Synthesis and Pharmacological Properties of the Azo-Conjugate of Erythropoietin β with Poly(Ethylene Glycol)

被引:0
作者
Sheremet'ev, S., V [1 ]
Lonshakov, D., V [1 ]
Belosludtseva, E. M. [1 ]
Borisova, O., V [2 ]
Sidorova, A., V [1 ]
Kalinskii, A., V [1 ]
机构
[1] FORT LLC, Okskoe 390540, Ryazan Region, Russia
[2] II Mechnikov Inst Vaccines & Sera, 5a Malyi Kazennyi Pereulok, Moscow 105064, Russia
关键词
PEGylated proteins; azo coupling; erythropoietin beta; Mircera; pharmacokinetics; bioequivalence; POLYETHYLENE-GLYCOL; ANEMIA; DISEASE; PEGYLATION; DIALYSIS; IRON;
D O I
10.1007/s11094-021-02480-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A conjugate of erythropoietin beta with 30 kDa linear methoxy poly(ethylene glycol) characterized by the presence of an azo spacer between the protein fragment and poly(ethylene glycol) was developed for import-substitution of Mircera drug in the Russian Federation. The erythropoietic activity of the synthesized conjugate was determined. Its pharmacokinetics in CBA mice were found to be comparable to those of Mircera. The bioequivalence of the proposed azo conjugate and Mircera was established based on the calculated drug pharmacokinetic parameters in mice.
引用
收藏
页码:698 / 705
页数:8
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