Identification

Name

Peginesatide

Accession Number

DB08894

Description

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

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.

Affected organisms

• Humans and other mammals

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
Unlock Additional Data
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.
Acarbose	Acarbose may decrease the excretion rate of Peginesatide which could result in a higher serum level.
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.
Acetaminophen	Acetaminophen may decrease the excretion rate of Peginesatide which could result in a higher serum level.
Acetazolamide	Acetazolamide may increase the excretion rate of Peginesatide which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid	Acetylsalicylic acid may decrease the excretion rate of Peginesatide which could result in a higher serum level.
Aclidinium	Peginesatide may decrease the excretion rate of Aclidinium which could result in a higher serum level.

Additional Data Available

Extended Description
Extended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
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Severity
Severity
A severity rating for each drug interaction, from minor to major.
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Evidence Level
Evidence Level
A rating for the strength of the evidence supporting each drug interaction.
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Action
Action
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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Food Interactions

Not Available

Products

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	Region	Image
Unlock Additional Data
Omontys	Solution	6 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
Omontys	Solution	3 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23
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
Omontys	Solution	1 mg/0.5mL	Intravenous; Parenteral; Subcutaneous	Takeda	2012-04-23	2013-02-23

Additional Data Available

Application Number
Application Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
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Product Code
Product Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories

ATC Codes

B03XA04 — Peginesatide

• B03XA — Other antianemic preparations
• B03X — OTHER ANTIANEMIC PREPARATIONS
• B03 — ANTIANEMIC PREPARATIONS
• B — BLOOD AND BLOOD FORMING ORGANS

Drug Categories

• Alcohols
• Amino Acids, Peptides, and Proteins
• Antianemic Preparations
• Blood and Blood Forming Organs
• Compounds used in a research, industrial, or household setting
• Drugs that are Mainly Renally Excreted
• Erythropoiesis-Stimulating Agents
• Ethylene Glycols
• Glycols
• Increased Erythroid Cell Production
• Macromolecular Substances
• Pegylated agents
• Polymers

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

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. [PubMed:23506424]
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. [PubMed:22188389]
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. [PubMed:23318685]

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

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) / Chronic Renal Failure (CRF)	4
2	Completed	Treatment	Anemia	2
2	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF)	4
2	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF) / Pure Red Cell Aplasia	1
2	Completed	Treatment	Chemotherapy Induced Anemia / Malignancies	1
2	Terminated	Treatment	Anemia / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF)	3
1	Completed	Treatment	Anemia / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF) / Malignancies	1
1	Terminated	Treatment	Anemia	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)	Region
Unlock Additional Data
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

Additional Data Available

Filed On
Filed On
The date on which a patent was filed with the relevant government.
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Properties

State

Liquid

Experimental Properties

Property	Value	Source

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There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.

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Drug created on June 01, 2013 16:45 / Updated on June 12, 2020 11:42