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

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MOLSDFPDBSMILESInChI

Similar Structures

Structure for Ferric derisomaltose (DB15617)

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Weight

Average: 562.297
Monoisotopic: 562.117975

Chemical Formula

C₁₈H₃₄FeO₁₆

Synonyms

• Ferric derisomaltose

External IDs

• NS32
• WHO 9712

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

• Iron Deficiency Anemia (IDA)
• Requirement 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

Target	Actions	Organism
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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Ferric ammonium citrate	The absorption of Ferric ammonium citrate can be decreased when combined with Ferric derisomaltose.
Ferric cation	The absorption of Ferric cation can be decreased when combined with Ferric derisomaltose.
Ferric maltol	The absorption of Ferric maltol can be decreased when combined with Ferric derisomaltose.
Ferric sulfate	The absorption of Ferric sulfate can be decreased when combined with Ferric derisomaltose.
Ferrous bisglycinate	The absorption of Ferrous bisglycinate can be decreased when combined with Ferric derisomaltose.
Ferrous fumarate	The absorption of Ferrous fumarate can be decreased when combined with Ferric derisomaltose.
Ferrous gluconate	The absorption of Ferrous gluconate can be decreased when combined with Ferric derisomaltose.
Ferrous succinate	The absorption of Ferrous succinate can be decreased when combined with Ferric derisomaltose.
Ferrous sulfate anhydrous	The absorption of Ferrous sulfate anhydrous can be decreased when combined with Ferric derisomaltose.
Ferumoxides	The absorption of Ferumoxides can be decreased when combined with Ferric derisomaltose.

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Food Interactions

No interactions found.

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Monoferric	Solution	500 mg/5mL	Intravenous	Pharmacosmos A/S	2020-01-16	Not applicable
Monoferric	Injection, solution	500 mg/5mL	Intravenous	Pharmacosmos Therapeutics Inc.	2020-01-16	Not applicable
Monoferric	Injection, solution	100 mg/1mL	Intravenous	Pharmacosmos Therapeutics Inc.	2020-01-16	Not applicable
Monoferric	Solution	100 mg / mL	Intravenous	Pharmacosmos A/S	2018-10-17	Not applicable
Monoferric	Solution	100 mg/1mL	Intravenous	Pharmacosmos A/S	2020-01-16	Not applicable
Monoferric	Solution	1000 mg/10mL	Intravenous	Pharmacosmos A/S	2020-01-16	Not applicable
Monoferric	Injection, solution	1000 mg/10mL	Intravenous	Pharmacosmos Therapeutics Inc.	2020-01-16	Not applicable

Categories

Drug Categories

• Anemia, Iron-Deficiency
• Antianemia Drugs
• Antianemic Preparations
• Carbohydrates
• Iron Compounds
• Iron Preparations
• Oligosaccharides
• Parenteral Iron Replacement
• Polysaccharides

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]

External Links

RxNav

2274394

Wikipedia

Ferric_derisomaltose

FDA label

Download (388 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Chronic Heart Failure (CHF) / Iron Deficiency (ID) / Systolic Left Ventricular Dysfunction	1
4	Enrolling by Invitation	Treatment	Postoperative Anaemia	1
4	Not Yet Recruiting	Treatment	Adults / Perioperative Anemia / Spinal Deformities / Surgery	1
4	Not Yet Recruiting	Treatment	Anemia / Surgery	1
4	Recruiting	Treatment	Anemia of Pregnancy / Iron Deficiency Anemia (IDA) / Low Birth Weight Infants	1
4	Recruiting	Treatment	Heart Failure With Preserved Ejection Fraction (HFpEF) / Iron Deficiency (ID)	1
4	Recruiting	Treatment	Iron Deficiency Anemia (IDA)	1
3	Completed	Treatment	Chronic Kidney Disease (CKD) / Iron Deficiency Anemia (IDA)	1
3	Completed	Treatment	Iron Deficiency Anemia (IDA)	4
3	Not Yet Recruiting	Treatment	Anemia / Iron Deficiency (ID) / Reproductive neoplasms female malignant and unspecified	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Parenteral
Injection, solution	Intravenous	100 mg/ml
Injection, solution	Intravenous bolus; Intravenous drip	100 mg/ml
Injection, solution	Intravenous	100 mg/1mL
Injection, solution	Intravenous	1000 mg/10mL
Injection, solution	Intravenous	500 mg/5mL
Solution	Intravenous	100 mg/1mL
Solution	Intravenous	100 mg / mL
Solution	Intravenous	1000 mg/10mL
Solution	Intravenous	500 mg/5mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US10414831	No	2019-09-17	2029-03-25
US8815301	No	2014-08-26	2029-08-14

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	284.0 mg/mL	ALOGPS
logP	-3.2	ALOGPS
logP	-7.3	Chemaxon
logS	-0.25	ALOGPS
pKa (Strongest Acidic)	11.86	Chemaxon
pKa (Strongest Basic)	-3.6	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	16	Chemaxon
Hydrogen Donor Count	12	Chemaxon
Polar Surface Area	279.68 Å2	Chemaxon
Rotatable Bond Count	11	Chemaxon
Refractivity	103.23 m3·mol-1	Chemaxon
Polarizability	47.86 Å3	Chemaxon
Number of Rings	2	Chemaxon
Bioavailability	0	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Not Available

Targets

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insights and accelerate drug research.

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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...

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Components:

Name	UniProt ID
Transferrin receptor protein 1	P02786
Transferrin receptor protein 2	Q9UP52

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]

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Drug created at February 03, 2020 17:03 / Updated at June 08, 2023 10:19