Peginesatide

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.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.

CAT No: 10-101-162

CAS No:913976-27-9, 910576-32-8

Synonyms/Alias:AF37702;AF 37702;Hematide;HSDB 8181;Peginesatide;UNII-JX56W9N61Q

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M.F/Formula
C233H352N62O60S6
M.W/Mr.
5174.06
Labeling Target
Erythropoietin receptor
Application
Treatment of anemia associated with chronic kidney disease
Activity
Stimulator
Biological Activity
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.
Areas of Interest
Chronic kidney disease
Functions
Identical protein binding

Peginesatide is a synthetic, PEGylated peptide-based compound designed to mimic the biological activity of endogenous erythropoietin. Engineered for enhanced stability and prolonged circulation in biological systems, Peginesatide features a unique molecular structure that allows it to interact selectively with erythropoietin receptors. Its innovative design incorporates polyethylene glycol (PEG) chains, which improve solubility and reduce immunogenicity, making it a valuable tool for research in hematopoiesis and erythropoiesis. The compound's robust in vitro and in vivo activity has attracted significant interest from the scientific community, particularly in studies focused on red blood cell production, receptor binding dynamics, and peptide modification strategies. As a chemically synthesized peptide, Peginesatide supports a wide range of experimental protocols and is compatible with various analytical methods, including cell-based assays, protein interaction studies, and pharmacodynamic evaluations.

Erythropoiesis Research: Peginesatide is extensively utilized in basic and translational research to investigate the mechanisms underlying red blood cell formation. By serving as an erythropoietin receptor agonist, it stimulates erythroid progenitor cells, enabling scientists to dissect signaling pathways that regulate erythropoiesis. Its ability to activate similar downstream pathways as natural erythropoietin makes it a reliable surrogate in experiments that require precise control over erythroid differentiation and proliferation. Researchers leverage this property to model erythropoietic responses in vitro, facilitating the identification of novel regulators and potential therapeutic targets within the erythropoietic cascade.

Receptor Binding and Signal Transduction Studies: The unique structure of Peginesatide makes it an ideal probe for characterizing erythropoietin receptor interactions and downstream signaling events. Its PEGylated backbone allows for detailed mapping of binding affinities, receptor activation kinetics, and conformational changes upon ligand engagement. Scientists employ Peginesatide in receptor cross-linking assays, competition binding studies, and phosphorylation analysis to elucidate the molecular determinants of erythropoietin receptor activation. These insights contribute to a deeper understanding of receptor-ligand specificity and the development of next-generation peptide therapeutics.

Pharmacokinetics and Drug Delivery Research: Peginesatide's extended half-life and enhanced solubility due to PEGylation make it a valuable model compound for studying the pharmacokinetics of peptide-based drugs. Researchers use it to evaluate absorption, distribution, metabolism, and excretion profiles in preclinical settings, providing critical data for optimizing drug delivery systems. Insights gained from these studies inform the design of novel PEGylated peptides with improved bioavailability and reduced dosing frequency, advancing the field of long-acting biologics.

Peptide Engineering and Modification: The design of Peginesatide serves as a reference point for the rational engineering of synthetic peptides with tailored pharmacological properties. Its modular structure and successful PEGylation strategy offer a blueprint for modifying other bioactive peptides to enhance stability, reduce immunogenicity, and prolong systemic exposure. Researchers in peptide chemistry and drug design draw upon Peginesatide's attributes to develop innovative analogs and conjugates for diverse biomedical applications.

Biomarker and Diagnostic Tool Development: The well-characterized activity of Peginesatide enables its application in the development of in vitro diagnostics and biomarker discovery platforms related to erythropoietic activity. By acting as a standardized agonist in cell-based assays, it allows for the quantification of erythropoietin receptor function and the assessment of erythroid cell responsiveness. Analytical laboratories utilize it to validate assay sensitivity, monitor batch-to-batch variability, and benchmark novel diagnostic reagents, supporting robust quality control in research and development pipelines.

In summary, Peginesatide stands as a multifunctional research tool with broad utility across erythropoiesis research, receptor biology, pharmacokinetics, peptide engineering, and diagnostic development. Its synthetic, PEGylated nature provides superior experimental flexibility, making it indispensable for scientists seeking to advance understanding in hematopoietic signaling, optimize peptide-based drug candidates, and establish reliable bioanalytical assays. Through its diverse applications, Peginesatide continues to drive innovation in the fields of peptide science and hematology research.

Source#
Synthetic
Organism
Human
References

Peginesatide is a peptide-based erythropoiesis-stimulating agent (ESA) that may have therapeutic potential for anemia in patients with advanced chronic kidney disease. We evaluated the safety and efficacy of peginesatide, as compared with another ESA, darbepoetin, in 983 such patients who were not undergoing dialysis.

Peginesatide for Anemia in Patients with Chronic Kidney Disease Not Receiving Dialysis

Peginesatide, a synthetic peptide-based erythropoiesis-stimulating agent (ESA), is a potential therapy for anemia in patients with advanced chronic kidney disease. Peginesatide, administered monthly, was as effective as epoetin, administered one to three times per week, in maintaining hemoglobin levels in patients undergoing hemodialysis.

Peginesatide in Patients with Anemia Undergoing Hemodialysis

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