| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 2g |
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| Other Sizes |
Purity: =100%
| Targets |
Metabolic Disease
Ferric maltol targets the iron transport and storage pathways in the body. The compound delivers ferric iron (Fe³⁺) in a stable, non-reactive form that is absorbed via the divalent metal transporter 1 (DMT1) in the duodenum. Once absorbed, the iron is released from the maltol complex and bound to transferrin for transport to the bone marrow for erythropoiesis or stored in the liver as ferritin. The maltol ligand acts as a protective agent, preventing the iron from causing oxidative damage and reducing gastrointestinal irritation. |
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| ln Vitro |
Serum ferritin, blood hemoglobin, reticulocyte hemoglobin, serum iron, and serum ferritin levels are all increased when iron maltol is taken [1].
In vitro, Ferric maltol has been studied for its iron uptake and bioavailability. Studies using Caco-2 cell monolayers have shown that ferric maltol is efficiently absorbed via DMT1. The compound's iron is released from the maltol complex at the apical membrane of the intestinal cells and transported into the cells. The maltol ligand itself is not absorbed and is excreted in the feces. The compound's stability and lack of reactivity with dietary components contribute to its improved bioavailability compared to iron(II) salts. |
| ln Vivo |
According to research on animals, unabsorbed iron from iron maltol can at least stay in the small intestine in a chelated form, lowering the possibility of local toxicity and the risk of free iron damaging intestinal mucosa [1].
In vivo, Ferric maltol has demonstrated efficacy in treating iron deficiency anemia in both animal models and human clinical trials. In patients with inflammatory bowel disease, ferric maltol has been shown to increase hemoglobin levels and improve iron stores, with a favorable safety profile. The compound's oral bioavailability and reduced gastrointestinal side effects make it a convenient and well-tolerated option for iron replacement therapy. It is indicated for the treatment of iron deficiency in adults. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to Ferric maltol, as it is an iron supplement rather than a pharmacologically active compound targeting a specific enzyme or receptor. However, its iron uptake and transport can be studied using cell-based assays. Caco-2 cells are grown on Transwell inserts to form a polarized monolayer, and the transport of iron from the apical to the basolateral compartment is measured. The amount of iron transported is quantified using inductively coupled plasma mass spectrometry (ICP-MS) or colorimetric assays.
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| Cell Assay |
In vitro cellular experiments for Ferric maltol involve studying its iron uptake in intestinal epithelial cells. Caco-2 cells are treated with varying concentrations of ferric maltol, and the cellular iron content is measured using ICP-MS or a ferrozine-based colorimetric assay. The expression of iron transporters such as DMT1 and ferroportin is assessed by Western blot or qPCR. The effects of ferric maltol on cellular oxidative stress are also evaluated by measuring reactive oxygen species (ROS) levels.
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| Animal Protocol |
Introduction: Iron deficiency anemia affects up to three quarters of patients with inflammatory bowel disease (IBD). It can significantly impact the quality of life and the ability to work by impairing physical, emotional, and cognitive functioning. The etiology of iron deficiency anemia is multifactorial and oral or intravenous iron replacement is necessary. However, oral iron supplements are often discontinued prematurely due to poor tolerability or insufficient efficacy. Moreover, intravenous supplementation is inconvenient, associated with potentially serious safety risks, and a burden on healthcare resources.[1]
Areas covered: Ferric maltol is a novel ferric iron compound with potential use as an oral therapy for iron deficiency anemia. This overview explains how the molecule’s design impacts clinical outcomes and summarizes available clinical data (ranging from early comparisons with ferrous sulfate to randomized, placebo-controlled, Phase III data in patients with IBD known to be intolerant of oral ferrous products).[1] Expert opinion: Ferric maltol offers the ability to treat iron deficiency anemia in mild-to-moderate IBD without resorting to intravenous therapy, even in those who are intolerant of oral ferrous products. This clinical benefit has the potential to change treatment pathways and increase choice, not only in IBD but also perhaps in many areas beyond gastroenterology. In vivo animal studies for Ferric maltol are conducted using rat or mouse models of iron deficiency anemia. Animals are fed an iron-deficient diet to induce anemia and then treated with ferric maltol via oral gavage. Hemoglobin levels, hematocrit, and serum iron parameters are measured to assess the efficacy of the treatment. The iron content in tissues such as the liver and spleen is also measured. The compound's safety is assessed by monitoring body weight, clinical signs, and histopathological changes in major organs. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Maltol iron dissociates in the gastrointestinal tract, resulting in a time to peak iron concentration (Tmax) of 1.5–3.0 hours. Following a single dose, the mean serum iron concentration in iron-deficient patients increases by 14 ± 6 µmol/L. The bioavailability of a 60 mg dose is approximately 14%. Sixty minutes after injection of radiolabeled maltol iron, 11 ± 2% of the dose is present in the bone marrow, 18 ± 1% in the liver, and 2.6 ± 1% in the urine. The AUC of maltol is 0.022–0.205 hµg/mL, and the AUC of maltol glucuronide is 9.83–30.9 hµg/mL. After oral administration of maltol iron, 39.8–60% is excreted in the urine as a glucuronide conjugate. Iron and maltol iron are not excreted in the urine; unabsorbed maltol iron is excreted in the feces. Data regarding the volume of distribution of ferric maltol are unclear. Data regarding the clearance rate of ferric maltol are unclear. Metabolism/Metabolites In vitro studies have shown that the metabolism of ferric maltol mainly involves UGT1A6-mediated glucuronidation and sulfation of maltol. Biological Half-Life The half-life of maltol is 0.7 hours. Ferric maltol exhibits favorable pharmacokinetic properties following oral administration. The compound is absorbed in the duodenum via DMT1. The iron is released from the maltol complex and bound to transferrin for transport in the circulation. The half-life of iron in the circulation is determined by the body's iron stores and the rate of erythropoiesis. The maltol ligand is not absorbed and is excreted in the feces. The pharmacokinetic profile of ferric maltol supports its once- or twice-daily dosing. |
| Toxicity/Toxicokinetics |
Protein Binding
There is currently no publicly available data regarding the protein binding of maltol iron. The toxicity profile of Ferric maltol is favorable compared to iron(II) salts. Common adverse effects include gastrointestinal symptoms such as nausea, diarrhea, and constipation, but these are less frequent and less severe than with iron(II) salts. The compound's stable iron(III) complex reduces the generation of reactive oxygen species and gastrointestinal irritation. In clinical trials, ferric maltol has been shown to be well-tolerated, with a safety profile comparable to placebo. |
| References |
[1]. Stallmach A, et al. Ferric maltol (ST10): a novel oral iron supplement for the treatment of iron deficiency anemia in inflammatory bowel disease. Expert Opin Pharmacother. 2015;16(18):2859-67.
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| Additional Infomation |
Ferric maltol is a complex of three maltol molecules bound to iron (III) atoms. It has higher bioavailability than ferrous iron and does not deposit in the duodenum as insoluble ferric hydroxide and ferric phosphate. Ferric maltol was described as a potential treatment for iron deficiency in the literature as early as the late 1980s. Ferric maltol was approved by the U.S. Food and Drug Administration (FDA) on July 25, 2019.
See also: Ferric cations (containing the active moiety). Drug Indications Feraccru is indicated for the treatment of iron deficiency in adults. Feraccru is indicated for the treatment of iron deficiency in adults. Treatment of Iron Deficiency Mechanism of Action When ferric maltol dissociates, the iron atoms are provided to an unknown iron absorption mechanism in the ileum and duodenum, possibly β3 integrin or divalent metallotransferrin 1. After entering the bloodstream, the iron binds to transferrin and ferritin. Pharmacodynamics Ferric maltol is used to supplement iron in patients with iron deficiency. It has a broad therapeutic index, and patients typically take 30 mg twice daily, while concentrations of 20 mg/kg may cause toxicity. Patients should be informed of the risks of inflammatory bowel disease flare-ups, iron overload, and accidental ingestion in children. Ferric maltol is an orally active iron(III) complex used to treat iron deficiency anemia, particularly in patients with inflammatory bowel disease. It consists of one iron atom complexed with three maltol molecules, which improves the bioavailability of iron and reduces gastrointestinal side effects compared to iron(II) salts. The compound is marketed under the brand names Accrufer and Feraccru. Ferric maltol has been shown to be effective in increasing hemoglobin levels and improving iron stores in clinical trials. It represents a significant advancement in the treatment of iron deficiency anemia. |
| Molecular Formula |
C₁₈H₁₅FEO₉
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|---|---|
| Molecular Weight |
431.15
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| Exact Mass |
431.006
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| Elemental Analysis |
C, 50.14; H, 3.51; Fe, 12.95; O, 33.40
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| CAS # |
33725-54-1
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| PubChem CID |
169535
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| Appearance |
Typically exists as Purple to purplish red solids at room temperature
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
28
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| Complexity |
200
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.CC1C=CC(C(C(N2CCCCC2)C)=O)=C(C)C=1
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| InChi Key |
AHPWLYJHTFAWKI-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/3C6H6O3.Fe/c3*1-4-6(8)5(7)2-3-9-4;/h3*2-3,8H,1H3;/q;;;+3/p-3
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| Chemical Name |
iron(3+);2-methyl-4-oxopyran-3-olate
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| Synonyms |
Ferric maltol; Iron (III) maltol; ST10; ST 10021; WHO 9974ST-10; ST 10-021ST-10021; WHO-9974ST; 10 ST10-021; ST-10-021; ST10021; WHO9974; Ferric maltol; 33725-54-1; Iron (III) maltol; st10; iron maltol; MA10QYF1Z0; Ferric maltol [INN]; Ferric maltol [USAN];
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~28.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (2.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3194 mL | 11.5969 mL | 23.1938 mL | |
| 5 mM | 0.4639 mL | 2.3194 mL | 4.6388 mL | |
| 10 mM | 0.2319 mL | 1.1597 mL | 2.3194 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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