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Comprehensive Characterization of N ‐Glycosylation in Darbepoetin Alfa
Author(s) -
Lee Jung Rok,
Choi Doyoung,
Choi Inseong,
Park Mikyung,
Choi Eunyoung,
Lee Yoon Jung,
Park Jeehye,
Yang Yoo Hee,
Ha GyongSik,
Chul Jin Hong,
Kim Kwang Pyo
Publication year - 2019
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11856
Subject(s) - darbepoetin alfa , glycan , glycosylation , sialic acid , glycoprotein , chemistry , n linked glycosylation , biochemistry , computational biology , biology , hemoglobin
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.