Peginesatide

Identification

Generic Name
Peginesatide
DrugBank Accession Number
DB08894
Background

Peginesatide is a synthetic peptide attached to polyethylene glycol for the treatment of anemia. The polyethylene glycol moiety helps make the drug less immunogenic and prolongs its plasma half-life. Chemically, peginesatide is designed to mimic the pharmacological activity of erythropoietin, but is not a replica of the structure itself. Peginesatide consists of two 21-amino acid chains that are covalently bonded by a linker derived from iminodiacetic acid and β-alanine. FDA approved March 27, 2012.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Peptides
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Hematide
  • Peginesatide
External IDs
  • AF-37702
  • AF37702

Pharmacology

Indication

Peginesatide is used for the treatment of anemia due to chronic kidney disease (CKD) in adult patients on dialysis

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Peginesatide increases the reticulocyte count and levels of hemoglobin. It also increases RBC count, hematocrit, and soluble transferrin receptor protein in a dose-dependent manner.

Mechanism of action

Peginesatide binds to and activates the human erythropoietin receptor and stimulates erythropoiesis in human red cell precursors in vitro.

TargetActionsOrganism
AErythropoietin receptor
stimulator
Humans
Absorption

Tmax, SubQ dose = 48 hours;
Bioavailability, SubQ dose = 46%; Peginesatide does not accumulate when administered every 4 weeks following intravenous or subcutaneous administration.

Volume of distribution

IV dose, dialysis patients = 34.9 ± 13.8 mL/kg;

Protein binding

Peginesatide does not bind to serum albumin or lipoprotein as demonstrated in in-vitro studies.

Metabolism

Preclinical radiolabeled peginesatide study indicated that peginesatide is not metabolized.

Route of elimination

Peginesatide administered intravenously or subcutaneously is primarily excreted via urine. Most of the excreted dose is in the form of unchanged drug. Elimination from the plasma is biphasic and rapid from vascular compartments. In contrast, the drug is selectively retained in sites of erythropoiesis like the bone marrow.

Half-life

IV dose, healthy subjects = 25.0 ± 7.6 hours; SubQ, healthy subjects = 53.0 ± 17.7 hours; IV dose, dialysis patients = 47.9 ± 16.5 hours;

Clearance

Systemic clearance, IV dose, dialysis patients = 0.5 ± 0.2 mL/hr•kg

Adverse Effects
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Toxicity

The most common adverse events (≥10%) are dyspnea, diarrhea, nausea, cough, and arteriovenous fistula site complication.

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
AbacavirAbacavir may decrease the excretion rate of Peginesatide which could result in a higher serum level.
AbemaciclibThe risk or severity of Thrombosis can be increased when Peginesatide is combined with Abemaciclib.
AbirateroneThe risk or severity of Thrombosis can be increased when Peginesatide is combined with Abiraterone.
AceclofenacAceclofenac may decrease the excretion rate of Peginesatide which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Peginesatide which could result in a higher serum level.
Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Peginesatide acetate44STI720CW1185870-58-9Not applicable
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OmontysSolution10 mg/1mLIntravenous; Parenteral; SubcutaneousTakeda2012-04-232013-02-23US flag
OmontysSolution4 mg/0.5mLIntravenous; Parenteral; SubcutaneousTakeda2012-04-232013-02-23US flag
OmontysSolution1 mg/0.5mLIntravenous; Parenteral; SubcutaneousTakeda2012-04-232013-02-23US flag
OmontysSolution6 mg/0.5mLIntravenous; Parenteral; SubcutaneousTakeda2012-04-232013-02-23US flag
OmontysSolution3 mg/0.5mLIntravenous; Parenteral; SubcutaneousTakeda2012-04-232013-02-23US flag

Categories

ATC Codes
B03XA04 — Peginesatide
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
  • Humans and other mammals

Chemical Identifiers

UNII
JX56W9N61Q
CAS number
913976-27-9

References

General References
  1. Schmid H: Peginesatide for the treatment of renal disease-induced anemia. Expert Opin Pharmacother. 2013 May;14(7):937-48. doi: 10.1517/14656566.2013.780695. Epub 2013 Mar 18. [Article]
  2. Woodburn KW, Holmes CP, Wilson SD, Fong KL, Press RJ, Moriya Y, Tagawa Y: Absorption, distribution, metabolism and excretion of peginesatide, a novel erythropoiesis-stimulating agent, in rats. Xenobiotica. 2012 Jul;42(7):660-70. doi: 10.3109/00498254.2011.649310. Epub 2011 Dec 22. [Article]
  3. Woodburn KW, Fong KL, Wilson SD, Sloneker S, Strzemienski P, Solon E, Moriya Y, Tagawa Y: Peginesatide clearance, distribution, metabolism, and excretion in monkeys following intravenous administration. Drug Metab Dispos. 2013 Apr;41(4):774-84. doi: 10.1124/dmd.112.048033. Epub 2013 Jan 14. [Article]
KEGG Drug
D09947
PubChem Substance
175427138
RxNav
1248798
ChEBI
66895
ChEMBL
CHEMBL2107866
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Peginesatide
FDA label
Download (272 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4TerminatedTreatmentAnemia1
3CompletedTreatmentAnemia / Chronic Kidney Disease (CKD)1
3CompletedTreatmentAnemia / Chronic Kidney Disease (CKD) / Renal Failure, Chronic Renal Failure4
2CompletedTreatmentAnemia2
2CompletedTreatmentAnemia / Chronic Kidney Disease (CKD) / Pure Red Cell Aplasia / Renal Failure, Chronic Renal Failure1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SolutionIntravenous; Parenteral; Subcutaneous1 mg/0.5mL
SolutionIntravenous; Parenteral; Subcutaneous10 mg/1mL
SolutionIntravenous; Parenteral; Subcutaneous2 mg/0.5mL
SolutionIntravenous; Parenteral; Subcutaneous20 mg/2mL
SolutionIntravenous; Parenteral; Subcutaneous3 mg/0.5mL
SolutionIntravenous; Parenteral; Subcutaneous4 mg/0.5mL
SolutionIntravenous; Parenteral; Subcutaneous5 mg/0.5mL
SolutionIntravenous; Parenteral; Subcutaneous6 mg/0.5mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7084245No2006-08-012024-05-12US flag
US7414105No2008-08-192024-05-12US flag
US7550433No2009-06-232026-06-02US flag
US7919461No2011-04-052026-06-02US flag
US7528104No2009-05-052024-05-12US flag
US7919118No2011-04-052024-05-12US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource

Targets

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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
References
  1. Woodburn KW, Fong KL, Wilson SD, Sloneker S, Strzemienski P, Solon E, Moriya Y, Tagawa Y: Peginesatide clearance, distribution, metabolism, and excretion in monkeys following intravenous administration. Drug Metab Dispos. 2013 Apr;41(4):774-84. doi: 10.1124/dmd.112.048033. Epub 2013 Jan 14. [Article]

Drug created at June 01, 2013 22:45 / Updated at January 02, 2024 23:48