Deferasirox (marketed as Exjade, Desirox, Defrijet, Desifer...) is an iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose.
CAT No: 10-101-115
CAS No:201530-41-8
Synonyms/Alias:4-[3,5-Bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid; CGP-72670; ICL-670; ICL-670A
Chemical Name:4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid
Deferasirox is a tridentate iron chelator belonging to the class of synthetic hydroxypyridinone derivatives, widely recognized for its high affinity and selectivity for ferric ions. As a small-molecule chelating agent, it is structurally designed to coordinate iron(III) efficiently, forming stable complexes that are soluble and readily excretable. Its physicochemical properties and iron-binding capacity make it a valuable tool in biochemical and pharmacological research, particularly in studies involving iron homeostasis, metal-catalyzed oxidative stress, and the molecular mechanisms of chelation. The compound is of significant interest in both fundamental and applied research settings, where precise modulation of iron availability is required to elucidate biological processes or to develop new analytical methodologies.
Iron metabolism research: Deferasirox serves as a robust experimental tool for investigating cellular and systemic iron regulation. By selectively binding ferric ions, it enables researchers to manipulate labile iron pools within in vitro and ex vivo models. This facilitates the study of iron transport, storage, and regulatory pathways, including the activity of proteins such as ferritin, transferrin, and hepcidin. Its use allows for controlled depletion of bioavailable iron, providing insights into the consequences of iron deficiency or overload on gene expression, cell viability, and metabolic flux.
Oxidative stress and redox biology: The chelating activity of deferasirox is instrumental in studies focused on iron-catalyzed oxidative processes. Iron is a key catalyst in Fenton chemistry, generating reactive oxygen species (ROS) that contribute to cellular damage and redox imbalance. Researchers utilize deferasirox to attenuate these reactions in cell culture and biochemical assays, thereby dissecting the specific roles of iron in oxidative stress signaling, mitochondrial dysfunction, and antioxidant defense mechanisms. This application is particularly relevant in models of neurodegeneration, ischemia-reperfusion injury, and other conditions where iron-mediated ROS production is a critical factor.
Analytical chemistry and assay development: In analytical laboratories, deferasirox is employed in the development and validation of iron quantification protocols and chelation assays. Its well-characterized binding kinetics and specificity make it an excellent reference compound for calibrating spectrophotometric or chromatographic methods aimed at detecting free or bound iron in complex biological matrices. Additionally, it can be used to benchmark the performance of novel chelators or to standardize assays measuring iron mobilization and sequestration.
Metal toxicity modeling: The compound is frequently incorporated into experimental systems designed to model metal-induced toxicity, particularly in studies examining the interplay between iron and other transition metals. By modulating iron availability, deferasirox assists in delineating metal-specific toxicological pathways and in evaluating the protective or synergistic effects of chelation. This application supports research into environmental toxicology, metallomics, and the development of metal detoxification strategies.
Drug discovery and screening: Deferasirox is a valuable tool compound in high-throughput screening platforms aimed at identifying new iron chelators or modulators of iron-dependent enzymes. Its defined mechanism of action and favorable pharmacokinetic profile allow it to serve as a positive control or comparator in biochemical screens, cell-based assays, and structure-activity relationship studies. This facilitates the discovery and optimization of next-generation chelating agents for research use, advancing both basic science and translational applications in metal biology.
Iron accumulation is a consequence of regular red cell transfusions, and can occur as a result of ineffective erythropoiesis secondary to increased intestinal iron absorption, in patients with various anemias. Without appropriate treatment, iron overload can lead to increased morbidity and mortality. Deferasirox is an oral iron chelator effective for reduction of body iron in iron-overloaded patients with transfusion-dependent anemias and non-transfusion-dependent thalassemia, with a well-established safety profile. This review summarizes the clinical pharmacokinetics, pharmacodynamics, and drug-drug interaction profile of deferasirox, and the claims supporting once-daily dosing for effective chelation.
Tanaka, C. (2014). Clinical pharmacology of deferasirox. Clinical pharmacokinetics, 53(8), 679-694.
The Thalassemia Clinical Research Network collected adherence information from 79 patients on deferoxamine and 186 on deferasirox from 2007 to 2009. Chelation adherence was defined as percent of doses administered in the last 4 weeks (patient report) out of those prescribed(chart review). Chelation history since 2002 was available for 97 patients currently on deferoxamine and 217 on deferasirox, with crude estimates of adherence from chart review. Self-reported adherence to both deferoxamine and deferasirox were quite high, with slightly higher adherence to the oral chelator (97 vs. 92%). Ninety percent of patients on deferasirox reported at least 90% adherence, compared with 75% of patients on deferoxamine. Adherence to both chelators was highest in children, followed by adolescents and older adults.
Trachtenberg, F., Vichinsky, E., Haines, D., Pakbaz, Z., Mednick, L., Sobota, A., ... & Giardina, P. J. (2011). Iron chelation adherence to deferoxamine and deferasirox in thalassemia. American journal of hematology, 86(5), 433-436.
Thirty-nine children with Fanconi aplastic anemia (FAA) have been followed up in our center between January 2008 and November 2010. Eight of these children (20%) with a transfusional iron overload had been undergoing deferasirox treatment during the study period. In the English literature, transfusional iron overload and the use of an iron chelator in children with FAA has not yet been evaluated. Here, we have presented the effectivity and tolerability of deferasirox in children with FAA and a transfusional iron overload. Before the deferasirox treatment, the mean serum ferritin level was 3377 ± 2200 ng/mL. After a mean 13.6-month treatment duration, the mean ferritin level decreased to 2274 ± 1300 ng/mL (P<0.05). In our series, 3 patients had renal and 3 had hepatic toxicity during the treatment. Two patients had peliosis hepatis and 2 had congenital renal abnormalities before the treatment. There may be differences in the side-effect profiles of deferasirox treatment in patients with FAA. In our series, despite the low number of cases, nephrotoxicity and hepatotoxicity were common side effects instead of gastrointestinal disturbances reported in other studies. Deferasirox is an oral, easily applicable, and effective iron chelator; baseline hepatotoxicity and nephrotoxicity may increase the development of toxic side effects in children with FAA. Patients with FAA receiving deferasirox treatment should be followed up closely for these side effects.
Tunç, B., Tavil, B., Karakurt, N., Yarali, N., Azik, F. M., Kara, A., ... & Ozkasap, S. (2012). Deferasirox therapy in children with Fanconi aplastic anemia. Journal of pediatric hematology/oncology, 34(4), 247-251.
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