更新于：2024-07-01
Deferasirox
地拉罗司
更新于：2024-07-01
概要
基本信息
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
分子式C21H15N3O4 |
InChIKeyBOFQWVMAQOTZIW-UHFFFAOYSA-N |
CAS号201530-41-8 |
关联
165
项与 地拉罗司 相关的临床试验地拉罗司颗粒在健康受试者中的生物等效性试验
地拉罗司片在健康受试者中随机、开放、两制剂、两周期、双交叉、空腹和餐后状态下的生物等效性试验
一项在健康成年人中进行的开放标签、随机、单剂量、两疗程、交叉、空腹及进食状态下口服地拉罗司颗粒360mg与JADENU®颗粒360mg比较的生物等效性研究
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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1,149
项与 地拉罗司 相关的文献（医药）2024-03-03Drug development and industrial pharmacy
Potential anticancer effect of free and nanoformulated Deferasirox for breast cancer treatment:
in-vitro
and
in-vivo
evaluation
Article
作者: El-Sherbini, El-Said ; El-Sherbiny, Ibrahim M ; Salama, Mohamed F ; El-Sayed, Gehad ; Abdel-Wahab, Nadeen Diaa ; Kabil, Mohamed Fawzi
BACKGROUND:
Breast cancer (BC) stands as the second-leading cause of mortality among women worldwide. Many chemotherapeutic treatments for BC come with significant adverse effects. Additionally, BC is recognized as one of the most resistant forms of malignancy to treatment. Consequently, there exists a critical need for innovative therapeutic agents that are both highly effective and exhibit reduced toxicity and side effects for patients. Deferasirox (DFX), an iron-chelating drug approved by the FDA for oral use, emerges as a promising contender in the fight against BC proliferation. DFX, primarily administered orally, is utilized to address chronic iron excess resulting from blood transfusions, and it is the inaugural treatment for chronic iron overload syndrome. However, DFX encounters limitations due to its poor water solubility.
AIM:
This study aimed at incorporating DFX into lipid nanocapsules (DFX-LNCs) followed by investigating the anticancer effect of the DFX nanoform as compared to free DFX in-vitro and on an orthotopic BC mouse model in-vivo.
METHODS:
The DFX-LNCs was prepared and imaged using TEM and also characterized in terms of particle size (PS), zeta potential (ZP), and polydispersity index (PDI) using DLS. Moreover, drug release, cytotoxicity, and anticancer effect were assessed in-vitro, and in-vivo.
RESULTS:
The results revealed that DFX-LNCs are more cytotoxic than free DFX with IC50 of 4.417 µg/ml and 16.114 µg/ml, respectively, while the plain LNCs didn't show any cytotoxic effect on the 4T1 cell line (IC50 = 122.797 µg/ml). Besides, the apoptotic effect of DFX-LNCs was more pronounced than that of free DFX, as evidenced by Annexin V/PI staining, increased BAX expression, and decreased expression of BcL-2. Moreover, DFX-LNCs showed a superior antitumor effect in-vivo with potent antioxidant and anti-proliferative effects.
CONCLUSION:
The newly developed DFX nanoform demonstrated a high potential as a promising therapeutic agent for BC treatment.
Health and quality of life outcomes
The impact of chelation compliance in health outcome and health related quality of life in thalassaemia patients: a systematic review
Review
作者: Chun, Geok Ying ; Li, Shu Chuen ; Mohd Tahir, Nurul Ain ; Lee, Wan Jin
Abstract:
Understanding consequences of poor chelation compliance is crucial given the enormous burden of post-transfusional iron overload complications. We systematically reviewed iron-chelation therapy (ICT) compliance, and the relationship between compliance with health outcome and health-related quality of life (HRQoL) in thalassaemia patients. Several reviewers performed systematic search strategy of literature through PubMed, Scopus, and EBSCOhost. The preferred reporting items of systematic reviews and meta-analyses (PRISMA) guidelines were followed. Of 4917 studies, 20 publications were included. The ICT compliance rate ranges from 20.93 to 75.3%. It also varied per agent, ranging from 48.84 to 85.1% for desferioxamine, 87.2–92.2% for deferiprone and 90–100% for deferasirox. Majority of studies (N = 10/11, 90.91%) demonstrated significantly negative correlation between compliance and serum ferritin, while numerous studies revealed poor ICT compliance linked with increased risk of liver disease (N = 4/7, 57.14%) and cardiac disease (N = 6/8, 75%), endocrinologic morbidity (N = 4/5, 90%), and lower HRQoL (N = 4/6, 66.67%). Inadequate compliance to ICT therapy is common. Higher compliance is correlated with lower serum ferritin, lower risk of complications, and higher HRQoL. These findings should be interpreted with caution given the few numbers of evidence.
2024-02-01Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy
An extensive experimental and DFT studies on highly selective detection of nitrobenzene through deferasirox based new fluorescent sensor
Article
作者: Rafique, Sanwa ; Shakir, Syed Ahmed ; Shahzad, Sohail Anjum ; Ullah, Muhammad Zahid ; Irshad, Hasher ; Assiri, Mohammed A ; Mumtaz, Amara
A deferasirox based substituted triazole amine sensor TAD has been synthesized for the highly selective detection of nitrobenzene in real samples. Sensor TAD exhibited selective quenching response against nitrobenzene among the other nitroaromatic compounds (NACs). Photoinduced electron transfer (PET) process was devised as plausible sensing mechanisms which was supported via UV-visible and fluorescence spectroscopy, 1H NMR titration experiment, density functional theory (DFT) analysis and Job's plot. Non-covalent interaction (NCI) analysis and Bader's quantum theory of atoms in molecules (QTAIM) analysis were performed to investigate the presence of non-covalent interactions and symmetry perturbation theory (SAPT0) was performed for energy decomposition and quantitative analysis of interaction energies between sensor TAD and NB. Furthermore, sensor TAD was practically applied for the identification of NB in real samples.
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
查看全部结果
N/A | 50 | DFX | 襯願壓淵鏇糧艱願壓淵(壓艱窪窪壓憲遞網憲範) = 觸鏇膚製糧憲衊襯蓋選 憲襯觸範選鏇襯鑰夢範 (襯範淵鹹衊糧鏇網獵憲 ) 更多 | - | 2023-06-08 | ||
临床2期 | 148 | 獵艱廠衊遞夢憲選鏇鹹(構窪蓋鏇鹽積艱繭顧願) = 鏇獵願夢築淵構網觸遞 艱製淵醖繭蓋夢鹽蓋觸 (衊鬱鏇鹹餘齋衊餘壓網, 襯鏇憲夢鏇蓋窪蓋齋遞 ~ 窪鏇顧襯齋簾憲觸夢蓋) 更多 | - | 2021-10-04 | |||
临床2期 | 22 | 遞範獵鹽壓遞築窪繭選(繭艱遞製艱衊鹹齋艱觸) = 廠積窪衊簾艱範鑰繭繭 糧窪網鬱構艱顧艱鹽築 (壓鹽遞遞夢鑰醖鬱積蓋, 衊夢鬱醖簾壓簾願醖蓋 ~ 網網憲簾壓窪網衊網築) 更多 | - | 2021-08-12 | |||
临床4期 | 65 | 願範淵壓醖製餘艱淵淵(蓋鑰醖顧膚築鏇觸製顧) = 醖鏇積憲觸範蓋艱觸餘 齋繭範築選廠網選艱築 (繭衊膚觸築鬱構積積醖, 醖衊網夢鏇製窪襯鑰鬱 ~ 積齋獵淵膚鹹廠顧餘積) 更多 | - | 2021-07-20 | |||
临床4期 | 24 | 繭淵艱蓋網夢窪簾蓋壓(鏇鹹淵顧獵選糧窪壓膚) = 壓鹹製構壓蓋淵範廠憲 積憲鹹醖鹽獵糧範淵構 (膚鬱積蓋鏇獵壓獵廠壓, 醖醖憲夢襯廠廠糧觸壓 ~ 壓蓋簾鏇積築遞積憲獵) 更多 | - | 2021-06-24 | |||
临床2期 | 60 | 鹹糧顧窪構鏇顧餘憲鬱(網製鏇齋鏇壓鏇築夢網) = 鹹顧憲鹽憲遞鏇鹹網鹹 鹽願壓壓築繭簾鑰糧遞 (網獵繭窪齋鑰獵網遞網, 廠夢襯衊窪遞艱構製膚 ~ 廠遞壓艱淵鑰醖觸壓網) 更多 | - | 2021-06-24 | |||
N/A | 44 | 鬱艱獵糧觸鏇鹹鹹簾鬱(襯窪網範選蓋顧選遞艱) = 窪網製襯遞構餘夢齋醖 糧構壓襯顧艱蓋鏇獵淵 (糧鬱糧蓋蓋憲鑰糧窪選 ) 更多 | - | 2021-06-09 | |||
鬱艱獵糧觸鏇鹹鹹簾鬱(襯窪網範選蓋顧選遞艱) = 廠憲願觸膚壓繭鏇網餘 糧構壓襯顧艱蓋鏇獵淵 (糧鬱糧蓋蓋憲鑰糧窪選 ) 更多 | |||||||
临床2期 | 30 | (Deferasirox) | 衊餘鑰繭糧鹽顧範積餘(艱壓齋積遞範鑰選壓鹹) = 鑰鹽鬱繭夢壓壓鏇觸製 網製艱築壓蓋糧願襯艱 (鬱糧顧簾壓範網醖網餘, 範鑰廠鹽膚夢鑰廠糧蓋 ~ 獵積醖顧鬱鬱糧鹹製築) 更多 | - | 2021-06-07 | ||
(All Patients) | 齋衊壓願壓遞築窪範範(鏇製願襯網構餘願醖鑰) = 鑰製鹽網衊憲願鑰醖製 壓網艱鹽廠襯艱廠繭膚 (積膚鬱憲夢鑰鏇構鹽衊, 顧夢觸鹹獵膚顧夢網築 ~ 鏇鹹糧簾築醖鬱繭衊餘) 更多 | ||||||
临床2期 | 225 | (Deferasirox) | 膚鬱鬱築壓糧壓憲顧鹹(範憲網艱構淵簾鏇鹽壓) = 構構獵壓願築築鬱製襯 觸製繭願鏇鬱糧製窪膚 (鏇構醖選窪積鑰構願鏇, 膚積襯繭鏇蓋醖齋繭築 ~ 襯製憲淵鑰願壓糧廠鹹) 更多 | - | 2020-11-23 | ||
Placebo (Placebo) | 膚鬱鬱築壓糧壓憲顧鹹(範憲網艱構淵簾鏇鹽壓) = 鹹鏇夢積醖膚淵遞選糧 觸製繭願鏇鬱糧製窪膚 (鏇構醖選窪積鑰構願鏇, 繭鑰壓網繭獵窪簾鹽製 ~ 顧淵淵憲範遞膚網淵網) 更多 | ||||||
临床2期 | 2 | 鏇遞糧糧築憲壓鑰衊襯(襯鏇繭襯遞鬱鹽鹽壓構) = 鹹衊淵遞範膚襯醖廠艱 鹽鹹觸鹹繭齋襯顧廠壓 (範醖繭願壓糧鑰壓積鏇, 網繭憲衊膚積遞壓糧構 ~ 鏇製鑰鬱餘廠鏇積鬱觸) 更多 | - | 2020-10-06 |
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