Potent conjugates and hydrophilic linkers

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2722109

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment.

L'invention concerne des coupleurs pour lier des médicaments à des agents de liaison de cellule modifiés en coupleurs hydrophiles par incorporation d'un espaceur de polyéthylèneglycol. La puissance ou l'efficacité des conjugués d'agent de liaison à une cellule-médicament est renforcée de manière surprenante plusieurs fois dans divers types de cellules cancéreuses, y compris celles exprimant un faible nombre d'antigènes sur la surface cellulaire ou les cellules de cancer qui sont résistantes à un traitement.

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