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US 9,764,038 B2Granted
Enzymatic conjugation of antibodies
AssigneesInnate Pharma, Paul Scherrer Institut
InventorsPatrick Dennler, Delphine Bregeon, Laurent Gauthier, François Romagné, Christian Belmant, Eliane Fischer, Roger Schibli
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Abstract
The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
Claims13
A method for attaching a lysine-based linker to an antibody, comprising:
- a) providing a human or humanized antibody comprising one or more solvent exposed glutamine residues in a variable region and at least one acceptor glutamine residue in a constant region or in a sequence fused to a constant region or fused to a variable region, wherein said one or more solvent exposed glutamine residues are present in a light chain variable domain (VL) CDR at a Kabat position selected from the group consisting of 27, 55, and a combination thereof;
- and
- b) reacting said antibody with a lysine-based linker in the presence of a transglutaminase, under conditions permitting said lysine-based linker to be covalently linked to said at least one acceptor glutamine residue in a constant region or in a sequence fused to a constant region or fused to a variable region in said human or humanized antibody.
Dependencies are inferred from the claim text.