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.
CAT No: 10-101-162
CAS No:913976-27-9, 910576-32-8
Synonyms/Alias:AF37702;AF 37702;Hematide;HSDB 8181;Peginesatide;UNII-JX56W9N61Q
Peginesatide is a synthetic peptide-based erythropoiesis-stimulating agent designed to mimic the biological activity of endogenous erythropoietin. Structurally, it is a pegylated, dimeric peptide that binds to and activates the erythropoietin receptor, thereby promoting the proliferation and differentiation of erythroid progenitor cells. Its unique peptide architecture, combined with polyethylene glycol (PEG) conjugation, enhances molecular stability and prolongs systemic circulation, making it a valuable tool for researchers investigating erythropoiesis and receptor-mediated signaling pathways. Peginesatide's distinct lack of sequence homology with endogenous erythropoietin further allows for specific mechanistic studies and analytical differentiation in experimental systems.
Erythropoiesis research: Peginesatide serves as a robust model compound for studying the molecular mechanisms underlying erythropoietin receptor activation and downstream erythroid cell development. By providing a non-endogenous ligand for the erythropoietin receptor, it enables researchers to dissect signaling cascades, evaluate receptor binding kinetics, and analyze the transcriptional events driving erythroid lineage commitment. Its use facilitates controlled investigations into the regulation of red blood cell production under various physiological and pathological conditions.
Receptor-ligand interaction studies: The synthetic nature and defined structure of peginesatide make it ideal for probing the specificity and affinity of peptide interactions with the erythropoietin receptor. Researchers can utilize it in binding assays, surface plasmon resonance experiments, and structural biology studies to map receptor binding domains, elucidate conformational changes upon ligand engagement, and compare the receptor activation profiles of peptide mimetics versus native erythropoietin. These insights are critical for advancing the understanding of receptor pharmacology and the design of next-generation peptide therapeutics.
Analytical method development: Peginesatide is frequently employed as a reference standard or analytical control in the development and validation of quantitative assays for erythropoiesis-stimulating agents. Its unique sequence and pegylation pattern allow for the establishment of highly specific detection protocols using techniques such as liquid chromatography, mass spectrometry, or immunoassays. These analytical methods are essential for monitoring compound stability, assessing pharmacokinetics, and ensuring the integrity of bioprocessing workflows in research settings.
Pharmacokinetic and biodistribution studies: The pegylated structure of this peptide facilitates investigations into the effects of PEG conjugation on peptide half-life, tissue distribution, and metabolic fate. Researchers can utilize it in in vitro and in vivo models to examine how molecular modifications influence absorption, distribution, metabolism, and excretion profiles. Such studies provide valuable data for optimizing peptide drug design, improving delivery strategies, and understanding the impact of structural modifications on biological performance.
Peptide synthesis and formulation research: Peginesatide offers a relevant model for evaluating advanced peptide synthesis techniques, PEGylation strategies, and formulation approaches. Its complex structure provides opportunities to optimize solid-phase synthesis protocols, study the impact of PEG attachment on peptide folding and solubility, and develop novel delivery vehicles for peptide-based agents. These applications support the advancement of peptide engineering and contribute to the broader field of peptide-based drug development and biopharmaceutical innovation.
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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