Calicheamicin conjugation by antibody deglycosylation

Details Calicheamicin conjugation by antibody deglycosylation Calicheamicin conjugation by antibody deglycosylation

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2557866

The present invention provides processed for preparing a calicheamicin conjugate comprising removing glycosylation of a protein and reacting (i) an activated calicheamicin-hydrolyzable linker derivative and (ii) the deglycosylated protein. In one embodiment, the protein is an antibody, such as an anti-CD33 antibody (e.g., hp67.6), an anti-CD22 antibody (e.g., G544), an anti-Lewis Y antibody (e.g., G193), an anti-5T4 antibody (e.g., H8) or an anti- CD20 antibody (e.g., rituximab). In another embodiment, the calicheamicin derivative is an N-acyl derivative of calicheamicin or a disulfide analog of calicheamicin, such as N-acetyl gamma calicheamicin dimethyl hydrazide (N- acetyl calicheamicin DMH) and the hydrolyzable linker is 4-(4~acetylephenoxy) butanoic acid (AcBut) or (3-Acetylphenyl) acetic acid (AcPAc). Also provided are calicheamicin conjugates produced by such processes.

La présente invention concerne des processus de préparation d'un conjugué de calichéamicine qui consiste à extraire la glycosylation d'une protéine et à faire réagir (i) un dérivé de lieur hydrolysable par calichéamicine activée et (ii) cette protéine déglycosylée. Dans un mode de réalisation, la protéine est un anticorps, tel qu'un anticorps anti CD33 (par exemple hp67,6), un anticorps anti CD22 (par exemple G544), un anticorps Y anti Lewis (par exemple CG193), un anticorps anti 5T4 (par exemple H8) ou un anticorps anti CD20 (par exemple rituximab). Dans un autre mode de réalisation, le dérivé de calichéamicine est un dérivé N-acyle de calichéamicine qu'un analogue disulfure de calichéamicine, tel que N-acétyle gamma calichéamicine diméthyle hydrazide (N-acétyle calichéamicine DMH) et le lieur hydrolysable est 4-(4-acétylephénoxy) acide butanoïque (AcBut) ou (3-Acétylphényle) acide acétique (AcPAc). Cette invention concerne aussi des conjugués de calichéamicine produits selon ces procéssus.

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