Targeting of erb antigens

Details Targeting of erb antigens Targeting of erb antigens

A - Human Necessities

61

K

A61K 39/395 (2006.01) A61K 51/10 (2006.01) C07K 17/02 (2006.01) G01N 33/543 (2006.01)

Patent

CA 2547435

A conjugate comprising a) a trifunctional cross-linking moiety, to which is coupled b) an affinity ligand via a linker 1, c) a cytotoxic agent, optionally via a linker 2, and d) an anti Erb antibody or variants thereof having the ability to bind to Erb antigens expressed on mammalian tumour surfaces with an affinity-binding constant of at least 5x106M-1, wherein the affinity ligand is biotin, or a biotin derivative having essentially the same binding function to avidin or streptavidin as biotin, wherein stability towards enzymatic cleavage of the biotinamide bond has been introduced in linker 1.

La présente invention a trait à un conjugué comportant : a) un groupe fonctionnel de réticulation trifonctionnel, auquel est couplé b) un ligand d'affinité via un lieur 1, c) un agent cytotoxique, éventuellement via un lieur 2, et d) un anticorps anti-Erb ou des variants de celui-ci ayant la capacité de se lier aux antigènes Erb exprimés sur des surfaces tumorales mammaliennes avec une constante d'affinité de liaison d'au moins 5x10?6¿M?-1¿, dans lequel le ligand d'affinité est la biotine, ou un dérivé de biotine ayant sensiblement la même fonction de liaison à l'avidine ou la streptavidine, ou un dérivé de biotine, dans lequel la stabilité vis-à-vis de clivage enzymatique d'une liaison biotinamide a été introduite dans le lieur 1.

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