Iron sucrose

Identification

Summary

Iron sucrose is an compound used as a source of iron in patients with iron deficiency anemia associated with chronic kidney disease (CKD).

Brand Names
Velphoro, Venofer
Generic Name
Iron sucrose
DrugBank Accession Number
DB09146
Background

Iron sucrose (sucroferric oxyhydroxide or iron saccharate) is used as a source of iron in patients with iron deficiency anemia with chronic kidney disease (CKD), including those who are undergoing dialysis (hemodialysis or peritoneal) and those who do not require dialysis. Due to less side effects than iron dextran, iron sucrose is more preferred in chronic kidney disease patients.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 866.546
Monoisotopic: 866.764181
Chemical Formula
C12H29Fe5Na2O23
Synonyms
  • Ferric hydroxide sucrose complex
  • Iron oxide saccharated
  • Iron saccharate
  • Iron sucrose
  • Iron sucrose complex
  • Iron sugar
  • Iron(III) hydroxide sucrose complex
  • Saccharated ferric oxide
  • Saccharated iron
  • Saccharated iron oxide
  • Sucroferric oxyhydroxide
External IDs
  • XI 921

Pharmacology

Indication

Iron sucrose is elemental iron as an injection. It replenishes body iron stores in patients with iron deficiency.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Significant increases in serum iron and serum ferritin and significant decreases in total iron binding capacity occurred four weeks from the initiation of iron sucrose treatment.

Mechanism of action

Following intravenous administration, iron sucrose is dissociated into iron and sucrose and the iron is transported as a complex with transferrin to target cells including erythroid precursor cells. The iron is then incorporated into hemoglobin as the cells mature into red blood cells.

Absorption

The intravensously administered iron sucrose injection would result rapidly in high serum iron levels. Maximum measured levels occured after 10 min of injection with an average of 30.00 mg/l.

Volume of distribution

Vd is 7.3 L

Protein binding

It binds with transferrin.

Metabolism

Following IV administration, dissociated into iron and sucrose by the reticuloendothelial system.

Route of elimination

Renal elimination of iron contributed very little to the total elimination (in average less than 5%). While, renal elimination of sucrose accounts for 68-75% of the administered dose after 4 and 24 hours respectively.

Half-life

6 hours.

Clearance

Total body clearance is 20.5 ml/min.

Adverse Effects
Adverseeffects
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Toxicity

Hypersensitivity reactions, including anaphylactic shock, loss of consciousness, collapse, hypotension, dyspnea, and seizure. Monitor iron toxicity through the periodic evaluation of lab works which monitor the body concentration of iron. Lab monitoring of the following parameters: transferrin saturation, serum ferritin concentrations, hemoglobin, and hematocrit could be helpful to avoid iron overload. Severe allergic symptoms include: rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); burning or pain at the injection site; burning, numbness, or tingling; chest pain; fainting; loss of consciousness; severe or persistent dizziness, headache, or light-headedness; seizures; shortness of breath; swelling of the hands, ankles, or feet.

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
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be decreased when it is combined with Iron sucrose.
Alendronic acidIron sucrose 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 Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphateAluminium phosphate can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
AsenapineAsenapine can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium PhosphateIron sucrose can cause a decrease in the absorption of Calcium Phosphate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium phosphate dihydrateIron sucrose can cause a decrease in the absorption of Calcium phosphate dihydrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
CarbidopaIron sucrose can cause a decrease in the absorption of Carbidopa resulting in a reduced serum concentration and potentially a decrease in efficacy.
Interactions
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Food Interactions
  • Take with food. Take with meals to maximize phosphate binding capacity and reduce phosphate absorption.

Products

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Active Moieties
NameKindUNIICASInChI Key
IronunknownE1UOL152H77439-89-6XEEYBQQBJWHFJM-UHFFFAOYSA-N
Ferric cationionic91O4LML61120074-52-6VTLYFUHAOXGGBS-UHFFFAOYSA-N
Product Images
International/Other Brands
Colliron IV / Encifer / Fe-back / Feojectin / Ferijet / Ferosoft S / Ferplex SS / Ferrivenin
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
VelphoroTablet, chewable500 mg/1OralFresenius Medical Care North America2013-11-27Not applicableUS flag
VelphoroTablet, chewable500 mgOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VelphoroTablet, chewable500 mgOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VelphoroTablet, chewable500 mgOralVifor Fresenius Medical Care Renal Pharma Ltd2019-11-20Not applicableCanada flag
VelphoroTablet, chewable500 mgOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VelphoroTablet125 mgOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VelphoroTablet, chewable500 mgOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VenoferInjection, solution20 mg/1mLIntravenousA-S Medication Solutions2000-11-10Not applicableUS flag
VenoferInjection, solution20 mg/1mLIntravenousAMERICAN REGENT, INC.2007-06-12Not applicableUS flag
VenoferInjection, solution20 mg/1mLIntravenousFresenius Medical Care Holdings, Inc.2008-11-04Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Myferon 150Capsule150 mg/1OralMartin Ekwealor Pharmaceuticals, Inc.1996-12-01Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Bal-Care DHAIron sucrose (1.35 mg/1) + Ascorbic acid (120 mg/1) + Beta carotene (2850 [iU]/1) + Calcium carbonate (219 mg/1) + Cholecalciferol (840 [iU]/1) + Cupric oxide (2 mg/1) + Cyanocobalamin (.012 mg/1) + DL-alpha tocopheryl acetate (3 mg/1) + Folic acid (1 mg/1) + Iodine (.223 mg/1) + Magnesium oxide (25 mg/1) + Nicotinamide (20 mg/1) + Omega-3 fatty acids (430 mg/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (4 mg/1) + Sodium feredetate (25.65 mg/1) + Thiamine mononitrate (1.8 mg/1) + Zinc oxide (25 mg/1)KitOralPru Gen Pharmaceuticals2012-05-01Not applicableUS flag
Bal-Care DHA EssentialIron sucrose (1.35 mg/1) + Ascorbic acid (120 mg/1) + Beta carotene (2850 [iU]/1) + Calcium carbonate (219 mg/1) + Cholecalciferol (840 [iU]/1) + Cupric oxide (2 mg/1) + Cyanocobalamin (.012 mg/1) + DL-alpha tocopheryl acetate (3 mg/1) + Folic acid (1 mg/1) + Iodine (.223 mg/1) + Magnesium oxide (25 mg/1) + Nicotinamide (20 mg/1) + Omega-3 fatty acids (374 mg/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (4 mg/1) + Sodium feredetate (25.65 mg/1) + Thiamine mononitrate (1.8 mg/1) + Zinc oxide (25 mg/1)KitOralPru Gen Pharmaceuticals2012-05-01Not applicableUS flag
Choice OB DHAIron sucrose (29 mg/1) + Ascorbic acid (60 mg/1) + Beta carotene (1700 [iU]/1) + Cholecalciferol (400 [iU]/1) + Cyanocobalamin (5 ug/1) + DL-alpha tocopheryl acetate (30 [iU]/1) + Doconexent (250 mg/1) + Folic acid (1 mg/1) + Magnesium oxide (25 mg/1) + Nicotinamide (15 ug/1) + Pyridoxine hydrochloride (2.5 mg/1) + Riboflavin (1.8 mg/1) + Thiamine mononitrate (1.6 mg/1) + Zinc oxide (15 mg/1)KitOralAcella Pharmaceuticals, LLC2013-05-172015-07-31US flag42192 035320210515 23896 1iunez7
DEMROSE 100 MG/5 ML IV ENJEKSIYON VE INFUZYON ICIN KONSANTRE COZELTI ICEREN AMPUL, 5 ADETIron sucrose (100 mg/5ml)SolutionIntravenousPHARMADA İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
HemeNatal OBIron sucrose (28 mg/1) + Biotin (30 ug/1) + Cholecalciferol (400 [iU]/1) + Cupric sulfate pentahydrate (0.8 mg/1) + Cyanocobalamin (12 ug/1) + Folic acid (1 mg/1) + Heme iron polypeptide (6 mg/1) + Nicotinamide (17 mg/1) + Calcium pantothenate (10 mg/1) + Potassium Iodide (250 ug/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (1.6 mg/1) + Sodium selenate (65 ug/1) + Thiamine mononitrate (1.5 mg/1) + Zinc oxide (4.5 mg/1) + alpha-Tocopherol succinate (10 [iU]/1)TabletOralWh Nutritionals, Llc2012-03-082018-06-30US flag
HemeNatal OB plus DHAIron sucrose (28 mg/1) + Biotin (30 ug/1) + Cholecalciferol (400 [iU]/1) + Cupric sulfate pentahydrate (0.8 mg/1) + Cyanocobalamin (12 ug/1) + Doconexent (200 mg/1) + Folic acid (1 mg/1) + Heme iron polypeptide (6 mg/1) + Nicotinamide (17 mg/1) + Osbond acid (2.5 mg/1) + Calcium pantothenate (10 mg/1) + Potassium Iodide (250 ug/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (1.6 mg/1) + Sodium selenate (65 ug/1) + Thiamine mononitrate (1.5 mg/1) + Zinc oxide (4.5 mg/1) + alpha-Linolenic acid (0.5 mg/1) + alpha-Tocopherol succinate (10 [iU]/1)KitOralWh Nutritionals, Llc2012-03-082019-04-30US flag
HemetabIron sucrose (22 mg/1) + Cyanocobalamin (25 ug/1) + Folic acid (1 mg/1) + Heme iron polypeptide (6 mg/1)TabletOralWh Nutritionals, Llc2012-05-01Not applicableUS flag
Marnatal FIron sucrose (60 mg/1) + Ascorbic acid (100 mg/1) + Calcium carbonate (150 mg/1) + Cholecalciferol (400 [iU]/1) + Cupric oxide (2 mg/1) + Cyanocobalamin (12 ug/1) + D-alpha-Tocopherol acetate (30 [iU]/1) + Folic acid (1000 ug/1) + Magnesium oxide (25 mg/1) + Nicotinamide (20 mg/1) + Pyridoxine hydrochloride (5 mg/1) + Riboflavin (3.4 mg/1) + Thiamine mononitrate (3 mg/1)CapsuleOralMarnel Pharmaceuticals, Llc2010-01-08Not applicableUS flag
Myferon 150Iron sucrose (150 mg/1)CapsuleOralMartin Ekwealor Pharmaceuticals, Inc.1996-12-01Not applicableUS flag
Myferon 150 ForteIron sucrose (150 mg/1) + Cyanocobalamin (25 ug/1) + Folic acid (1 mg/1)CapsuleOralMartin Ekwealor Pharmaceuticals, Inc.1996-12-01Not applicableUS flag

Categories

ATC Codes
B03AB02 — Saccharated iron oxideV03AE05 — Sucroferric oxyhydroxide
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as o-glycosyl compounds. These are glycoside in which a sugar group is bonded through one carbon to another group via a O-glycosidic bond.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Carbohydrates and carbohydrate conjugates
Direct Parent
O-glycosyl compounds
Alternative Parents
Disaccharides / C-glycosyl compounds / Ketals / Oxanes / Tetrahydrofurans / Secondary alcohols / Polyols / Oxacyclic compounds / Organic transition metal salts / Primary alcohols
show 5 more
Substituents
Acetal / Alcohol / Aliphatic heteromonocyclic compound / C-glycosyl compound / Disaccharide / Hydrocarbon derivative / Ketal / O-glycosyl compound / Organic alkali metal salt / Organic hydroxide
show 12 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
FZ7NYF5N8L
CAS number
8047-67-4
InChI Key
FWZTTZUKDVJDCM-CEJAUHOTSA-M
InChI
InChI=1S/C12H22O11.5Fe.2Na.4H2O.8O/c13-1-4-6(16)8(18)9(19)11(21-4)23-12(3-15)10(20)7(17)5(2-14)22-12;;;;;;;;;;;;;;;;;;;/h4-11,13-20H,1-3H2;;;;;;;;4*1H2;;;;;;;;/q;5*+3;2*+1;;;;;8*-2/p-1/t4-,5-,6-,7-,8+,9-,10+,11-,12+;;;;;;;;;;;;;;;;;;;/m1.................../s1
IUPAC Name
pentairon(3+) ion disodium (2R,3R,4S,5S,6R)-2-{[(2S,3S,4S,5R)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]oxy}-6-(hydroxymethyl)oxane-3,4,5-triol trihydrate hydroxide octaoxidandiide
SMILES
O.O.O.[OH-].[O--].[O--].[O--].[O--].[O--].[O--].[O--].[O--].[Na+].[Na+].[Fe+3].[Fe+3].[Fe+3].[Fe+3].[Fe+3].OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O

References

General References
  1. monograph [Link]
  2. article [Link]
  3. FDA Approved Drug Products: Velphoro Sucroferric Oxyhydroxide Oral Tablet [Link]
PubChem Compound
91663255
PubChem Substance
310265059
ChemSpider
32699616
RxNav
1484283
ChEMBL
CHEMBL1200823
Wikipedia
Iron_sucrose

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedDiagnosticAnemia in Chronic Renal Disease1
4CompletedSupportive CareAnemia of Chronic Kidney Disease1
4CompletedTreatmentAnemia1
4CompletedTreatmentAnemia of Chronic Kidney Disease1
4CompletedTreatmentChronic Heart Failure (CHF) / Iron Deficiency (ID)1
4CompletedTreatmentHyperphosphataemia / Hypoalbuminemia / Peritoneal dialysis complication1
4CompletedTreatmentIron Deficiency Anemia (IDA)1
4CompletedTreatmentIron Deficiency Anemia (IDA) / Renal Failure, Chronic Renal Failure1
4Not Yet RecruitingOtherVariola Major (Smallpox)1
4Unknown StatusPreventionHip Fracture / Surgical Intervention1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
KitOral
InjectionIntravenous
SolutionParenteral20 mg/1ml
Injection, solutionParenteral
Solution, concentrateParenteral
SolutionIntravenous20 mg
InjectionIntravenous400 MG
TabletOral
CapsuleOral
CapsuleOral150 mg/1
SolutionOral
Tablet, coatedOral
Suspension / dropsOral
Capsule, liquid filledOral
CapsuleOral
Powder, for suspensionOral125 MG
TabletOral125 mg
TabletOral500 MG
Tablet, chewableOral500 mg
Tablet, chewableOral500 mg/1
InjectionIntravenous75 mg/3.75mL
Injection, solutionIntravenous
Injection, solutionIntravenous20 MG/ML
Injection, solutionIntravenous20 mg/1mL
Injection, solutionParenteral20 mg/1ml
Injection, solution, concentrateIntravenous
SolutionIntravenous100 mg
SolutionIntravenous
Tablet, film coatedOral
Capsule, gelatin coatedOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6174442No2001-01-162016-12-19US flag
US9561251Yes2017-02-072030-07-23US flag
US10624855Yes2020-04-212035-05-26US flag
US10682376Yes2020-06-162029-05-13US flag
US10695367Yes2020-06-302029-05-13US flag
US10925896Yes2021-02-232029-05-13US flag
US10925897Yes2021-02-232029-05-13US flag
US10933090Yes2021-03-022029-05-13US flag
US11013761Yes2009-05-132029-05-13US flag
US11013762Yes2009-05-132029-05-13US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility9.52 mg/mLALOGPS
logP1.99ALOGPS
logP-4.5ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)11.84ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count11ChemAxon
Hydrogen Donor Count8ChemAxon
Polar Surface Area189.53 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity68.77 m3·mol-1ChemAxon
Polarizability30.97 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created on October 01, 2015 16:49 / Updated on October 20, 2021 19:48