New Technologies to Prolong Life-time of Peptide and Protein Drugs In vivo

被引:0
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作者
Y. Shechter
M. Mironchik
A. Saul
E. Gershonov
L. Precido-Patt
K. Sasson
H. Tsubery
B. Mester
A. Kapitkovsky
S. Rubinraut
Y. Vachutinski
G. Fridkin
M. Fridkin
机构
[1] Weizmann Institute of Science,Department of Biological Chemistry
[2] Weizmann Institute of Science,Department of Organic Chemistry
关键词
diabetes; FMS-technology; insulin; peptide/protein drugs; prodrugs; prolongation; reversible-pegylation;
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摘要
Most peptide and protein drugs are short-lived species in vivo with a circulatory half-life of several minutes. This is particularly valid for non-glycosylated proteins with a molecular mass of less than 50 kDa. Since peptide/protein drugs are not absorbed orally, prolonged maintenance of therapeutically active drugs in the circulatory system is of primary clinical importance. Another major obstacle of injected polypeptide drugs is the elevated concentration of 100–1000 times above the therapeutical level that may be present in the circulatory system shortly after administration. Such overdosing may lead to undesirable side effects such as over-stimulation or down-regulation of receptor sites.
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页码:105 / 117
页数:12
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