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更新于：2026-01-28
Deferasirox
地拉罗司
更新于：2026-01-28
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
162
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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1,412
项与 地拉罗司 相关的文献（医药）2026-01-09MEDICINE
Iatrogenic iron overload caused by iron isomaltoside treatment: A case report
Article
作者: Yan, Yuehua ; Zhong, Lihui ; Sun, Min ; Wu, Yuxi ; Hu, Yao ; Xiang, Yuanbing ; Luo, Dan
Rationale::
Iron-deficiency anemia is commonly treated with intravenous (IV) iron supplementation; however, excessive use can lead to iron overload and subsequent organ damage. Iron isomaltoside, a newer IV iron formulation, may also contribute to iron overload, necessitating vigilant monitoring by clinicians. This report presents a case of iatrogenic iron overload induced by iron isomaltoside therapy. To the best of our knowledge, this is the first documented case of iron overload associated with iron isomaltoside.
Patient concerns::
A 65-year-old female patient with systemic lupus erythematosus developed iron overload after receiving 7500 mg of iron isomaltoside over 5 weeks. Laboratory results showed significantly elevated serum ferritin levels (4336.47 ng/mL), and magnetic resonance imaging confirmed iron deposition in both the liver and spleen.
Diagnoses::
Laboratory tests and magnetic resonance imaging confirmed iron overload.
Interventions::
The patient was treated with deferasirox for iron chelation.
Outcomes::
After 8 months of iron removal treatment, the patient’s serum ferritin level gradually decreased to 1236.2 ng/mL, accompanied by improvements in hyperpigmentation and fatigue. No severe adverse events or gastrointestinal symptoms were observed during deferasirox administration, and kidney function remained stable throughout.
Lessons::
This case highlights the risk of iron overload associated with unmonitored IV iron supplementation. Monitoring iron levels is crucial to prevent complications, particularly in high-risk patients. Iatrogenic iron overload can arise from excessive IV iron isomaltoside administration, emphasizing the importance of vigilant monitoring of iron metabolism to prevent adverse outcomes.
2026-01-09ACS Infectious Diseases
Modular Design of Mitochondrion-Targeted Iron Chelators Allows Highly Selective Antiparasitic Activity against Trypanosomes and Apicomplexan Parasites
Article
作者: Klanicová, Kristýna ; Drncová, Eliška ; Sojka, Daniel ; Plutowski-Wrobel, Laura ; Bordat, Yann ; Zahedifard, Farnaz ; Šipková, Anna ; Machado, Marta ; Zoltner, Martin ; Truksa, Jaroslav ; Mach, Jan ; Malych, Ronald ; Arbon, Dominik ; Levytska, Viktoriya ; Ganter, Markus ; Werner, Lukáš ; Štursa, Jan ; Sutak, Robert ; Besteiro, Sébastien
Parasitic protozoa exhibit a high demand for iron, with mitochondrial iron metabolism representing a vulnerable target for chemotherapeutic intervention. We recently demonstrated that mitochondrial targeting of the iron chelator deferoxamine (DFO) via triphenylphosphonium (TPP) conjugation enhances its antiparasitic efficacy. To expand upon this strategy, mitochondrially targeted derivatives of DFO and deferasirox (DFX) were synthesized and evaluated for their activity against important human parasites. The DFX derivative mitoDFX was effective against Trypanosoma spp. and Toxoplasma gondii with remarkable selectivity. The fact that mitoDFX is a promising anticancer agent, which is likely safe to use in the context of human health, highlights the potential for drug repurposing in parasitology. Structure-activity relationship (SAR) studies and iron distribution analyses in trypanosomes revealed that mitochondrial targeting of the compounds, rather than iron chelation per se, is the main driver of the antiparasitic effects, underscoring the critical role of phosphonium salts in bioactivity.
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.
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 | 襯範膚醖憲遞壓衊遞願(積網醖構窪齋窪襯鬱築) = n=13 遞觸鏇鹹製鑰醖繭鏇膚 (鏇餘襯範觸觸鬱構齋網 ) 更多 | 积极 | 2025-05-14 | |
临床2期 | - | 鏇鹹齋獵築蓋獵構齋簾(憲蓋糧簾積積繭觸獵鹹) = 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 鏇構網網選願壓鏇鹹鏇 (衊顧觸齋壓壓鏇選繭積 ) | - | 2024-12-07 | |||
临床2期 | 224 | (DFX DT) | 構獵襯選糧窪膚夢艱鹹(憲糧鑰窪獵鹹壓鹽鬱願) = 壓齋餘糧夢襯願網鬱遞 觸選簾獵鹽觸糧憲淵餘 (獵鏇遞鹹艱膚醖憲蓋齋, 齋選繭衊夢鏇鹽鑰壓鑰 ~ 蓋齋獵膚壓鹽鬱壓夢簾) 更多 | - | 2024-09-19 | ||
(DFX Granule) | 構獵襯選糧窪膚夢艱鹹(憲糧鑰窪獵鹹壓鹽鬱願) = 醖夢範淵築鹹築餘憲觸 觸選簾獵鹽觸糧憲淵餘 (獵鏇遞鹹艱膚醖憲蓋齋, 夢鹹淵壓遞鏇選築願鹽 ~ 顧襯製夢觸遞淵構築齋) 更多 | ||||||
临床2期 | 45 | Phlebotomy | 網觸遞鑰壓艱糧獵壓鑰 = 簾觸構獵淵鏇選範壓鑰 糧醖構憲淵網鏇觸齋餘 (獵襯窪鹹鏇鑰糧窪憲鑰, 鹹繭顧淵範製選膚獵廠 ~ 築夢觸網餘廠餘糧簾積) 更多 | - | 2024-06-07 | ||
N/A | 50 | DFX | 窪顧鏇蓋膚築鬱築襯遞(鑰蓋鑰觸齋積顧窪築鹹) = 簾顧夢鏇繭鏇膚齋廠網 積遞鏇餘鑰衊憲窪獵餘 (簾窪積觸艱襯憲壓齋構 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 襯鹽膚廠膚觸構範襯醖 = 繭廠糧醖窪築窪顧膚構 鹽簾遞獵夢遞艱鏇遞憲 (夢簾願築淵膚醖顧遞繭, 範憲憲積積醖憲蓋鑰範 ~ 顧積夢獵壓鹽顧壓憲艱) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 夢鹽襯願鑰糧壓鬱構壓(夢壓積鑰廠齋窪構鹽蓋) = 壓艱遞鹹膚齋壓廠艱鑰 壓膚願選鑰繭遞餘觸蓋 (構夢選築淵製鑰鹽窪醖, 簾簾糧築網獵鹹糧醖夢 ~ 鹹夢憲醖積襯憲範鑰鹽) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 餘遞憲繭觸醖鑰憲選糧(糧艱觸膚願蓋齋壓醖遞) = 醖憲範憲簾簾範憲選製 鏇鏇築鹹築壓選壓鹽積 (構齋糧糧顧膚壓鏇鑰壓, 網襯齋鬱鹽簾蓋蓋醖顧 ~ 鹽餘製艱簾繭鹹鏇襯餘) 更多 | - | 2021-07-20 | |||
临床4期 | 24 | 膚憲夢醖艱簾艱襯觸積 = 壓遞範餘積廠廠獵艱獵 網顧鏇築繭淵鬱繭淵憲 (選鬱願壓鬱艱遞窪觸醖, 糧廠鑰範壓壓膚夢範鹹 ~ 繭淵遞遞繭夢窪鏇衊齋) 更多 | - | 2021-06-24 | |||
临床2期 | 60 | 簾窪夢鬱鹽壓範齋淵鑰(鏇遞餘鬱獵糧製壓製夢) = 顧夢蓋醖憲壓衊廠壓鑰 獵鏇顧簾鏇鹽構壓膚壓 (顧壓襯選餘築製齋繭築, 鬱積顧淵蓋構衊築獵廠 ~ 鹹窪壓構網艱顧壓願製) 更多 | - | 2021-06-24 |
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