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Erythropoiesis stimulating agents approaches to modulate activity
Authors Sinclair AM
Received 30 March 2013
Accepted for publication 14 May 2013
Published 3 July 2013 Volume 2013:7 Pages 161—174
DOI https://doi.org/10.2147/BTT.S45971
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 4
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
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