Human growth hormone conjugated with biocompatible polymer

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) C07K 14/61 (2006.01)

Patent

CA 2616187

The present invention relates to conjugates of biocompatible polymers and hGH, particularly PEG-hGH, where the activated biocompatible polymer is conjugated to a carboxyl group of hGH at a molar ratio of 2:1 or less, preferably 1:1, methods of preparation, and related pharmaceutical compositions. The PEG-hGH conjugates have up to 20% of the activity of the native hGH while the in vivo half life is increased 10 fold. The PEG-hGH conjugates may be used therapeutically to treat growth retardation or growth failure, especially short stature in children, and conditions related to aging.

L'invention porte sur des conjugués de polymères biocompatibles et de hGH en particulier de PEG-hGH, dans lesquels le polymère biocompatible activé est conjugué à un groupe carbonyle de hGH dans un ratio molaire de 2:1 ou moins, et de préférence de 1:1, L'invention porte également sur leurs méthodes de préparation et sur des préparations pharmaceutiques associées. Les conjugués de PEG-hGH, qui présentent jusqu'à 20 % de l'activité des hGH natives, et dont la demi-vie in vivo est multipliée par 10, peuvent être utilisés en thérapie pour traiter les retards ou les défauts de croissance, spécialement des enfants de courte stature, et les états liés à l'âge.

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