	US 12,076,412 B2
	Antibody-drug conjugates through specific linker oligopeptides
Philipp Spycher, Au (CH); Philipp Probst, Au (CH); Isabella Attinger-Toller, Au (CH); Romain Bertrand, Au (CH); Ramona Stark, Au (CH); and Dragan Grabulovski, Au (CH)
Assigned to ARARIS BIOTECH AG, Au (CH)
Filed by ARARIS BIOTECH AG, Au (CH)
Filed on Mar. 23, 2023, as Appl. No. 18/188,991.
Application 18/188,991 is a continuation of application No. PCT/EP2021/079560, filed on Oct. 25, 2021.
Prior Publication US 2023/0263904 A1, Aug. 24, 2023
Int. Cl. A61K 47/68 (2017.01); A61P 35/00 (2006.01); C12N 9/10 (2006.01)

CPC A61K 47/6889 (2017.08) [A61P 35/00 (2018.01); C12N 9/1044 (2013.01); C12Y 203/02013 (2013.01)]

26 Claims

1. An antibody-drug conjugate comprising:

a) an IgG antibody; and

b) a linker comprising a drug moiety B, wherein the drug moiety B is a toxin covalently linked to a peptide selected from the group consisting of: RKAA (SEQ ID NO:1), RKA (SEQ ID NO:2), ARK (SEQ ID NO:3), or RK-Val-Cit (SEQ ID NO:54);

wherein the linker is conjugated to the IgG antibody via an isopeptide bond formed between the γ-carboxamide group of glutamine residue Q295 (EU numbering) of the C_H2 domain of the antibody and the primary amine comprised in the side chain of the lysine residue comprised in the peptide.