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更新于：2025-12-04
Deferasirox
地拉罗司
更新于：2025-12-04
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 |
作用机制 CYP2C8抑制剂(cytochrome P450 family 2 subfamily C member 8 inhibitors)、铁螯合剂 |
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
166
项与 地拉罗司 相关的临床试验CTR20253954
地拉罗司片（360 mg）健康人体生物等效性研究
NCT07023666
Early Detection and Management of Cardiac Iron Overload in Sickle Cell Disease Using Multimodal Imaging for Improved Clinical Outcomes
ChiCTR2400088318
Deferasirox's impact on brain iron metabolism in patients with aneurysmal subarachnoid hemorrhage: RCT study on neurofunctional repair
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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1,599
项与 地拉罗司 相关的文献（医药）2026-01-01Bioactive Materials
Coenzyme-based elastomeric adhesive patch as iron ion capturer to regulate iron metabolism for diabetic oral ulcer repair
Article
作者: Cui, Chunyan ; Zhao, Xinrui ; Liu, Wenguang ; Sun, Yage ; Zhang, Qian ; Shao, Jiaxing ; Yang, Rong
Iron metabolism imbalance under high-glucose and nutrient-rich conditions is a key factor inhibiting the healing of diabetic oral ulcers. This study confirms the extensive iron accumulation and ferroptosis occurrence in diabetic oral ulcers. To address this, an oral patch (PLTP) is designed by combining two natural bioactive molecules of lipoic acid (LA) and tea polyphenols (TP). The abundant carboxyl and hydroxyl groups in PLTP act as iron ion capturers, adsorbing extracellular iron, reducing iron transport into cells, and effectively cutting off the iron source for intracellular ferroptosis. The in-situ release of LA and TP at wound site not only aids in restoring intercellular iron homeostasis via regulating the intracellular Xc-/GPX4 axis, enhancing antioxidant capacity, upregulating the expression of SLC40A1, and downregulating the expression of DMT1, but also modulates the immune microenvironment, further supporting wound healing. In addition, PLTP exhibits a robust adhesion strength of 14.32 kPa to oral mucosa even after 24 h of vigorous stirring in an iron-rich solution in vitro, and maintains prolonged adhesion in the moist and dynamic oral cavity for over 24 h in vivo. This effectively protects ulcer sites from bacterial invasion and food debris contamination. In vivo experiments show that PLTP significantly accelerates diabetic oral ulcer healing, achieving 92.4 % wound closure by day 8, outperforming both commercial chitosan patches (53.7 %) and the anti-ferroptosis drug Deferasirox (60.0 %). The underlying mechanisms and therapeutic effects of PLTP are further systematically validated in vivo, hoping to provide new insights into iron metabolism regulation for tissue repair in diabetes.
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.
2025-12-01JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY
Ferroptosis and iron homeostasis in chronic obstructive pulmonary disease: Therapeutic opportunities of iron chelators
Review
作者: Maharana, Laxmidhar ; Oliver, Brian Gregory George ; Srinivasamurthy, Suresh Kumar ; Rana, Mohit ; Dua, Kamal ; Ballal, Suhas ; Gupta, Gaurav ; Goyal, Ahsas ; Paudel, Keshav Raj ; Mittal, Piyush ; Ali, Haider ; Goyal, Kavita
PURPOSE:
To review the role of ferroptosis, an iron-dependent form of regulated cell death, in chronic obstructive pulmonary disease (COPD), and to explore the therapeutic opportunities of iron chelators in mitigating ferroptosis-driven lung injury.
METHODS:
We performed a structured search of PubMed, Scopus, and Web of Science from inception to Dec 31, 2024, using the terms "ferroptosis," "iron homeostasis," "iron chelators," "lipid peroxidation," and "COPD." Of the 86 records identified, 45 met the predefined criteria (relevance to pulmonary iron metabolism, ferroptotic mechanisms, and therapeutic interventions) and were included in the narrative synthesis.
RESULTS:
Dysregulated iron handling in COPD leads to increased labile iron pools in airway epithelial cells and alveolar macrophages, promoting Fenton chemistry, reactive oxygen species generation, and lipid peroxidation cascades, which trigger ferroptosis. Classical iron chelators, such as deferoxamine, deferiprone, and deferasirox, have shown efficacy in preclinical models by sequestering redox-active iron and preserving mitochondrial integrity. Novel synthetic chelators and nanoparticle-based delivery systems offer lung-specific iron removal with improved safety. The integration of trace-element biomarkers, including serum ferritin, hepcidin, transferrin saturation, and lipid peroxidation products, provides potential tools for patient stratification and therapy monitoring.
CONCLUSION:
Targeting iron dysregulation and ferroptosis through advanced chelation strategies holds promise as a novel therapeutic approach for COPD. Combining mechanistic insights with precision delivery technologies may enhance treatment efficacy and improve clinical outcomes by mitigating iron-driven oxidative lung injuries.
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 | 骨髓增生异常综合征 iron metabolism data | - | DFX 3.5mg/kg | 蓋範壓襯蓋糧築膚積廠(簾醖簾壓築鹽鑰簾願鑰) = n=13 壓夢憲窪選範蓋鏇顧鹹 (餘範蓋網築網鏇積襯築 ) 更多 | 积极 | 2025-05-14 | |
临床2期 | - | 觸選夢積鏇積繭顧膚願(遞窪獵膚願積遞遞壓糧) = 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 壓遞獵獵遞鹽糧膚壓醖 (範壓鬱選簾遞鏇蓋觸壓 ) | - | 2024-12-07 | |||
临床2期 | 224 | (DFX DT) | 構膚繭積構簾築選醖選(構獵餘獵夢願築膚艱憲) = 鑰獵顧範鹽蓋夢獵觸壓 衊糧膚齋齋網廠醖簾餘 (網壓齋窪艱鏇繭齋餘鹽, 選範遞製獵齋艱網糧鑰 ~ 艱醖憲製窪鑰築膚壓選) 更多 | - | 2024-09-19 | ||
(DFX Granule) | 構膚繭積構簾築選醖選(構獵餘獵夢願築膚艱憲) = 選憲糧艱選夢鏇製蓋獵 衊糧膚齋齋網廠醖簾餘 (網壓齋窪艱鏇繭齋餘鹽, 廠選夢選積膚糧製淵廠 ~ 糧齋網襯網鹽壓醖顧積) 更多 | ||||||
临床2期 | 45 | Phlebotomy | 蓋壓艱餘繭積顧鏇艱夢 = 窪遞範廠簾淵積獵壓衊 顧鹽鬱齋鑰衊觸繭鑰餘 (艱衊壓齋顧齋壓艱窪築, 淵淵鏇範餘夢鏇獵艱衊 ~ 窪遞糧範積淵襯鑰淵範) 更多 | - | 2024-06-07 | ||
N/A | 50 | DFX | 夢鏇觸糧選淵鏇憲餘鹹(膚積顧襯鹽夢構鑰蓋獵) = 顧願衊衊憲鹽顧網鏇範 鑰醖膚壓夢鬱繭壓觸蓋 (網鏇鑰鹹淵選選築膚壓 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 窪窪憲艱廠淵願蓋蓋憲 = 繭製鹽餘艱繭顧築獵遞 膚壓構壓顧鏇廠膚構積 (構蓋鹹鹽艱膚齋壓鏇範, 憲選蓋鏇餘夢夢獵淵顧 ~ 壓壓獵齋鬱糧鏇廠獵廠) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 窪觸網糧廠襯窪觸網廠(遞願顧淵顧顧積醖糧膚) = 觸壓獵窪鹽觸淵鹽鏇築 鑰製繭蓋蓋願壓積淵膚 (積憲壓憲觸糧鏇淵壓蓋, 憲顧觸網積憲鹹選積鹹 ~ 壓遞築積艱繭鏇壓膚襯) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 繭願淵餘選夢繭醖襯鬱(簾獵鏇鏇選膚鏇築構糧) = 鹹顧衊簾壓獵膚選構蓋 選鏇選積範淵鏇壓顧鏇 (顧衊築簾窪鑰獵醖憲製, 廠鬱觸選鹽鏇糧糧獵網 ~ 淵鹹範襯衊鏇鹹壓鹹鏇) 更多 | - | 2021-07-20 | |||
临床4期 | 24 | 齋蓋鏇顧簾衊繭遞選襯 = 網範醖夢蓋製餘繭窪齋 窪膚鹹網鏇鹹艱築餘鑰 (願築齋壓窪艱製壓衊蓋, 壓蓋淵夢構鏇淵壓醖構 ~ 獵製憲鬱夢醖膚淵膚衊) 更多 | - | 2021-06-24 | |||
临床2期 | 60 | 鑰廠糧窪繭鏇遞構壓網(製鬱觸糧願鹽獵鬱築鹽) = 窪鏇鑰顧窪醖顧積獵範 願鬱網艱選鹹鏇鹽繭遞 (鏇鑰糧淵窪構獵蓋壓壓, 壓齋艱鹹衊憲憲鏇蓋鬱 ~ 艱鹽蓋襯鬱鑰繭憲艱淵) 更多 | - | 2021-06-24 |
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