Specific sites for modifying antibodies to make immunoconjugates
AssigneeNovartis AG
InventorsBernhard Hubert Geierstanger, Weijia Ou, Tetsuo Uno
Life of this patent
Estimating the term…
Abstract
The present invention provides specific sites for modifying antibodies or antibody fragments by replacing at least one native amino acid in the constant region of a parental antibody or antibody fragment with cysteine, which can be used as a site of attachment for a payload or linker-payload combination.
Claims18
An immunoconjugate comprising a modified antibody or antigen binding fragment thereof, wherein said modified antibody or antigen binding fragment comprises a substitution of the amino acid at position 152 of the heavy chain constant region of said antibody or antigen binding fragment thereof with a cysteine, wherein said position is numbered according to the EU system.
An immunoconjugate comprising a modified antibody or antigen binding fragment thereof, wherein said modified antibody or antigen binding fragment comprises two amino acid substitutions with a cysteine, wherein the substitutions are selected from:
- a. positions 152 and 375 of the heavy chain constant region of said antibody or antigen binding fragment thereof, wherein said positions are numbered according to the EU system;
- or
- b. position 107 of the light chain constant region of said antibody or antigen binding fragment thereof, wherein said light chain is a kappa light chain, and position 360 of the heavy chain constant region of said antibody or antigen binding fragment thereof, wherein said positions are numbered according to the EU system.
A modified antibody or antigen binding fragment thereof comprising a substitution of the amino acid at position 152 of the heavy chain constant region of said antibody or antigen binding fragment with a cysteine, wherein said position is numbered according to the EU system.
A modified antibody or antigen binding fragment thereof comprising two amino acid substitutions with cysteine, wherein the substitutions are selected from:
- a. positions 152 and 375 of the heavy chain constant region of said antibody or antigen binding fragment thereof, wherein said positions are numbered according to the EU system;
- or
- b. position 107 of the light chain constant region of said antibody or antigen binding fragment thereof, wherein said light chain is a kappa light chain, and position 360 of the heavy chain constant region of said antibody or antigen binding fragment thereof, wherein said positions are numbered according to the EU system.
Dependencies are inferred from the claim text.