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.
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Peginesatide is used for the treatment of anemia due to chronic kidney disease (CKD) in adult patients on dialysis
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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.
Tmax, SubQ dose = 48 hours;
|Volume of distribution|
IV dose, dialysis patients = 34.9 ± 13.8 mL/kg;
Peginesatide does not bind to serum albumin or lipoprotein as demonstrated in in-vitro studies.
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.
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;
Systemic clearance, IV dose, dialysis patients = 0.5 ± 0.2 mL/hr•kg
The most common adverse events (≥10%) are dyspnea, diarrhea, nausea, cough, and arteriovenous fistula site complication.
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|ATC Codes||B03XA04 — Peginesatide|
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|FDA label||Download (272 KB)|
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- Pharmacological action
- 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 some cell types, can also activate STAT1 and STAT3. May also activate the LYN tyrosine kinase.Isoform EPOR-T acts as a dominant-negative receptor of EPOR-mediated signaling.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Erythropoietin receptor
- Molecular Weight:
- 55064.725 Da
- 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 ]