Erythropoiesis stimulating agents approaches to modulate activity

Angus M Sinclair Amgen Inc, Thousand Oaks, CA, USA Abstract: 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 t...

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Autor principal:	Sinclair AM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/c50b66a52a4947e6b18f0a2108cca0f7
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spelling	oai:doaj.org-article:c50b66a52a4947e6b18f0a2108cca0f72021-12-02T00:07:36ZErythropoiesis stimulating agents approaches to modulate activity1177-54751177-5491https://doaj.org/article/c50b66a52a4947e6b18f0a2108cca0f72013-07-01T00:00:00Zhttp://www.dovepress.com/erythropoiesis-stimulating-agents-approaches-to-modulate-activity-a13543https://doaj.org/toc/1177-5475https://doaj.org/toc/1177-5491Angus M Sinclair Amgen Inc, Thousand Oaks, CA, USA Abstract: 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 pharmacokinetic 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. Keywords: darbepoetin alfa, erythropoiesis, erythropoietin, glycosylation, pharmacokinetics, pharmacology, polyethylene glycolsSinclair AMDove Medical PressarticleMedicine (General)R5-920ENBiologics: Targets & Therapy, Vol 2013, Iss default, Pp 161-174 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Sinclair AM Erythropoiesis stimulating agents approaches to modulate activity
description	Angus M Sinclair Amgen Inc, Thousand Oaks, CA, USA Abstract: 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 pharmacokinetic 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. Keywords: darbepoetin alfa, erythropoiesis, erythropoietin, glycosylation, pharmacokinetics, pharmacology, polyethylene glycols
format	article
author	Sinclair AM
author_facet	Sinclair AM
author_sort	Sinclair AM
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
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/c50b66a52a4947e6b18f0a2108cca0f7
work_keys_str_mv	AT sinclairam erythropoiesisstimulatingagentsapproachestomodulateactivity
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Erythropoiesis stimulating agents approaches to modulate activity

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