Ferrous sulfate

Identification

Summary

Ferrous sulfate is an iron supplement used to prevent or treat iron deficiency anemia.

Generic Name
Ferrous sulfate anhydrous
Commonly known or available as Ferrous sulfate
DrugBank Accession Number
DB13257
Background

Iron deficiency anemia is a large public health concern worldwide, especially in young children, infants, and women of childbearing age.4 This type of anemia occurs when iron intake, iron stores, and iron loss do not adequately support the formation of erythrocytes, also known as red blood cells.8

Ferrous sulfate is a synthetic agent used in the treatment of iron deficiency. It is the gold standard of oral iron therapy in the UK and many other countries.14,18

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 151.908
Monoisotopic: 151.886671311
Chemical Formula
FeO4S
Synonyms
  • iron sulfate (1:1)
  • iron(2+) sulfate (anhydrous)
  • iron(II) sulfate

Pharmacology

Indication

Ferrous sulfate is used for the prevention and treatment of iron deficiency anemia in adults and children.4,17,22

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAnaemia folate deficiencyCombination Product in combination with: Folic acid (DB00158)••••••••••••••••••• •••• ••••••
Used in combination to preventAnaemia folate deficiencyCombination Product in combination with: Folic acid (DB00158)••••••••••••••••••• •••• ••••••
Used in combination to preventAnemiaCombination Product in combination with: Folic acid (DB00158)••••••••••••••••••• •••• ••••••
Used in combination to treatAnemiaCombination Product in combination with: Folic acid (DB00158)••••••••••••••••••• •••• ••••••
Used in combination to treatFolate deficiencyCombination Product in combination with: Ascorbic acid (DB00126), Folic acid (DB00158)••••••••••••••••••••••••••••••••• •••••••• •••••••
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Ferrous sulfate replenishes iron, an essential component in hemoglobin, myoglobin, and various enzymes. It replaces the iron that is usually found in hemoglobin and myoglobin. Iron participates in oxygen transport and storage, electron transport and energy metabolism, antioxidant and beneficial pro-oxidant functions, oxygen sensing, tissue proliferation and growth, as well as DNA replication and repair.6,9

Mechanism of action

Iron is required to maintain optimal health, particularly for helping to form red blood cells (RBC) that carry oxygen around the body. A deficiency in iron indicates that the body cannot produce enough normal red blood cells.9,22 Iron deficiency anemia occurs when body stores of iron decrease to very low levels, and the stored iron is insufficient to support normal red blood cell (RBC) production. Insufficient dietary iron, impaired iron absorption, bleeding, pregnancy, or loss of iron through the urine can lead to iron deficiency.9,24 Symptoms of iron deficiency anemia include fatigue, breathlessness, palpitations, dizziness, and headache.

Taking iron in supplement form, such as ferrous sulfate, allows for more rapid increases in iron levels when dietary supply and stores are not sufficient.12 Iron is transported by the divalent metal transporter 1 (DMT1) across the endolysosomal membrane to enter the macrophage. It can then can be incorporated into ferritin and be stored in the macrophage or carried of the macrophage by ferroportin. This exported iron is oxidized by the enzyme to ceruloplasmin to Fe3+, followed by sequestration by transferrin for transport in the serum to various sites, including the bone marrow for hemoglobin synthesis or into the liver.6 Iron combines with porphyrin and globin chains to form hemoglobin, which is critical for oxygen delivery from the lungs to other tissues.19

TargetActionsOrganism
AHemoglobin subunit alpha
binder
Humans
ATransferrin receptor
substrate
Humans
Absorption

Approximately 5 – 10% of dietary iron is absorbed, and this absorption rate increases to up to 30% in iron deficiency states. Oral iron supplements are absorbed up to 60% via active and passive transport processes.17 Gastrointestinal absorption of iron occurs via strict regulation by the enterocyte and duodenal cytochrome and ferric reductase enzymes.6,24 The hormone hepcidin heavily regulates iron absorption and distribution throughout the body.22

The median time to maximum serum concentration (Tmax) is generally 4 hours after administration. Between 2-8 hours post administration, average serum iron concentrations fluctuate by 20%, according to one study.1 Bioavailability of iron depends on whether it is administered in a film coated tablet or enteric coated tablet. One pharmacokinetic study in healthy volunteers revealed a 30% bioavailability for enteric coated tablets. The AUC of enteric coated tablets varied between a lower limit of -46.93 to 5.25 µmolxh/l. Cmax is higher for film coated tablets, ranging from 3.4 to 22.1 µmol/h/l.10

It is advisable to take ferrous sulfate with ascorbic acid, as this practice may increase absorption.22,24 Avoid antacids, tea, coffee,tea, dairy products, eggs, and whole-grain bread for at least an hour after taking ferrous sulfate. Calcium can decrease iron absorption by 33% if taken concomitantly.17

Volume of distribution

About 60% of iron is distributed the erythrocytes.6 The remainder of the iron is found in muscle tissues (as a part of myoglobin), and in a variety of different enzymes, as well as in storage form. Most stored iron is in the form of ferritin, which can be found in the liver, bone marrow, spleen and, and muscle. Iron crosses the placenta and is also found in breast milk.17

Protein binding

The protein binding for ferrous sulfate is equal to or greater than 90%.17 It is bound to transferrin and ferritin, ferroportin, myoglobin, and other enzymes.22,24 Approximately 60% of iron is located in the erythrocytes as part of hemoglobin.6

Metabolism

The metabolism of iron is complex. Normally, iron exists in the ferrous (Fe2+) or ferric (Fe3+) state, but since Fe2+ is oxidized to Fe3+, which hydrolyzes to insoluble iron(III)hydroxides in neutral aqueous solutions, iron binds to plasma proteins and is either transported or stored throughout the body.6

There are three proteins that serve to regulate the storage and transport of ingested iron. The first protein , transferrin, transports iron in both the plasma and extracellular fluid. Ceruloplasmin in the plasma and hephaestin on the enterocyte participate in the oxidation and binding of iron to transferrin. The main role of transferrin is the chelation of iron to prevent the production of reactive oxygen species, while facilitating its transport into cells.24 The transferrin receptor, located on many cells that require iron, binds the transferrin complex and internalizes this complex. Ferritin is a protein that stores iron, making it readily available for body requirements.6

Route of elimination

Oral iron is recycled, with some loss in the urine, sweat, and desquamation. Some iron can be lost during menstrual bleeding9,17 This loss is balanced by changes in intestinal absorption. The enzyme hepcidin promotes the excretion of iron via the sloughing of enterocytes with ferritin stores into the feces.24

Half-life

The half-life of orally administered iron is not readily available in the literature, with total effects lasting 2-4 months (congruent with the red blood cell life span)11 with an onset of action of 4 days and peak activity at 7-10 days.17

Clearance

Not Available

Adverse Effects
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Toxicity

The toxicity of ferrous sulfate in humans depends on the amount of iron ingested. Up to 20 mg/kg of elemental iron is not toxic, 20-60 mg/kg has mild toxicity, and more than 60 mg/kg can lead to severe symptoms and morbidity.13

Overdose information

Iron containing products are the primary cause of drug overdose in children under 6 years of age.20 Iron is toxic to the gastrointestinal system, cardiovascular system, in addition to central nervous system. The most early reported effects following the excess ingestion of iron include nausea, flatulence, abdominal pain, diarrhea, constipation, and black/tarry stools.14 Symptoms of overdose in the later stages include bluish lips, fingernails, and palms, drowsiness, tachycardia, seizures, metabolic acidosis, hepatic injury, and cardiovascular dysfunction. Sequelae of iron sulfate overdose include intestinal obstruction, pyloric stenosis, and gastric scarring.17 If the patient is comatose or seizing, gastric lavage with sodium bicarbonate should be performed. Deferoxamine is the antidote for iron poisoning. Other supportive treatments to support fluid and electrolyte balance and correct metabolic acidosis are also advised.17 Hospitalization should continue for 24 h after the patient becomes asymptomatic to monitor for delayed onset of shock/gastrointestinal bleeding.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Alendronic acidFerrous sulfate anhydrous can cause a decrease in the absorption of Alendronic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlmasilateAlmasilate can cause a decrease in the absorption of Ferrous sulfate anhydrous resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphateAluminium phosphate can cause a decrease in the absorption of Ferrous sulfate anhydrous resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Ferrous sulfate anhydrous resulting in a reduced serum concentration and potentially a decrease in efficacy.
AsenapineAsenapine can cause a decrease in the absorption of Ferrous sulfate anhydrous resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
  • Avoid milk and dairy products. Take ferrous sulfate at least 2 hours before or after milk.
  • Limit caffeine intake. Food and beverages containing caffeine may reduce iron absorption.
  • Take at least 2 hours before or after calcium supplements.
  • Take separate from antacids. Take ferrous sulfate at least 2 hours before or after antacids.
  • Take with food. This may reduce gastric irritation.
  • Take with foods containing vitamin C. Foods rich in vitamin C increase the absorption of iron.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Ferrous sulfate39R4TAN1VT7782-63-0SURQXAFEQWPFPV-UHFFFAOYSA-L
Ferrous sulfate dihydrateG0Z544944910028-21-4KFJBRJOPXNCARV-UHFFFAOYSA-L
Ferrous sulfate monohydrateRIB00980VW17375-41-6XBDUTCVQJHJTQZ-UHFFFAOYSA-L
Ferrous sulfate sesquihydrate1OA214846O13463-43-9JJUUPAANEJLKEY-UHFFFAOYSA-J
Active Moieties
NameKindUNIICASInChI Key
IronunknownE1UOL152H77439-89-6XEEYBQQBJWHFJM-UHFFFAOYSA-N
Ferrous cationionicGW89581OWR15438-31-0CWYNVVGOOAEACU-UHFFFAOYSA-N
Product Images
International/Other Brands
Anemifer / Aritoferon / Bioron / Blissferon / Caron / Dyaferon / Fe-Plus / Feklon / Feromin / Ferrifol / Ferrocebrina Solucion / Ferrogeme / Ferroglobin / Ferrograd / Ferrolin / Ferrosi / Ferrosi sulfas / Ferrous Sulfate Washington Pharm / Ferrous Sulfate-Minsheng Pharm / Fertonic / Fesyrup / Hierro Fabra / Hierro Richet / Hierro Vannier / Iberol / Inshel / Iron-200 / Jeferin / Kdiron / Kidiron / Pediafer Goutt / Pharmafer / Rhea Ferrous Sulfate / Sulfas Ferrosus / Sulfato Ferroso / Sulfato Ferroso Ecar / Sulfato Ferroso Kronos / Sulfato Ferroso L.Ch. / Sulfato Ferroso Richet / Sulfato Ferroso Sant Gall Friburg / Sulfato Ferroso Valma / TGI / Tibilin / United Home Fersulfate Iron / Valdefer / Vitafer-Fol
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ferrous SulfateTablet65 mg/1OralHealthlife of Usa2017-12-05Not applicableUS flag
Ferrous SulfateTablet65 mg/1OralBoca Pharmacal, Inc.2010-09-142018-06-30US flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ferinsol DropsSolution / drops125 mg / mLOralMead Johnson Nutritionals1951-12-311996-09-30Canada flag
Fero Grad FilmtabTablet, extended release105 mgOralAbbott1961-12-312008-06-06Canada flag
Ferrous SulfateElixir220 mg/5mLOralRij Pharmaceutical Corporation1999-03-16Not applicableUS flag
Ferrous SulfateTablet325 mg/1OralPreferred Pharmaceuticals, Inc.2004-06-182019-09-18US flag
Ferrous SulfateTablet325 mg/1OralA-S Medication Solutions2001-02-19Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Aktiferrin - SaftFerrous sulfate (3.42 g/100ml) + Serine (2.58 g/100ml)SyrupOralTeva B.V.1978-02-13Not applicableAustria flag
Aktiferrin - TropfenFerrous sulfate (1.416 g/30ml) + Serine (1.068 g/30ml)Solution / dropsOralTeva B.V.1978-02-13Not applicableAustria flag
FERBEAPLEX TABLETSFerrous sulfate anhydrous (200 mg) + Nicotinamide (10 mg) + Riboflavin (1.5 mg) + Thiamine hydrochloride (3 mg)Tablet, sugar coatedOralBEACONS PHARMACEUTICALS PTE. LTD.1991-02-19Not applicableSingapore flag
Fero Grad 500Ferrous sulfate (105 mg) + Ascorbic acid (500 mg)Tablet, extended releaseOralAbbott1961-12-311999-08-09Canada flag
FEROCOM TABLETSFerrous sulfate (180 mg) + Folic acid (5 mg) + Nicotinamide (10 mg) + Riboflavin (1.5 mg) + Thiamine (3 mg)Tablet, coatedOralSUNWARD PHARMACEUTICAL SDN. BHD.2020-09-08Not applicableMalaysia flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AbaviteFerrous sulfate (30 mg/1) + Ascorbic acid (60 mg/1) + Cholecalciferol (0.025 mg/1) + DL-alpha tocopheryl acetate (13.5 mg/1) + Folic acid (1 mg/1) + Magnesium oxide (25 mg/1) + Mecobalamin (0.5 mg/1) + Niacin (15 mg/1) + Calcium pantothenate (5 mg/1) + Potassium Iodide (0.25 mg/1) + Riboflavin (1.8 mg/1) + Thiamine mononitrate (1.6 mg/1) + Vitamin A palmitate (0.33 mg/1) + Zinc oxide (15 mg/1)TabletOralABACOS HEALTH2021-03-31Not applicableUS flag
Exact-Rx SODIUM SULFACETAMIDE and SULFER 10%/5% CleanserFerrous sulfate (50 mg/1g) + Sulfacetamide sodium (100 mg/1g)LotionTopicalExact Rx, Inc.2011-08-012017-04-20US flag
Ferrous SulfateFerrous sulfate (220 mg/5mL)ElixirOralRij Pharmaceutical Corporation1999-03-16Not applicableUS flag
Ferrous SulfateFerrous sulfate (325 mg/1)Tablet, film coatedOralCentral Texas Community Health Centers2014-07-01Not applicableUS flag
Ferrous SulfateFerrous sulfate (325 mg/1)TabletOralQualitest2001-02-192020-03-30US flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of inorganic compounds known as transition metal sulfates. These are inorganic compounds in which the largest oxoanion is sulfate, and in which the heaviest atom not in an oxoanion is a transition metal.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Transition metal oxoanionic compounds
Sub Class
Transition metal sulfates
Direct Parent
Transition metal sulfates
Alternative Parents
Inorganic salts / Inorganic oxides
Substituents
Inorganic oxide / Inorganic salt / Transition metal sulfate
Molecular Framework
Not Available
External Descriptors
metal sulfate, iron molecular entity (CHEBI:75832)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
2IDP3X9OUD
CAS number
7720-78-7
InChI Key
BAUYGSIQEAFULO-UHFFFAOYSA-L
InChI
InChI=1S/Fe.H2O4S/c;1-5(2,3)4/h;(H2,1,2,3,4)/q+2;/p-2
IUPAC Name
lambda2-iron(2+) sulfate
SMILES
[Fe++].[O-]S([O-])(=O)=O

References

Synthesis Reference

Mitchell AG. The preparation and characterization of ferrous sulphate hydrates. (1984 Aug).J Pharm Pharmacol.

General References
  1. Leary A, Barthe L, Clavel T, Sanchez C, Oulmi-Castel M, Paillard B, Edmond JM, Brunner V: Pharmacokinetics of Ferrous Sulphate (Tardyferon(R)) after Single Oral Dose Administration in Women with Iron Deficiency Anaemia. Drug Res (Stuttg). 2016 Jan;66(1):51-6. doi: 10.1055/s-0035-1549934. Epub 2015 May 19. [Article]
  2. Conrad ME, Umbreit JN, Moore EG, Hainsworth LN, Porubcin M, Simovich MJ, Nakada MT, Dolan K, Garrick MD: Separate pathways for cellular uptake of ferric and ferrous iron. Am J Physiol Gastrointest Liver Physiol. 2000 Oct;279(4):G767-74. doi: 10.1152/ajpgi.2000.279.4.G767. [Article]
  3. Tolkien Z, Stecher L, Mander AP, Pereira DI, Powell JJ: Ferrous sulfate supplementation causes significant gastrointestinal side-effects in adults: a systematic review and meta-analysis. PLoS One. 2015 Feb 20;10(2):e0117383. doi: 10.1371/journal.pone.0117383. eCollection 2015. [Article]
  4. Santiago P: Ferrous versus ferric oral iron formulations for the treatment of iron deficiency: a clinical overview. ScientificWorldJournal. 2012;2012:846824. doi: 10.1100/2012/846824. Epub 2012 May 2. [Article]
  5. Waldvogel-Abramowski S, Waeber G, Gassner C, Buser A, Frey BM, Favrat B, Tissot JD: Physiology of iron metabolism. Transfus Med Hemother. 2014 Jun;41(3):213-21. doi: 10.1159/000362888. Epub 2014 May 12. [Article]
  6. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  7. Cancado RD, Munoz M: Intravenous iron therapy: how far have we come? Rev Bras Hematol Hemoter. 2011;33(6):461-9. doi: 10.5581/1516-8484.20110123. [Article]
  8. Miller JL: Iron deficiency anemia: a common and curable disease. Cold Spring Harb Perspect Med. 2013 Jul 1;3(7). pii: cshperspect.a011866. doi: 10.1101/cshperspect.a011866. [Article]
  9. Abbaspour N, Hurrell R, Kelishadi R: Review on iron and its importance for human health. J Res Med Sci. 2014 Feb;19(2):164-74. [Article]
  10. Walker SE, Paton TW, Cowan DH, Manuel MA, Dranitsaris G: Bioavailability of iron in oral ferrous sulfate preparations in healthy volunteers. CMAJ. 1989 Sep 15;141(6):543-7. [Article]
  11. Kaestner L, Bogdanova A: Regulation of red cell life-span, erythropoiesis, senescence, and clearance. Front Physiol. 2014 Jul 18;5:269. doi: 10.3389/fphys.2014.00269. eCollection 2014. [Article]
  12. FERROUS SULFATE - National Library of Medicine HSDB Database - Toxnet [Link]
  13. Iron poisoning [Link]
  14. Ferrous Sulfate Supplementation Causes Significant Gastrointestinal Side-Effects in Adults: A Systematic Review and Meta-Analysis [Link]
  15. Ferrous sulfate, Daily Med [Link]
  16. Ferrous sulfate, epocrates [Link]
  17. Ferrous sulfate DavisPlus [Link]
  18. Ferrous Sulfate Tablet, Delayed Release (Enteric Coated) [Link]
  19. Antianemia Drugs [Link]
  20. Dailymed: Ferrous sulfate tablets [Link]
  21. The Science Company: Ferrous sulfate MSDS [Link]
  22. ODS Health Professional Fact Sheet: Iron [Link]
  23. Medicines UK: Ferrous sulfate 200mg oral tablets [Link]
  24. NIH Statpearls: Biochemistry, Iron Absorption [Link]
PubChem Compound
62662
PubChem Substance
347829289
ChemSpider
22804
ChEBI
75832
ChEMBL
CHEMBL1200830
Wikipedia
Iron(II)_sulfate

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherAbnormal Uterine Bleeding / Iron Deficiency Anemia (IDA) / Menstrual Bleeding, Heavy1
4CompletedTreatmentAnemia1
4CompletedTreatmentAnemia / Colorectal Neoplasms1
4CompletedTreatmentCrohn's Disease (CD) / Ulcerative Colitis1
4CompletedTreatmentDelivery Complications / Iron Deficiency Anemia (IDA)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SyrupOral
Tablet, film coatedOral100 mg/1
LotionTopical
SolutionOral15 mg/1mL
Tablet, sugar coatedOral200 mg
Solution / dropsOral125 mg / mL
Tablet, coatedOral0.34 g
Tablet, extended releaseOral105 mg
Tablet, coatedOral
Syrup
Tablet, film coatedOral105 mg
Tablet, extended releaseOral
Tablet, extended releaseOral329.7 mg
SolutionOral25 mg
TabletOral
ElixirOral220 mg/5mL
TabletOral
TabletOral324 mg/1
TabletOral325 mg/1
TabletOral65 mg/1
Tablet, coatedOral325 mg/1
Tablet, film coatedOral325 mg/1
Tablet, film coatedOral65 mg/1
Tablet, delayed releaseOral65 mg/1
Tablet, coatedOral65 mg/1
TabletOral325 mg
TabletOral35 mg
Capsule, delayed releaseOral
Capsule, extended releaseOral30 mg
Tablet, coatedOral150 mcg
Tablet, extended releaseOral35 mg / srt
Tablet, extended releaseOral50 mg
PowderOral
Tablet, effervescentOral
Capsule, liquid filledOral
Liquid; tabletOral
LiquidOral
SolutionOral
Tablet, delayed releaseOral300 mg
TabletOral300 mg
LiquidOral220 mg/5mL
CapsuleOral
Suspension / dropsOral
Tablet, coatedOral
Tablet, delayed releaseOral60 mg
Tablet, coatedOral100 mg
SyrupOral4 g
Tablet, coatedOral300 mg
Tablet, extended releaseOral80 MG
Tablet, extended releaseOral247.25 mg
Tablet, film coatedOral247.25 mg
Tablet, film coatedOral
Solution / dropsOral
SolutionOral125.000 mg
TabletOral200.00 mg
SyrupOral60 mg/5ml
Tablet, coatedOral163 mg
SyrupOral125 mg/5ml
Tablet, sugar coatedOral200 mg
Tablet, coatedOral200 mg
Tablet, sugar coatedOral
Tablet, sugar coatedOral165 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)64https://www.chemicalbook.com/ProductChemicalPropertiesCB9232125_EN.htm
boiling point (°C)> 300 °CMSDS
water solubility25.6 g/100 mLhttps://www.chemicalbook.com/ProductChemicalPropertiesCB9232125_EN.htm
logP-0.84http://foodb.ca/compounds/FDB014740
pKa-3http://foodb.ca/compounds/FDB014740
Predicted Properties
PropertyValueSource
logP-0.84Chemaxon
pKa (Strongest Acidic)-3Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area80.26 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity11.53 m3·mol-1Chemaxon
Polarizability5.81 Å3Chemaxon
Number of Rings0Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Oxygen transporter activity
Specific Function
Involved in oxygen transport from the lung to the various peripheral tissues.
Gene Name
HBA1
Uniprot ID
P69905
Uniprot Name
Hemoglobin subunit alpha
Molecular Weight
15257.405 Da
References
  1. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  2. Johnson-Wimbley TD, Graham DY: Diagnosis and management of iron deficiency anemia in the 21st century. Therap Adv Gastroenterol. 2011 May;4(3):177-84. doi: 10.1177/1756283X11398736. [Article]
  3. Alleyne M, Horne MK, Miller JL: Individualized treatment for iron-deficiency anemia in adults. Am J Med. 2008 Nov;121(11):943-8. doi: 10.1016/j.amjmed.2008.07.012. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
General Function
Virus receptor activity
Specific Function
Cellular uptake of iron occurs via receptor-mediated endocytosis of ligand-occupied transferrin receptor into specialized endosomes. Endosomal acidification leads to iron release. The apotransferri...

Components:
References
  1. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  2. Johnson-Wimbley TD, Graham DY: Diagnosis and management of iron deficiency anemia in the 21st century. Therap Adv Gastroenterol. 2011 May;4(3):177-84. doi: 10.1177/1756283X11398736. [Article]
  3. Alleyne M, Horne MK, Miller JL: Individualized treatment for iron-deficiency anemia in adults. Am J Med. 2008 Nov;121(11):943-8. doi: 10.1016/j.amjmed.2008.07.012. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Ferroxidase activity
Specific Function
Ceruloplasmin is a blue, copper-binding (6-7 atoms per molecule) glycoprotein. It has ferroxidase activity oxidizing Fe(2+) to Fe(3+) without releasing radical oxygen species. It is involved in iro...
Gene Name
CP
Uniprot ID
P00450
Uniprot Name
Ceruloplasmin
Molecular Weight
122204.45 Da
References
  1. Sozmen EY, Kavakli K, Cetinkaya B, Akcay YD, Yilmaz D, Aydinok Y: Effects of iron(II) salts and iron(III) complexes on trace element status in children with iron-deficiency anemia. Biol Trace Elem Res. 2003 Jul;94(1):79-86. doi: 10.1385/BTER:94:1:79. [Article]
  2. Frieden E, Hsieh HS: Ceruloplasmin: the copper transport protein with essential oxidase activity. Adv Enzymol Relat Areas Mol Biol. 1976;44:187-236. doi: 10.1002/9780470122891.ch6. [Article]
  3. The Pharmacokinetics and Pharmacodynamics of Iron Preparations [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Liver-produced hormone that constitutes the main circulating regulator of iron absorption and distribution across tissues. Acts by promoting endocytosis and degradation of ferroportin, leading to the retention of iron in iron-exporting cells and decreased flow of iron into plasma. Controls the major flows of iron into plasma: absorption of dietary iron in the intestine, recycling of iron by macrophages, which phagocytose old erythrocytes and other cells, and mobilization of stored iron from hepatocytes (PubMed:22306005).
Specific Function
Hormone activity
Gene Name
HAMP
Uniprot ID
P81172
Uniprot Name
Hepcidin
Molecular Weight
9408.075 Da
References
  1. Zimmermann MB, Troesch B, Biebinger R, Egli I, Zeder C, Hurrell RF: Plasma hepcidin is a modest predictor of dietary iron bioavailability in humans, whereas oral iron loading, measured by stable-isotope appearance curves, increases plasma hepcidin. Am J Clin Nutr. 2009 Nov;90(5):1280-7. doi: 10.3945/ajcn.2009.28129. Epub 2009 Sep 9. [Article]
  2. Hwang SI, Lee YY, Park JO, Norton HJ, Clemens E, Schrum LW, Bonkovsky HL: Effects of a single dose of oral iron on hepcidin concentrations in human urine and serum analyzed by a robust LC-MS/MS method. Clin Chim Acta. 2011 Nov 20;412(23-24):2241-7. doi: 10.1016/j.cca.2011.08.014. Epub 2011 Aug 16. [Article]
  3. NIH Statpearls: Biochemistry, Iron Absorption [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Transferrin receptor binding
Specific Function
Transferrins are iron binding transport proteins which can bind two Fe(3+) ions in association with the binding of an anion, usually bicarbonate. It is responsible for the transport of iron from si...
Gene Name
TF
Uniprot ID
P02787
Uniprot Name
Serotransferrin
Molecular Weight
77063.195 Da
References
  1. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  2. Abbaspour N, Hurrell R, Kelishadi R: Review on iron and its importance for human health. J Res Med Sci. 2014 Feb;19(2):164-74. [Article]
  3. NIH Statpearls: Biochemistry, Iron Absorption [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Ferroxidase activity
Specific Function
May function as a ferroxidase for ferrous (II) to ferric ion (III) conversion and may be involved in copper transport and homeostasis. Implicated in iron homeostasis and may mediate iron efflux ass...
Gene Name
HEPH
Uniprot ID
Q9BQS7
Uniprot Name
Hephaestin
Molecular Weight
130447.755 Da
References
  1. Anderson GJ, Frazer DM: Current understanding of iron homeostasis. Am J Clin Nutr. 2017 Dec;106(Suppl 6):1559S-1566S. doi: 10.3945/ajcn.117.155804. Epub 2017 Oct 25. [Article]
  2. Lonnerdal B: Calcium and iron absorption--mechanisms and public health relevance. Int J Vitam Nutr Res. 2010 Oct;80(4-5):293-9. doi: 10.1024/0300-9831/a000036. [Article]
  3. NIH Statpearls: Biochemistry, Iron Absorption [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Ferric-chelate reductase that reduces Fe(3+) to Fe(2+). Present at the brush border of duodenal enterocytes where it probably reduces dietary Fe(3+) thereby facilitating its transport into the mucosal cells. Uses ascorbate as electron donor. May be involved in extracellular ascorbate recycling in erythrocyte membranes. May also act as a ferrireductase in airway epithelial cells.
Specific Function
Ferric-chelate reductase activity
Gene Name
CYBRD1
Uniprot ID
Q53TN4
Uniprot Name
Cytochrome b reductase 1
Molecular Weight
31641.005 Da
References
  1. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  2. NIH Statpearls: Biochemistry, Iron Absorption [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion transmembrane transporter activity
Specific Function
Important in metal transport, in particular iron. Can also transport manganese, cobalt, cadmium, nickel, vanadium and lead. Involved in apical iron uptake into duodenal enterocytes. Involved in iro...
Gene Name
SLC11A2
Uniprot ID
P49281
Uniprot Name
Natural resistance-associated macrophage protein 2
Molecular Weight
62265.195 Da
References
  1. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  2. Wolff NA, Garrick MD, Zhao L, Garrick LM, Ghio AJ, Thevenod F: A role for divalent metal transporter (DMT1) in mitochondrial uptake of iron and manganese. Sci Rep. 2018 Jan 9;8(1):211. doi: 10.1038/s41598-017-18584-4. [Article]
  3. Zoller H, Koch RO, Theurl I, Obrist P, Pietrangelo A, Montosi G, Haile DJ, Vogel W, Weiss G: Expression of the duodenal iron transporters divalent-metal transporter 1 and ferroportin 1 in iron deficiency and iron overload. Gastroenterology. 2001 May;120(6):1412-9. doi: 10.1053/gast.2001.24033. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
May be involved in iron export from duodenal epithelial cell and also in transfer of iron between maternal and fetal circulation. Mediates iron efflux in the presence of a ferroxidase (hephaestin and/or ceruloplasmin).
Specific Function
Ferrous iron transmembrane transporter activity
Gene Name
SLC40A1
Uniprot ID
Q9NP59
Uniprot Name
Solute carrier family 40 member 1
Molecular Weight
62541.55 Da
References
  1. Zoller H, Koch RO, Theurl I, Obrist P, Pietrangelo A, Montosi G, Haile DJ, Vogel W, Weiss G: Expression of the duodenal iron transporters divalent-metal transporter 1 and ferroportin 1 in iron deficiency and iron overload. Gastroenterology. 2001 May;120(6):1412-9. doi: 10.1053/gast.2001.24033. [Article]
  2. Abbaspour N, Hurrell R, Kelishadi R: Review on iron and its importance for human health. J Res Med Sci. 2014 Feb;19(2):164-74. [Article]
  3. NIH Statpearls: Biochemistry, Iron Absorption [Link]

Drug created at June 23, 2017 20:38 / Updated at April 19, 2024 20:55