Peginesatide
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
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- Indication
Peginesatide is used for the treatment of anemia due to chronic kidney disease (CKD) in adult patients on dialysis
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- 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 stimulatorHumans - 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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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir 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. 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. Acrivastine Peginesatide may decrease the excretion rate of Acrivastine which could result in a higher serum level. 
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- Not Available
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- 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 Omontys Solution 5 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US 
Omontys Solution 2 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 10 mg/1mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 4 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 1 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 6 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 3 mg/0.5mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US Omontys Solution 20 mg/2mL Intravenous; Parenteral; Subcutaneous Takeda 2012-04-23 2013-02-23 US
Categories
- ATC Codes
- B03XA04 — Peginesatide
- 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
- 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]
- 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]
- 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
- 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 US7084245 No 2006-08-01 2024-05-12 US US7414105 No 2008-08-19 2024-05-12 US US7550433 No 2009-06-23 2026-06-02 US US7919461 No 2011-04-05 2026-06-02 US US7528104 No 2009-05-05 2024-05-12 US US7919118 No 2011-04-05 2024-05-12 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source
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
- 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]
Drug created on June 01, 2013 22:45 / Updated on April 03, 2021 09:53