NAV

Ferric derisomaltose

Identification

Summary

Ferric derisomaltose is an iron injection used in the treatment of iron deficiency anemia.

Generic Name
Ferric derisomaltose
DrugBank Accession Number
DB15617
Background

Iron deficiency is an extremely common condition and is the most frequent cause of anemia worldwide. Iron deficiency results when iron intake, iron stores, and loss of iron from the body do not adequately support production of erythrocytes, also known as red blood cells. Though it is generally considered non life-threatening, iron deficiency may considerably affect quality of life.3

Ferric derisomaltose is a form of iron used in the treatment of iron deficiency. This drug is a complex of iron (III) hydroxide and derisomaltose. The latter is an iron carbohydrate oligosaccharide that works to release iron. Ferric derisomaltose was developed by Pharmacosmos Therapeutics ad was granted FDA approval in January 2020.8,9 Clinical trials show that it is non-inferior to iron sucrose, another form of iron that is often administered in iron deficiency, and less likely to cause serious hypersensitivity that is associated with other forms of injectable iron.1,4

Type
Small Molecule
Groups
Approved
Structure
Similar Structures
Weight
Average: 562.297
Monoisotopic: 562.117975
Chemical Formula
C18H34FeO16
Synonyms
  • Ferric derisomaltose
External IDs
  • NS32
  • WHO 9712
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Pharmacology

Indication

This drug is indicated for the treatment of iron deficiency anemia in adult patients who have experienced intolerance to oral iron preparations or insufficient clinical response to orally administered iron. Ferric derisomaltase is also indicated for patients with non-hemodialysis dependent chronic kidney disease.8 In Australia and United Kingdom, ferric derisomaltase is indicated for cases in which rapid delivery of iron is required.10,11

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofIron deficiency anemia (ida)••••••••••••••••••••••••••••• •••••••• •• •••• •••••••••••••• ••••••••
Treatment ofIron deficiency anemia (ida)••••••••••••••••••••••••••••••••• ••••••••• ••••••• •••••• ••••••••••••••••• ••••••••
Treatment ofIron deficiency anemia (ida)•••••••••••••••••••••••••••• •• •••• •••• •••••••••••••••••••••• ••••••••
Treatment ofRequirement for rapid iron delivery•••••••••••••••••••••• ••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Ferric derisomaltase increases the reticulocyte count and ultimately increases hemoglobin, treating iron deficiency anemia and its various symptoms.5,3 Parenteral iron, such as ferric derisomaltose, may cause false elevations in serum bilirubin levels and falsely reduced serum calcium.10,11

Mechanism of action

This drug is a complex made of iron (III) hydroxide and derisomaltose, which is an iron carbohydrate oligosaccharide that works to releases iron. The released iron then binds to the transport protein, transferrin, and is taken to erythroid precursor cells3 for incorporation into the hemoglobin molecule.8,10

TargetActionsOrganism
UHemoglobin subunit alpha
binder
Humans
UTransferrin receptor
binder
Humans
Absorption

After a single 1000 mg dose, the Cmax and AUC of serum iron were 408 μg/mL and 17730 μg.h /mL, respectively. Serum ferritin concentrations reach their peak about 7 days after a single dose of intravenous ferric derisomaltose.8

A note on concomitant oral iron

The absorption of oral iron is decreased when administered with intravenous iron. The administration of oral iron should be delayed until at least 5 days after the last ferric derisomaltose injection.10

Volume of distribution

Ferric derisomaltose or released iron that was released is found in cells of the reticuloendothelial system (RES). It is found to be highly concentrated in the liver and spleen.10 The volume of distribution of other forms of intravenous iron is 3L, on average, in a 70 kg adult.5 Though the specific volume of distribution of ferric derisomaltose is not readily available in the literature, it is likely similar to other intravenous forms of iron.5

Protein binding

Iron binds to transferrin, the transport molecule responsible for transporting iron to erythroid precursor cells for the production of hemoglobin.5,8

Metabolism

Iron in the circulation is taken up by the plasma by cells of the RES. This binds proteins that form hemosiderin or ferritin, as well transferrin. Following this step, the bound iron replenishes low hemoglobin (Hb) and iron.10

Route of elimination

Renal elimination was not a significant route of elimination in single-dose pharmacokinetic studies. Iron can often accumulate in the body leading to iron overload followed by toxic effects.6 Small amounts of ferric derisomaltose are excreted in the urine and feces.10

Half-life

The plasma-half live of intravenous iron is about 1-4 days.10

Clearance

Intravenous iron is cleared from the plasma.6 Ferric derisomaltose is not eliminated via the kidneys, as the size of the complex is large and cannot be excreted via the nephron.10

Adverse Effects
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Toxicity

LD50 information for ferric derisomaltose is not readily available in the literature, however, the LD50 for iron sucrose (another form of intravenous iron) was 140 mg/kg in male rats.12 An overdose with ferric derisomaltose may lead to accumulation of stored iron, causing hemosiderosis.11 Symptoms may include abdominal pain, weakness, and lethargy, among others.7 Serum ferritin should be monitored. Employ supportive treatment including chelating agents.8,11

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
Integrate drug-drug
interactions in your software
Ferric ammonium citrateThe absorption of Ferric ammonium citrate can be decreased when combined with Ferric derisomaltose.
Ferric cationThe absorption of Ferric cation can be decreased when combined with Ferric derisomaltose.
Ferric maltolThe absorption of Ferric maltol can be decreased when combined with Ferric derisomaltose.
Ferric sulfateThe absorption of Ferric sulfate can be decreased when combined with Ferric derisomaltose.
Ferrous bisglycinateThe absorption of Ferrous bisglycinate can be decreased when combined with Ferric derisomaltose.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MonoferricSolution100 mg / mLIntravenousPharmacosmos A/S2018-10-17Not applicableCanada flag
MonoferricInjection, solution100 mg/1mLIntravenousPharmacosmos Therapeutics Inc.2020-01-16Not applicableUS flag
MonoferricSolution100 mg/1mLIntravenousPharmacosmos A/S2020-01-16Not applicableUS flag
MonoferricInjection, solution1000 mg/10mLIntravenousPharmacosmos Therapeutics Inc.2020-01-16Not applicableUS flag
MonoferricSolution1000 mg/10mLIntravenousPharmacosmos A/S2020-01-16Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
AHU547PI9H
CAS number
1345510-43-1
InChI Key
JTQTXQSGPZRXJF-DOJSGGEQSA-N
InChI
InChI=1S/C18H34O16.Fe/c19-1-5(21)9(23)10(24)6(22)3-31-17-16(30)14(28)12(26)8(34-17)4-32-18-15(29)13(27)11(25)7(2-20)33-18;/h5-30H,1-4H2;/q;+3/t5-,6+,7+,8+,9+,10+,11+,12+,13-,14-,15+,16+,17-,18-;/m0./s1
IUPAC Name
iron(3+) (2S,3R,4R,5R)-6-{[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-({[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}methyl)oxan-2-yl]oxy}hexane-1,2,3,4,5-pentol
SMILES
[Fe+3].OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H](O)[C@H]1O

References

Synthesis Reference

Christensen TS, Andreasen HB.(2019).WO2019048674A1. Retrieved from: https://patents.google.com/patent/WO2019048674A1/en

General References
  1. Pollock RF, Biggar P: Indirect methods of comparison of the safety of ferric derisomaltose, iron sucrose and ferric carboxymaltose in the treatment of iron deficiency anemia. Expert Rev Hematol. 2020 Feb;13(2):187-195. doi: 10.1080/17474086.2020.1709437. Epub 2020 Jan 11. [Article]
  2. Auerbach M, Henry D, Derman RJ, Achebe MM, Thomsen LL, Glaspy J: A prospective, multi-center, randomized comparison of iron isomaltoside 1000 versus iron sucrose in patients with iron deficiency anemia; the FERWON-IDA trial. Am J Hematol. 2019 Jun 26. doi: 10.1002/ajh.25564. [Article]
  3. 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]
  4. Rampton D, Folkersen J, Fishbane S, Hedenus M, Howaldt S, Locatelli F, Patni S, Szebeni J, Weiss G: Hypersensitivity reactions to intravenous iron: guidance for risk minimization and management. Haematologica. 2014 Nov;99(11):1671-6. doi: 10.3324/haematol.2014.111492. [Article]
  5. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  6. Adams PC, Deugnier Y, Moirand R, Brissot P: The relationship between iron overload, clinical symptoms, and age in 410 patients with genetic hemochromatosis. Hepatology. 1997 Jan;25(1):162-6. doi: 10.1002/hep.510250130. [Article]
  7. Bacon BR, Adams PC, Kowdley KV, Powell LW, Tavill AS: Diagnosis and management of hemochromatosis: 2011 practice guideline by the American Association for the Study of Liver Diseases. Hepatology. 2011 Jul;54(1):328-43. doi: 10.1002/hep.24330. [Article]
  8. FDA Approved Products: MONOFERRIC (ferric derisomaltose) for injection [Link]
  9. EMPR: Monoferric injection approved for iron deficiency anemia [Link]
  10. Auspar: Monofer (ferric derisomaltose) [Link]
  11. EMC: Monofer 100mg/ml solution for injection/infusion [Link]
  12. Canadian Monograph: Venofer (iron sucrose) [Link]
RxNav
2274394
Wikipedia
Ferric_derisomaltose
FDA label
Download (388 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAnemia of Pregnancy / Iron Deficiency Anemia (IDA) / Low Birth Weight Infants1
4CompletedTreatmentChronic Heart Failure (CHF) / Iron Deficiency (ID) / Systolic Left Ventricular Dysfunction1
4CompletedTreatmentPostoperative Anaemia1
4Not Yet RecruitingBasic ScienceAnemia / Iron Deficiency Anemia (IDA)1
4Not Yet RecruitingTreatmentAnemia / Surgery1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionParenteral
Injection, solutionParenteral100 mg/ml
Injection, solutionIntravenous100 mg/ml
Injection, solutionIntravenous bolus; Intravenous drip100 mg/ml
Injection, solutionIntravenous100 mg/1mL
Injection, solutionIntravenous1000 mg/10mL
Injection, solutionIntravenous500 mg/5mL
SolutionIntravenous100 mg / mL
SolutionIntravenous100 mg/1mL
SolutionIntravenous1000 mg/10mL
SolutionIntravenous500 mg/5mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US10414831No2019-09-172029-03-25US flag
US8815301No2014-08-262029-08-14US flag
US11633489No2016-06-222036-06-22US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility284.0 mg/mLALOGPS
logP-3.2ALOGPS
logP-7.3Chemaxon
logS-0.25ALOGPS
pKa (Strongest Acidic)11.86Chemaxon
pKa (Strongest Basic)-3.6Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count16Chemaxon
Hydrogen Donor Count12Chemaxon
Polar Surface Area279.68 Å2Chemaxon
Rotatable Bond Count11Chemaxon
Refractivity103.23 m3·mol-1Chemaxon
Polarizability47.86 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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Details1. Hemoglobin subunit alpha
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Peters F, Ellermann I, Steinbicker AU: Intravenous Iron for Treatment of Anemia in the 3 Perisurgical Phases: A Review and Analysis of the Current Literature. Anesth Analg. 2018 Apr;126(4):1268-1282. doi: 10.1213/ANE.0000000000002591. [Article]
  2. Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012. [Article]
  3. FDA Approved Products: MONOFERRIC (ferric derisomaltose) for injection [Link]
Details2. Transferrin receptor (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
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:
NameUniProt ID
Transferrin receptor protein 1P02786
Transferrin receptor protein 2Q9UP52
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. FDA Approved Products: MONOFERRIC (ferric derisomaltose) for injection [Link]
  3. EMC: Monofer 100mg/ml solution for injection/infusion [Link]

Transporters

Details1. Transferrin receptor (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
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:
NameUniProt ID
Transferrin receptor protein 1P02786
Transferrin receptor protein 2Q9UP52
References
  1. Auerbach M, Henry D, Derman RJ, Achebe MM, Thomsen LL, Glaspy J: A prospective, multi-center, randomized comparison of iron isomaltoside 1000 versus iron sucrose in patients with iron deficiency anemia; the FERWON-IDA trial. Am J Hematol. 2019 Jun 26. doi: 10.1002/ajh.25564. [Article]
  2. FDA Approved Products: MONOFERRIC (ferric derisomaltose) for injection [Link]
  3. Auspar: Monofer (ferric derisomaltose) [Link]

Drug created at February 03, 2020 17:03 / Updated at April 19, 2024 20:55