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

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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.

Target	Actions	Organism
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

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Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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.

Drug	Interaction
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Abacavir	Abacavir may decrease the excretion rate of Peginesatide which could result in a higher serum level.
Abemaciclib	The risk or severity of Thrombosis can be increased when Peginesatide is combined with Abemaciclib.
Abiraterone	The risk or severity of Thrombosis can be increased when Peginesatide is combined with Abiraterone.
Aceclofenac	Aceclofenac may decrease the excretion rate of Peginesatide which could result in a higher serum level.
Acemetacin	Acemetacin 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

Ingredient	UNII	CAS	InChI Key
Peginesatide acetate	44STI720CW	1185870-58-9	Not applicable

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Omontys	Solution	20 mg/2mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
Omontys	Solution	5 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
Omontys	Solution	2 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
Omontys	Solution	10 mg/1mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
Omontys	Solution	4 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23

Chemical Identifiers

UNII: JX56W9N61Q
CAS number: 913976-27-9

References

General References

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]
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]
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]

External Links

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Terminated	Treatment	Anemia	1
3	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD)	1
3	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD) / Renal Failure, Chronic Renal Failure	4
2	Completed	Treatment	Anemia	2
2	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD) / Pure Red Cell Aplasia / Renal Failure, Chronic Renal Failure	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Solution	Intravenous; Parenteral; Subcutaneous	1 mg/0.5mL
Solution	Intravenous; Parenteral; Subcutaneous	10 mg/1mL
Solution	Intravenous; Parenteral; Subcutaneous	2 mg/0.5mL
Solution	Intravenous; Parenteral; Subcutaneous	20 mg/2mL
Solution	Intravenous; Parenteral; Subcutaneous	3 mg/0.5mL
Solution	Intravenous; Parenteral; Subcutaneous	4 mg/0.5mL
Solution	Intravenous; Parenteral; Subcutaneous	5 mg/0.5mL
Solution	Intravenous; Parenteral; Subcutaneous	6 mg/0.5mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US7084245	No	2006-08-01	2024-05-12
US7414105	No	2008-08-19	2024-05-12
US7550433	No	2009-06-23	2026-06-02
US7919461	No	2011-04-05	2026-06-02
US7528104	No	2009-05-05	2024-05-12
US7919118	No	2011-04-05	2024-05-12

Properties

State

Liquid

Experimental Properties

Property	Value	Source

Targets

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Details1. Erythropoietin receptor

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

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

Peginesatide

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References