Comprehensive Characterization of N‐Glycosylation in Darbepoetin Alfa

EPO analogues are representative glycoprotein drugs composed of heterogeneous, multiple antennary N‐glycans. NESP® and Aranesp® are hyperglycosylated EPO, marketed under the same international nonproprietary name as darbepoetin alfa. The multiple antennary N‐glycans are a key factor that increases t...

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Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2019, 40(10), , pp.976-982
Main Authors: Lee, Jung Rok, Choi, Doyoung, Choi, Inseong, Park, Mikyung, Choi, Eunyoung, Lee, Yoon Jung, Park, Jeehye, Yang, Yoo Hee, Ha, Gyong‐Sik, Chul Jin, Hong, Kim, Kwang Pyo
Format: Article
Language:English
Subjects:
Darbepoetin alfa
Erythropoietin
HILIC
Mass
N‐glycan
화학
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Summary:EPO analogues are representative glycoprotein drugs composed of heterogeneous, multiple antennary N‐glycans. NESP® and Aranesp® are hyperglycosylated EPO, marketed under the same international nonproprietary name as darbepoetin alfa. The multiple antennary N‐glycans are a key factor that increases the half‐life of the drug in the body, which is closely related to efficacy. Thus, control of N‐glycosylation is important in providing patients with consistent efficacy. This paper reports on the comprehensive characterization of N‐glycosylation of darbepoetin alfa products. The results of N‐glycan analysis of NESP® and Aranesp® showed difference in the ratio of N‐glycans containing N‐acetyllactosamine and O‐acetylated sialic acid. Although there were some differences, the overall N‐glycan structures and profiles were comparable. In particular, darbepoetin alfa products accounted for the largest proportion of tetra‐sialo N‐glycans, greater than 75%. This study increases understanding of N‐glycan profiles and structural information of darbepoetin alfa. Characterization of N‐glycans in Darbepoetin alfa.
ISSN:1229-5949
0253-2964
1229-5949
DOI:10.1002/bkcs.11856