Methoxy polyethylene glycol-epoetin beta

Identification

Summary

Methoxy polyethylene glycol-epoetin beta is a synthetic erythropoiesis stimulating agent (ESA) used to treat anemia associated with chronic kidney disease.

Brand Names
Mircera
Generic Name
Methoxy polyethylene glycol-epoetin beta
DrugBank Accession Number
DB09107
Background

Methoxy polyethylene glycol-epoetin beta is a chemically synthesised Erythropoiesis Stimulating Agent (ESA) with a longer half-life than erythropoietin. ESA is used to increase synthesis of red blood cells to treat chronic kidney disease associated anemia.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • CERA
  • Pegzerepoetin alfa
External IDs
  • R-744
  • R744

Pharmacology

Indication

For the treatment of patients with anaemia associated with chronic kidney disease. Not a substitute for RBC transfusion if immediate correction of anemia is required.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Stimulates hemoglobin production by stimulating the erythropoetin receptor of erythroid progenitor cells in the bone marrow. Hemoglobin increase, following a single initial dose, occurs 7 to 15 days after.

Mechanism of action

Erythropoietin is a growth factor for erythroid development. It is produced in the kidney and released into the bloodstream in response to hypoxia, interacting with erythroid progenitor cells to increase red blood cell production. Production of endogenous erythropoietin is impaired in patients with chronic kidney disease (CKD), and erythropoietin deficiency is the primary cause of their anaemia. Administration of methoxy polyethylene glycol-epoetin beta acts like endogenous erythropoetin and stimulates erythropoetin receptor of the erythroid progenitor cells in the bone marrow.

TargetActionsOrganism
AErythropoietin receptor
stimulator
Humans
Absorption

Administered parenterally (subcutaneous or IV) therefore not absorbed.

Volume of distribution

~94.74 ml/kg

Protein binding

No protein binding

Metabolism

Not metabolized.

Route of elimination

Undergoes proteolysis at erythropoietin receptor

Half-life

In CKD patients on peritoneal dialysis with IV administration: 134 ± 65 hours In CKD patients on peritoneal dialysis with SC administration: 139 ± 67 hours

Clearance

In CKD patients on peritoneal dialysis : 0.49 ± 0.18 mL/hr/kg

Adverse Effects
Adverseeffects
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Toxicity

Overdosage can cause severe hypertension.

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
AbemaciclibThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Abemaciclib.
AbirateroneThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Abiraterone.
AfatinibThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Afatinib.
AldesleukinThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Aldesleukin.
AlectinibThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Alectinib.
AlemtuzumabThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Alemtuzumab.
AlitretinoinThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Alitretinoin.
AlpelisibThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Alpelisib.
AltretamineThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Altretamine.
AminoglutethimideThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Aminoglutethimide.
Interactions
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MirceraInjection, solution360 μg/0.6mlIntravenous; SubcutaneousRoche Registration Gmb H2016-09-08Not applicableEU flag
MirceraInjection, solution100 ug/0.3mLIntravenousVifor (International) Inc.2014-10-24Not applicableUS flag
MirceraInjection, solution40 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2016-09-08Not applicableEU flag
MirceraSolution250 mcg / 0.3 mLIntravenous; SubcutaneousHoffmann La RocheNot applicableNot applicableCanada flag
MirceraInjection, solution30 ug/0.3mLIntravenousVifor (International) Inc.2014-10-24Not applicableUS flag
MirceraInjection, solution150 ug/0.3mLIntravenousGenentech, Inc.2014-10-242019-07-31US flag
MirceraInjection, solution200 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2016-09-08Not applicableEU flag
MirceraSolution100 mcg / 0.3 mLIntravenous; SubcutaneousHoffmann La RocheNot applicableNot applicableCanada flag
MirceraInjection, solution75 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2016-09-08Not applicableEU flag
MirceraInjection, solution360 ug/0.6mLIntravenousVifor (International) Inc.2014-10-24Not applicableUS flag

Categories

ATC Codes
B03XA03 — Methoxy polyethylene glycol-epoetin beta
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
LR3UXN0193
CAS number
677324-53-7

References

General References
  1. Walrafen P, Verdier F, Kadri Z, Chretien S, Lacombe C, Mayeux P: Both proteasomes and lysosomes degrade the activated erythropoietin receptor. Blood. 2005 Jan 15;105(2):600-8. Epub 2004 Sep 9. [Article]
  2. Daily Med Micera Monograph [Link]
PubChem Substance
347910408
RxNav
729596
Wikipedia
Methoxy_polyethylene_glycol-epoetin_beta

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceRenal Anemia1
4CompletedTreatmentAnemia8
4CompletedTreatmentAnemia of End Stage Renal Disease1
4CompletedTreatmentAnemia, Kidney Disease, Chronic1
4CompletedTreatmentAnemia / Inflammation / Malnutrition1
4CompletedTreatmentRenal Anemia, Chronic1
4TerminatedTreatmentAnemia2
4Unknown StatusTreatmentPD1
3CompletedTreatmentAnemia32
3CompletedTreatmentAnemia in Pre-Dialysis Patients1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous100 ug/0.3mL
Injection, solutionIntravenous120 ug/0.3mL
Injection, solutionIntravenous150 ug/0.3mL
Injection, solutionIntravenous200 ug/0.3mL
Injection, solutionIntravenous250 ug/0.3mL
Injection, solutionIntravenous30 ug/0.3mL
Injection, solutionIntravenous360 ug/0.6mL
Injection, solutionIntravenous50 ug/0.3mL
Injection, solutionIntravenous75 ug/0.3mL
Injection, solutionIntravenous; Subcutaneous100 MCG
Injection, solutionIntravenous; Subcutaneous100 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous1000 MCG
Injection, solutionIntravenous; Subcutaneous120 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous120 MCG/0.3ML
Injection, solutionIntravenous; Subcutaneous150 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous150 MCG
Injection, solutionIntravenous; Subcutaneous200 MCG
Injection, solutionIntravenous; Subcutaneous200 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous250 MCG
Injection, solutionIntravenous; Subcutaneous250 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous30 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous30 MCG/0.3ML
Injection, solutionIntravenous; Subcutaneous300 MCG
Injection, solutionIntravenous; Subcutaneous360 μg/0.6ml
Injection, solutionIntravenous; Subcutaneous360 MCG/0.3ML
Injection, solutionIntravenous; Subcutaneous40 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous40 MCG/0.3ML
Injection, solutionIntravenous; Subcutaneous400 MCG
Injection, solutionIntravenous; Subcutaneous50 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous50 MCG
Injection, solutionIntravenous; Subcutaneous60 MCG/0.3ML
Injection, solutionIntravenous; Subcutaneous60 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous600 MCG
Injection, solutionIntravenous; Subcutaneous75 MCG
Injection, solutionIntravenous; Subcutaneous75 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous800 MCG
SolutionIntravenous; Subcutaneous100 mcg / mL
SolutionIntravenous; Subcutaneous100 mcg / 0.3 mL
SolutionIntravenous; Subcutaneous1000 mcg / mL
SolutionIntravenous; Subcutaneous150 mcg / 0.3 mL
SolutionIntravenous; Subcutaneous200 mcg / mL
SolutionIntravenous; Subcutaneous200 mcg / 0.3 mL
SolutionIntravenous; Subcutaneous250 mcg / 0.3 mL
SolutionIntravenous; Subcutaneous300 mcg / mL
SolutionIntravenous; Subcutaneous400 mcg / mL
SolutionIntravenous; Subcutaneous400 mcg / 0.6 mL
SolutionIntravenous; Subcutaneous50 mcg / mL
SolutionIntravenous; Subcutaneous50 mcg / 0.3 mL
SolutionIntravenous; Subcutaneous600 mcg / mL
SolutionIntravenous; Subcutaneous600 mcg / 0.6 mL
SolutionIntravenous; Subcutaneous75 mcg / 0.3 mL
Injection, solutionIntravenous; Subcutaneous
Injection, solutionParenteral100 UG/0.3ML
Injection, solutionParenteral100 µg/0.3ml
Injection, solutionParenteral120 UG/0.3ML
Injection, solutionParenteral120 µg/0.3ml
Injection, solutionParenteral150 UG/0.3ML
Injection, solutionParenteral150 µg/0.3ml
Injection, solutionParenteral200 UG/0.3ML
Injection, solutionParenteral200 µg/0.3ml
InjectionIntravenous; Subcutaneous
Injection, solutionParenteral250 UG/0.3ML
Injection, solutionParenteral250 µg/0.3ml
Injection, solutionParenteral30 UG/0.3ML
Injection, solutionParenteral30 µg/0.3ml
Injection, solutionParenteral360 UG/0.6ML
Injection, solutionParenteral360 µg/0.3ml
Injection, solutionParenteral50 UG/0.3ML
Injection, solutionParenteral50 µg/0.3ml
Injection, solutionParenteral75 UG/0.3ML
Injection, solutionParenteral75 µg/0.3ml
SolutionIntravenous; Subcutaneous30 mcg
SolutionIntravenous; Subcutaneous100 mcg
SolutionIntravenous; Subcutaneous150 mcg
SolutionIntravenous; Subcutaneous
SolutionIntravenous; Subcutaneous100 cg
SolutionIntravenous; Subcutaneous200 cg
SolutionIntravenous; Subcutaneous0.3 mg
SolutionIntravenous; Subcutaneous100 mcg/0.3ml
SolutionIntravenous; Subcutaneous120 mcg/0.3ml
SolutionIntravenous; Subcutaneous150 mcg/0.3ml
SolutionIntravenous; Subcutaneous50 mcg/0.3ml
SolutionIntravenous; Subcutaneous75 mcg/0.3ml
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2310536No2007-09-112020-06-28Canada flag

Properties

State
Solid
Experimental Properties
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Stimulator
General Function
Identical protein binding
Specific Function
Receptor for erythropoietin. Mediates erythropoietin-induced erythroblast proliferation and differentiation. Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade. In som...
Gene Name
EPOR
Uniprot ID
P19235
Uniprot Name
Erythropoietin receptor
Molecular Weight
55064.725 Da

Drug created on September 16, 2015 23:06 / Updated on September 19, 2021 19:53