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1. (WO2018160683) CYSTEINE MUTATED ANTIBODIES FOR CONJUGATION

Pub. No.:    WO/2018/160683    International Application No.:    PCT/US2018/020206
Publication Date: Sat Sep 08 01:59:59 CEST 2018 International Filing Date: Thu Mar 01 00:59:59 CET 2018
IPC: A61K 39/395
A61K 38/02
A61K 47/64
A61K 47/68
C07K 16/46
C12N 15/09
C12P 21/02
Applicants: SEATTLE GENETICS, INC.
Inventors: WAIGHT, Andrew
LEISKE, Chris
BIECHELE, Travis
SUSSMAN, Django
BURKE, Patrick
LEISKE, Jocelyn
Title: CYSTEINE MUTATED ANTIBODIES FOR CONJUGATION
Abstract:
The invention provides modified heavy chain constant regions including a cysteine at position 295 by EU numbering and optionally at position 239 by EU numbering. These cysteine residues provide sites for conjugation to a drug or label. When both cysteines are present in a normal heterodimeric antibody format, there are four such sites per molecule of antibody allowing a stoichiometry of one molecule of antibody to four of drug or label. Selection of the cysteine at position 295 with or without cysteine at position 239 is advantageous over cysteines at many other positions due to ease of expression, stability and cytotoxicity.