Catalog No.S1712 Synonyms: CGP-72670, ICL-670
Molecular Weight(MW): 373.36
Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.
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|Description||Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.|
Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels.  Deferasirox incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples.  Deferasirox inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM.  Deferasirox is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively. 
|In vivo||Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhances the host inflammatory response to mucormycosis. Deferasirox synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B.  Deferasirox administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%.Deferasirox is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. Deferasirox is 99.2% bound to plasma proteins.  Deferasirox monotherapy modestly prolongs survival of mice with IPA. |
-  Ibrahim AS, et al. J Clin Invest, 2007, 117(9), 2649-2657.
-  Messa E, et al. Haematologica, 2010, 95(8), 1308-1316.
-  Ohyashiki JH, et al. Cancer Sci, 2009, 100(5), 970-977.
|In vitro||DMSO||74 mg/mL (198.2 mM)|
|Ethanol||2 mg/mL (5.35 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03920657||Recruiting||Drug: Deferasirox||Myelodysplastic Syndromes||Fondazione Italiana Sindromi Mielodisplastiche Onlus||July 2019||Phase 2|
|NCT02663752||Terminated||Procedure: Bone marrow aspirate|Drug: Deferasirox||Myelodysplastic Syndrome||Novartis Pharmaceuticals|Novartis||May 30 2016||Phase 2|
|NCT02069886||Withdrawn||Drug: deferasirox||Thalassemia (Transfusion Delendent)||Novartis Pharmaceuticals|Novartis||December 2014||Phase 4|
|NCT02038816||Terminated||Drug: Deferasirox + Azacitidine|Drug: Azacitidine||Myelodysplastic Syndromes||Sunnybrook Health Sciences Centre|Novartis||March 2014||Phase 2|
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