Erythropoiesis stimulating agents: approaches to modulate activity

Recombinant human erythropoietin (rHuEPO), such as the approved agents epoetin alfa and epoetin beta, has been used successfully for over 20 years to treat anemia in millions of patients. However, due to the relatively short half-life of the molecule (approximately 8 hours), frequent dosing may be r...

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Main Author: Sinclair, Angus M
Format: Online
Language:English
Published: Dove Medical Press 2013
Online Access:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3704234/
id pubmed-3704234
recordtype oai_dc
spelling pubmed-37042342013-07-11 Erythropoiesis stimulating agents: approaches to modulate activity Sinclair, Angus M Review Recombinant human erythropoietin (rHuEPO), such as the approved agents epoetin alfa and epoetin beta, has been used successfully for over 20 years to treat anemia in millions of patients. However, due to the relatively short half-life of the molecule (approximately 8 hours), frequent dosing may be required to achieve required hemoglobin levels. Therefore, a need was identified in some anemic patient populations for erythropoiesis stimulating agents with longer half-lives that required less frequent dosing. This need led to the development of second generation molecules which are modified versions of rHuEPO with improved pharma-cokinetic and pharmacodynamic properties such as darbepoetin alfa, a hyperglycosylated analog of rHuEPO, and pegzyrepoetin, a pegylated rHuEPO. Third generation molecules, such as peginesatide, which are peptide mimetics that have no sequence homology to rHuEPO have also recently been developed. The various molecular, pharmacokinetic, and pharmacodynamic properties of these and other erythropoiesis stimulating agents will be discussed in this review. Dove Medical Press 2013 2013-07-03 /pmc/articles/PMC3704234/ /pubmed/23847411 http://dx.doi.org/10.2147/BTT.S45971 Text en © 2013 Sinclair, publisher and licensee Dove Medical Press Ltd This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
repository_type Open Access Journal
institution_category Foreign Institution
institution US National Center for Biotechnology Information
building NCBI PubMed
collection Online Access
language English
format Online
author Sinclair, Angus M
spellingShingle Sinclair, Angus M
Erythropoiesis stimulating agents: approaches to modulate activity
author_facet Sinclair, Angus M
author_sort Sinclair, Angus M
title Erythropoiesis stimulating agents: approaches to modulate activity
title_short Erythropoiesis stimulating agents: approaches to modulate activity
title_full Erythropoiesis stimulating agents: approaches to modulate activity
title_fullStr Erythropoiesis stimulating agents: approaches to modulate activity
title_full_unstemmed Erythropoiesis stimulating agents: approaches to modulate activity
title_sort erythropoiesis stimulating agents: approaches to modulate activity
description Recombinant human erythropoietin (rHuEPO), such as the approved agents epoetin alfa and epoetin beta, has been used successfully for over 20 years to treat anemia in millions of patients. However, due to the relatively short half-life of the molecule (approximately 8 hours), frequent dosing may be required to achieve required hemoglobin levels. Therefore, a need was identified in some anemic patient populations for erythropoiesis stimulating agents with longer half-lives that required less frequent dosing. This need led to the development of second generation molecules which are modified versions of rHuEPO with improved pharma-cokinetic and pharmacodynamic properties such as darbepoetin alfa, a hyperglycosylated analog of rHuEPO, and pegzyrepoetin, a pegylated rHuEPO. Third generation molecules, such as peginesatide, which are peptide mimetics that have no sequence homology to rHuEPO have also recently been developed. The various molecular, pharmacokinetic, and pharmacodynamic properties of these and other erythropoiesis stimulating agents will be discussed in this review.
publisher Dove Medical Press
publishDate 2013
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3704234/
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