Methoxy polyethylene glycol-epoetin beta

Identification

Name
Methoxy polyethylene glycol-epoetin beta
Accession Number
DB09107  (DB06279)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
Description

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.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
  • CERA
  • Pegzerepoetin alfa
External IDs
R-744 / R744
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MirceraSolution400 mcgIntravenous; SubcutaneousHoffmann La RocheNot applicableNot applicableCanada
MirceraInjection, solution50 ug/0.3mLIntravenousVifor Inc.2014-10-24Not applicableUs
MirceraInjection, solution50 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2007-07-20Not applicableEu
MirceraInjection, solution250 ug/0.3mLIntravenousVifor Inc.2014-10-24Not applicableUs
MirceraInjection, solution75 ug/0.3mLIntravenousGenentech, Inc.2014-10-242019-07-31Us
MirceraSolution50 mcgIntravenous; SubcutaneousHoffmann La RocheNot applicableNot applicableCanada
MirceraInjection, solution30 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2007-07-20Not applicableEu
MirceraInjection, solution50 μg/0.3mlIntravenous; SubcutaneousRoche Registration Gmb H2007-07-20Not applicableEu
MirceraInjection, solution100 ug/0.3mLIntravenousVifor Inc.2014-10-24Not applicableUs
MirceraSolution50 mcgIntravenous; SubcutaneousHoffmann La RocheNot applicableNot applicableCanada
Categories
UNII
LR3UXN0193
CAS number
677324-53-7

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.

Associated Conditions
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
Human
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

Toxicity

Overdosage can cause severe hypertension.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
Abicipar PegolThe therapeutic efficacy of Abicipar Pegol can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
Antihemophilic Factor (Recombinant), PEGylatedThe therapeutic efficacy of Antihemophilic Factor (Recombinant), PEGylated can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
Cepeginterferon alfa-2BThe therapeutic efficacy of Cepeginterferon alfa-2B can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
Certolizumab pegolThe therapeutic efficacy of Methoxy polyethylene glycol-epoetin beta can be decreased when used in combination with Certolizumab pegol.
CyclophosphamideThe risk or severity of pulmonary toxicity can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Cyclophosphamide.
Damoctocog alfa pegolThe therapeutic efficacy of Damoctocog alfa pegol can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
Egaptivon pegolThe therapeutic efficacy of Methoxy polyethylene glycol-epoetin beta can be decreased when used in combination with Egaptivon pegol.
ElapegademaseThe therapeutic efficacy of Elapegademase can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
Eptacog alfa pegol (activated)The therapeutic efficacy of Eptacog alfa pegol (activated) can be decreased when used in combination with Methoxy polyethylene glycol-epoetin beta.
GlycoPEG-GCSFThe therapeutic efficacy of Methoxy polyethylene glycol-epoetin beta can be decreased when used in combination with GlycoPEG-GCSF.
Food Interactions
Not Available

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. [PubMed:15358619]
  2. Daily Med Micera Monograph [Link]
External Links
PubChem Substance
347910408
Wikipedia
Methoxy_polyethylene_glycol-epoetin_beta
ATC Codes
B03XA03 — Methoxy polyethylene glycol-epoetin beta
AHFS Codes
  • 20:16.00 — Hematopoietic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedOtherReticulocyte Count1
2Active Not RecruitingTreatmentAnemias1
2CompletedTreatmentAcute Myocardial Infarction (AMI)1
2CompletedTreatmentAnemias5
2CompletedTreatmentAnemias / Chronic Kidney Disease (CKD)1
2CompletedTreatmentChronic Kidney Disease (CKD)1
2RecruitingTreatmentAnemias / Renal Insufficiency,Chronic1
3CompletedTreatmentAnemia in Pre-Dialysis Patients1
3CompletedTreatmentAnemias32
3CompletedTreatmentAnemias / Renal Anemia, Chronic2
3CompletedTreatmentHemodialysis Patients3
3CompletedTreatmentPeritoneal Dialysis Patients1
3CompletedTreatmentPredialysis Patients1
3TerminatedTreatmentAnemias6
3WithdrawnTreatmentAnemias1
4CompletedTreatmentAnemia of End Stage Renal Disease1
4CompletedTreatmentAnemia, Kidney Disease, Chronic1
4CompletedTreatmentAnemias8
4CompletedTreatmentAnemias / Inflammatory Reaction / Malnutrition1
4CompletedTreatmentAnemias / Renal Anemia, Chronic1
4TerminatedTreatmentAnemias2
4Unknown StatusTreatmentPD1
Not AvailableCompletedNot AvailableAnemia, Kidney Transplantation1
Not AvailableCompletedNot AvailableAnemias3
Not AvailableCompletedNot AvailableAnemias / Chronic Kidney Disease (CKD)1
Not AvailableCompletedNot AvailableChronic Kidney Disease (CKD)2
Not AvailableCompletedNot AvailableChronic Kidney Disease (CKD) / Renal Anemia of Chronic Kidney Disease1
Not AvailableCompletedNot AvailableImpaired Renal Function / Renal Anemia of Chronic Kidney Disease1

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 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous120 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous150 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous200 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous250 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous30 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous360 μg/0.6ml
Injection, solutionIntravenous; Subcutaneous40 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous50 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous60 μg/0.3ml
Injection, solutionIntravenous; Subcutaneous75 μg/0.3ml
SolutionIntravenous; Subcutaneous100 mcg
SolutionIntravenous; Subcutaneous1000 mcg
SolutionIntravenous; Subcutaneous150 mcg
SolutionIntravenous; Subcutaneous200 mcg
SolutionIntravenous; Subcutaneous250 mcg
SolutionIntravenous; Subcutaneous300 mcg
SolutionIntravenous; Subcutaneous400 mcg
SolutionIntravenous; Subcutaneous50 mcg
SolutionIntravenous; Subcutaneous600 mcg
SolutionIntravenous; Subcutaneous75 mcg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2310536No2007-09-112020-06-28Canada

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Human
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 17:06 / Updated on December 14, 2018 05:43