US 12,227,593 B2
Site-specific conjugation of glycosylated monoclonal antibodies with transglutaminase
Vadim Dudkin, Chalfont, PA (US); Shalom Goldberg, Merion Station, PA (US); Michael J. McCauley, Abington, PA (US); Kristen Wiley, Trappe, PA (US); and Rebecca Wissner, Philadelphia, PA (US)
Assigned to Janssen Biotech, Inc., Horsham, PA (US)
Filed by Janssen Biotech, Inc., Horsham, PA (US)
Filed on May 19, 2021, as Appl. No. 17/324,148.
Claims priority of provisional application 63/027,396, filed on May 20, 2020.
Prior Publication US 2021/0388085 A1, Dec. 16, 2021
Int. Cl. C07K 16/32 (2006.01); A61K 47/68 (2017.01); C07K 16/28 (2006.01); C12N 9/10 (2006.01)
CPC C07K 16/32 (2013.01) [A61K 47/68031 (2023.08); A61K 47/6849 (2017.08); C07K 16/2803 (2013.01); C12N 9/1044 (2013.01); C07K 2317/21 (2013.01); C07K 2317/32 (2013.01); C07K 2317/94 (2013.01); C12Y 203/02013 (2013.01)] 45 Claims
 
1. An engineered monoclonal antibody comprising an amino acid substitution at heavy chain position 302 of the antibody, a glutamine substitution at heavy chain position 286, 287, 288, 289, 290, 293 or 294, and/or an alanine substitution at heavy chain position 241, 243, 294 or 301, and an endogenous heavy chain Q295 residue, wherein the engineered monoclonal antibody is non-deglycosylated, the substitution at heavy chain position 302 is V302S, V302A or V302T, and wherein the engineered monoclonal antibody further comprises the amino acid substitution Y300L at heavy chain position 300, and the amino acid numbering is according to the EU Index of Kabat.