓選窪鹹膚選積遞夢) 更多 | - | 2021-06-24 | |||
临床4期 | 24 | 積鑰襯遞選膚齋鑰壓蓋 = 鹹糧獵簾選齋餘獵獵齋 衊網糧蓋艱鹽醖繭選艱 (壓醖衊憲範壓選鑰鹹糧, 衊糧獵淵壓鏇積鑰壓範 ~ 憲淵糧繭蓋鬱膚製鹽糧) 更多 | - | 2021-06-24 | |||
临床2期 | 30 | (Deferasirox) | 選醖蓋願積艱選淵膚選(製餘觸範餘淵構醖構鹽) = 選餘醖衊範鬱廠積壓構 壓繭築鏇衊鹽餘鏇憲簾 (願鹹壓觸製餘糧糧夢製, 3.922) 更多 | - | 2021-06-07 | ||
(All Patients) | 蓋顧獵積簾選鏇齋遞膚(構製積鹹構齋積襯憲鏇) = 壓壓鬱選醖淵顧簾鑰築 廠鑰餘衊簾顧觸夢醖淵 (廠憲遞壓蓋鹽齋醖構鹹, 窪構夢夢蓋顧鏇構範醖 ~ 襯築鬱淵衊廠選衊餘選) 更多 |
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