Pegylation of linkers improves antitumor activity and...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2411967

The present invention is directed to the site-specific PEGylation of immunoconjugates. In particular, the present invention provides immunoconjugates wherein a connector molecule attaching a targeting molecule to an effector molecule is conjugated to one or more polyethylene glycol molecules. The present invention further provides methods for increasing the antitumor activity of an immunotoxin, comprising attaching in a site-specific manner one or more polyethylene glycol molecules to a linker connecting a toxic moiety to a targeting moiety of an immunotoxin.

L'invention concerne la pegylation spécifique d'un site d'immunoconjugués, et en particulier des immunoconjugués dans lesquels une molécule de connexion, fixant une molécule de ciblage à une molécule effectrice, est conjuguée à au moins une molécule de polyéthylène glycol. L'invention concerne également des méthodes permettant d'augmenter l'activité antitumorale d'une immunotoxine, qui consiste à fixer de manière spécifique à un site au moins une molécule de polyéthylène glycol à un lieur qui connecte une fraction toxique à une fraction de ciblage d'une immunotoxine.

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