Deferasirox - CAS 201530-41-8
Catalog number: B0046-062367
Category: APIs
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Deferasirox is an oral iron chelator used to treat chronic iron overload in patients receiving long term blood transfusions.
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Catalog Number Size Price Stock Quantity
B0046-062367 250 mg $248 In stock
B0046-062367 500 mg $398 In stock
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CGP-72670, CGP 72670, CGP72670, ICL670; IC-L670; ICL 670; ICL-670A; ICL670A; IC L670A; Deferasirox. Brand name: Exjade; Desirox; Defrijet; Desifer.
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1. Oxygen catalyzed mobilization of iron from ferritin by iron(III) chelate ligands
Fadi Bou-Abdallah,* Justin McNally, Xing Xin Liu and Artem Melman*. Chem. Commun., 2011, 47, 731–733
In conclusion, chelate ligands of 2,4-bis[hydroxy(methyl)amino]-1,3,5-triazine family are capable of rapidly mobilizing iron from ferritin. Our data suggest that iron release from ferritin is catalyzed by oxygen and involves reduction of the iron core by superoxide anion. The reduced iron diffuses out of the ferritin shell and forms Fe(III)-complexes with BHT with the concomitant production of superoxide anions. A similar iron release process is suggested to occur with the commonly used iron-chelate desferroxamine (DFO) but not with deferasirox (DFX).
2. Design of iron chelators with therapeutic application
Tao Zhou, Yongmin Ma, Xiaole Kong and Robert C. Hider*. Dalton Trans., 2012, 41, 6371–6389
Triazoles have been investigated as ligands by Novartis. These molecules chelate iron(III) with two phenolate oxygens and one triazolyl nitrogen. The lead compound deferasirox (18) possesses a pFe3+ value of 22.5 and is extremely hydrophobic, with a log Pwater–octanol value of 3.8 and a log D7.4 value of 1.0. As a result, it can penetrate membranes easily and possesses good oral availability. Indeed, when orally administered to hypertransfused rats, deferasirox promotes the excretion of chelatable iron from hepatocellular iron stores four to five times more effectively than DFO. By virtue of a high proportion of both the free ligand and the 2 : 1 iron complex binding to albumin (greater than 98%), the ligand is relatively nontoxic despite its strong lipophilic character. The ability to bind to albumin also offers an explanation for the finding that deferasirox-induced iron excretion occurs mainly in the faeces, with little iron being excreted in the urine. The extreme hydro-phobicity of this chelator necessitates formulation in dispersion tablets, containing three disintegrants, SDS, povidone and cros-povidone. Thus deferasirox is typically given once daily each morning as a dispersed solution in water, half an hour before breakfast. Deferosirox has been demonstrated to be efficient at removing liver iron from regularly transfused patients but is apparently less effective at removing cardiac iron.
3. Deferitazole, a new orally active iron chelator
Robert C. Hider,* Xiaole Kong, Vincenzo Abbate, Rachel Harland, Kelly Conlon and Tim Luker. Dalton Trans.,2015, 44,5197–5204
Iron is essential for virtually all prokaryotes and eukaryotes because it has a critically important role in enzyme function; in humans it is a cofactor in over 400 enzymes including those involved in oxygen transport. However, excess iron leads to uncontrolled Fenton chemistry and resulting oxidative damage to proteins and cell membranes. Consequently, in the non-stressed individual, iron levels are maintained within carefully controlled limits. Iron accumulation in humans can result from increased absorption of dietary iron or from regular blood transfusions. The use of repeated blood transfusions to maintain hemoglobin levels is the cornerstone of treatment for the spectrum of hereditary anemias such as β-thalassemia major. Continued iron accumulation leads to liver disease, diabetes mellitus, and heart disease. As a consequence, treatment with an iron(III)-selective chelating agent is the favored approach to enhance the excretion of iron and to facilitate its removal from iron-loaded tissues. The iron chelators in current clinical use are desferrioxamine, deferiprone, and deferasirox. Desferrioxamine is not orally active and both deferiprone and deferasirox, although orally active, possess limitations in both efficacy of iron removal from certain tissues and in their associated side effects. Thus there is a demand for novel orally active iron chelators that possess a larger therapeutic window than those of deferiprone and deferasirox.
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CAS 201530-41-8 Deferasirox

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