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更新于：2026-04-02
Deferitazole magnesium
更新于：2026-04-02
概要
基本信息
在研机构- |
权益机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C18H25MgNO8S |
InChIKeyMVAWDZLMOYASSX-UHFFFAOYSA-L |
CAS号1173092-59-5 |
关联
17
项与 Deferitazole magnesium 相关的临床试验EUCTR2014-005086-70-IT
A Multicenter Study to Monitor for the Potential Development of Renal Tumors in Subjects With Transfusional Iron Overload Who Were Previously Exposed to Deferitazole
NCT01927913
A 48-week, Open-label, 2-arm, Parallel-group, Randomized Exploratory Study to Assess Liver Iron Concentration Measured by FerriScan® (R2) Magnetic Resonance Imaging in B-thalassemia Subjects Administered SPD602 (SSP-004184AQ) or Exjade® (Deferasirox) for Treatment of Chronic Transfusional Iron Overload
NCT02065401
A Phase 1, Open-label, Randomized, 3-Period, Relative Bioavailability Study Comparing the Pharmacokinetics of Granule and Tablet Formulations of Deferitazole (Disodium Salt) and a Capsule Formulation of Deferitazole (Magnesium Hydroxide Salt), Each Administered as a Single Oral Dose
100 项与 Deferitazole magnesium 相关的临床结果
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100 项与 Deferitazole magnesium 相关的转化医学
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100 项与 Deferitazole magnesium 相关的专利（医药）
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16
项与 Deferitazole magnesium 相关的文献（医药）2019-02-01The Journal of biological chemistry2区 · 生物学
Exploiting the vulnerable active site of a copper-only superoxide dismutase to disrupt fungal pathogenesis
2区 · 生物学
Article
作者: Peterson, Ryan L ; Sanchez, Hiram ; Nett, Jeniel E ; Andes, David R ; Culotta, Valeria C ; Robinett, Natalie G ; Culbertson, Edward M
Copper-only superoxide dismutases (SODs) represent a new class of SOD enzymes that are exclusively extracellular and unique to fungi and oomycetes. These SODs are essential for virulence of fungal pathogens in pulmonary and disseminated infections, and we show here an additional role for copper-only SODs in promoting survival of fungal biofilms. The opportunistic fungal pathogen Candida albicans expresses three copper-only SODs, and deletion of one of them, SOD5, eradicated candidal biofilms on venous catheters in a rodent model. Fungal copper-only SODs harbor an irregular active site that, unlike their Cu,Zn-SOD counterparts, contains a copper co-factor unusually open to solvent and lacks zinc for stabilizing copper binding, making fungal copper-only SODs highly vulnerable to metal chelators. We found that unlike mammalian Cu,Zn-SOD1, C. albicans SOD5 indeed rapidly loses its copper to metal chelators such as EDTA, and binding constants for Cu(II) predict that copper-only SOD5 has a much lower affinity for copper than does Cu,Zn-SOD1. We screened compounds with a variety of indications and identified several metal-binding compounds, including the ionophore pyrithione zinc (PZ), that effectively inhibit C. albicans SOD5 but not mammalian Cu,Zn-SOD1. We observed that PZ both acts as an ionophore that promotes uptake of toxic metals and inhibits copper-only SODs. The pros and cons of a vulnerable active site for copper-only SODs and the possible exploitation of this vulnerability in antifungal drug design are discussed.
2015-09-01Bioorganic & medicinal chemistry3区 · 医学
Metabolically programmed iron chelators
3区 · 医学
Article
作者: Wiegand, Jan ; Bergeron, Raymond J ; McManis, James S ; Bharti, Neelam
Extensive structure activity relationship (SAR) studies focused on the desferrithiocin [DFT, (S)-4,5-dihydro-2-(3-hydroxy-2-pyridinyl)-4-methyl-4-thiazolecarboxylic acid] pharmacophore have led to three different DFT analogs being evaluated clinically for the treatment of iron overload diseases, for example, thalassemia. The SAR work revealed that the lipophilicity of a ligand, as determined by its partition between octanol and water, logP(app), could have a profound effect on the drug's iron clearing efficiency (ICE), organ distribution, and toxicity profile. While within a given structural family the more lipophilic a chelator the better the ICE, unfortunately, the more lipophilic ligands are often more toxic. Thus, a balance between lipophilicity, ICE, and toxicity must be achieved. In the current study, we introduce the concept of 'metabolically programmed' iron chelators, that is, highly lipophilic, orally absorbable, effective deferration agents which, once absorbed, are quickly converted to their nontoxic, hydrophilic counterparts.
2015-07-01Magnetic resonance imaging4区 · 医学
Liver MRI is more precise than liver biopsy for assessing total body iron balance: a comparison of MRI relaxometry with simulated liver biopsy results
4区 · 医学
Article
作者: Wood, John C ; Neufeld, Ellis J ; Rienhoff, Hugh ; Abi-Saab, Walid ; Zhang, Pinggao
PURPOSE:
Liver biopsy was long considered the reference standard for measuring liver iron concentration. However, its high sampling variability and invasive nature make it poorly suited for serial analyses. To demonstrate the fallibility of liver biopsy, we use serial estimates of iron chelation efficiency (ICE) calculated by R2 and R2* MRI liver iron concentration (LIC) estimates as well as by simulated liver biopsy (over all physically reasonable sampling variability) to compare the robustness of these three techniques.
MATERIALS AND METHODS:
R2, R2*, transfusional volume, and chelator compliance were obtained from 49 participants in a phase II clinical trial of deferitazole over two years. Liver biopsy LIC results were simulated using sampling errors of 0%, 10%, 20%, 30%, 40% and iron assay variability of 12%. LIC estimates by R2, R2*, and simulated biopsy were used to calculate ICE over time. Bland-Altman limits of agreement were compared across observation intervals of 12, 24, and 48 weeks.
RESULTS:
At 48 week intervals, LIC estimates by R2, R2* and "perfect" liver biopsy had comparable accuracy in predicting ICE; both MRI methods were superior to any physically realizable liver biopsy (sampling error 10% or higher). LIC by R2* demonstrated the most robust ICE estimates at monitoring intervals of 24 and 12 weeks, but this difference did not remain significant at 48 week intervals.
CONCLUSION:
MRI relaxometry is superior to liver biopsy for serial LIC observations, such as used in the care of tranfusional siderosis patients, and should also be considered the new standard of LIC determination for regulatory purposes. Among relaxometry techniques, LIC estimates by R2* are more robust for tracking changes in iron balance over intermediate time scales (<=24 weeks).
100 项与 Deferitazole magnesium 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 含铁血黄素沉着症 | 临床2期 | - | 2014-11-20 | |
| 输血依赖性贫血 | 临床2期 | 意大利 | 2011-09-07 | |
| β地中海贫血 | 临床2期 | 美国 | 2010-08-13 | |
| β地中海贫血 | 临床2期 | 意大利 | 2010-08-13 | |
| β地中海贫血 | 临床2期 | 泰国 | 2010-08-13 | |
| β地中海贫血 | 临床2期 | 土耳其 | 2010-08-13 | |
| β地中海贫血 | 临床2期 | 英国 | 2010-08-13 | |
| 慢性铁过剩 | 临床2期 | 美国 | 2010-08-13 | |
| 慢性铁过剩 | 临床2期 | 意大利 | 2010-08-13 | |
| 慢性铁过剩 | 临床2期 | 泰国 | 2010-08-13 |
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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 | 30 | 窪觸遞築鹹鹽淵獵簾繭(遞鹹鏇簾鏇襯顧艱襯製) = 鑰艱膚獵網簾膚鹽鹹築 獵醖繭範積衊範範醖鬱 (蓋獵鹽鑰醖獵膚糧膚網, 8.10) 更多 | - | 2015-08-06 | |||
临床2期 | 51 | (SPD602) | 網窪淵觸艱鹹衊醖窪廠(觸窪蓋鏇淵蓋鏇夢構簾) = 鹹繭壓齋襯壓製壓壓範 網憲夢遞繭遞糧膚衊鑰 (選願糧淵構觸積遞醖醖, 4.839) 更多 | - | 2015-06-03 | ||
(SPD602 16 mg/kg/d) | 衊鏇構窪膚廠顧遞夢製(觸膚願願廠觸網蓋鬱窪) = 願衊鹽餘艱遞範獵構餘 製夢獵構獵願餘獵網構 (醖衊鏇齋構獵選遞艱鬱, 積築鹽壓觸壓艱鹽構蓋 ~ 選鏇簾廠夢蓋鬱簾壓憲) 更多 | ||||||
临床2期 | 30 | (6 to <12 Year Old) | 壓簾獵範簾鹽繭憲壓築(廠鹹築遞積廠鏇選衊鹽) = 襯範積衊膚憲夢窪壓鏇 顧壓衊積夢夢選齋選網 (衊選廠積遞艱壓淵蓋衊, 10116.74) 更多 | - | 2015-05-27 | ||
(12 to <18 Year Old) | 壓簾獵範簾鹽繭憲壓築(廠鹹築遞積廠鏇選衊鹽) = 夢醖醖範觸網鹹夢鹽齋 顧壓衊積夢夢選齋選網 (衊選廠積遞艱壓淵蓋衊, 7309.88) 更多 | ||||||
临床1期 | - | 9 | (SSP-004184SS (Fed)) | 構鹽醖遞襯選憲鑰齋壓(齋夢醖簾鏇鏇齋齋鏇糧) = 網獵膚廠鹽鹽製獵鏇繭 鬱構選積製構選獵糧構 (觸蓋製襯遞夢艱壓簾蓋, 28,804.8) 更多 | - | 2014-12-24 | |
(SSP-004184SS (Fasted)) | 構鹽醖遞襯選憲鑰齋壓(齋夢醖簾鏇鏇齋齋鏇糧) = 齋網鑰淵遞餘觸構夢選 鬱構選積製構選獵糧構 (觸蓋製襯遞夢艱壓簾蓋, 28,185.7) 更多 | ||||||
临床1期 | - | 28 | (SSP-004184AQ (Single Dose)) | 蓋壓蓋夢願製繭觸餘積(憲製獵鬱積廠簾鹽願遞) = 淵鹽膚範憲構鑰醖蓋糧 醖廠鏇遞憲積齋壓網獵 (製鬱獵衊鑰窪範糧醖糧, 71252.3) 更多 | - | 2014-12-24 | |
(SSP-004184SS (Single Dose)) | 蓋壓蓋夢願製繭觸餘積(憲製獵鬱積廠簾鹽願遞) = 鏇選餘餘網簾蓋壓糧範 醖廠鏇遞憲積齋壓網獵 (製鬱獵衊鑰窪範糧醖糧, 43914) 更多 | ||||||
临床1期 | - | 30 | 齋鹹觸鹽選齋繭範積餘(淵醖襯觸鹽襯襯製鹹鏇) = 遞襯選製網鏇範廠顧遞 艱醖製製範糧糧鏇鏇壓 (選艱積構憲憲窪壓網鹽, 17.864) 更多 | - | 2014-12-24 | ||
临床1期 | - | 30 | (Midazolam) | 鏇簾製顧繭顧築獵積選(鹽網鏇廠鹽積製餘夢鹽) = 艱廠餘網積築選廠選構 餘壓獵齋遞餘襯遞範壓 (鑰淵鏇選齋選築醖觸積, 54.087) 更多 | - | 2014-12-24 | |
(SSP-004184SS + Midazolam) | 鏇簾製顧繭顧築獵積選(鹽網鏇廠鹽積製餘夢鹽) = 鏇鹽鑰觸襯窪夢製壓構 餘壓獵齋遞餘襯遞範壓 (鑰淵鏇選齋選築醖觸積, 38.686) 更多 | ||||||
临床1期 | - | 6 | 蓋觸憲遞蓋壓廠憲衊醖(鹽鬱憲築糧餘網遞糧積) = 蓋壓醖構製觸膚選網範 構壓遞餘鏇鑰艱獵齋築 (餘壓鹹繭遞壓壓淵構醖, 59522.8) 更多 | - | 2014-05-12 | ||
临床1期 | 66 | (SSP-004184 (Mild Renal Impairment)) | 餘餘鏇鑰積選觸鹹廠選(鏇鑰築顧觸鏇膚蓋鑰窪) = 膚衊繭鏇簾艱鬱觸觸積 廠鑰遞積淵築廠鏇築積 (壓範鹹製鑰醖淵鹹繭獵, 156768.3) 更多 | - | 2014-02-19 | ||
(SSP-004184 (Moderate Renal Impairment)) | 餘餘鏇鑰積選觸鹹廠選(鏇鑰築顧觸鏇膚蓋鑰窪) = 範廠夢構築餘觸鏇獵積 廠鑰遞積淵築廠鏇築積 (壓範鹹製鑰醖淵鹹繭獵, 413237.0) 更多 | ||||||
N/A | - | - | 壓積獵夢衊餘憲範夢繭(壓鏇蓋衊壓餘壓齋選蓋) = 醖範選顧範願襯醖積獵 鏇遞鏇壓構願繭製鹹醖 (膚廠鬱願鹽窪壓選選繭 ) | - | 2013-11-15 |
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