US 12,291,577 B2
Anti-MUC1 antibody-drug conjugate
Johanna Gellert, Berlin (DE); Anke Flechner, Berlin (DE); Doreen Weigelt, Berlin (DE); Antje Danielczyk, Berlin (DE); and Akiko Nagase, Tokyo (JP)
Assigned to DAIICHI SANKYO CO., LTD., Tokyo (JP)
Filed by DAIICHI SANKYO CO., LTD., Tokyo (JP)
Filed on Jul. 10, 2023, as Appl. No. 18/349,438.
Application 18/349,438 is a continuation of application No. 17/878,611, filed on Aug. 1, 2022, granted, now 11,872,289.
Application 17/878,611 is a continuation of application No. 17/055,323, previously published as PCT/EP2019/062758, filed on May 17, 2019.
Claims priority of application No. 18173253 (EP), filed on May 18, 2018.
Prior Publication US 2023/0372520 A1, Nov. 23, 2023
Int. Cl. C07K 16/30 (2006.01); A61K 31/4745 (2006.01); A61K 39/395 (2006.01); A61K 47/54 (2017.01); A61K 47/65 (2017.01); A61K 47/68 (2017.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01); A61K 39/00 (2006.01)
CPC C07K 16/3092 (2013.01) [A61K 31/4745 (2013.01); A61K 39/39558 (2013.01); A61K 47/545 (2017.08); A61K 47/65 (2017.08); A61K 47/68037 (2023.08); A61K 47/6851 (2017.08); A61P 35/00 (2018.01); A61P 35/02 (2018.01); A61K 2039/505 (2013.01); C07K 2317/14 (2013.01); C07K 2317/24 (2013.01); C07K 2317/41 (2013.01); C07K 2317/55 (2013.01); C07K 2317/565 (2013.01); C07K 2317/73 (2013.01); C07K 2317/76 (2013.01); C07K 2317/92 (2013.01)] 30 Claims
 
1. A conjugate comprising an antibody conjugated to a cytotoxic agent, wherein the antibody is capable of binding to MUC1 or TA-MUC1, and wherein the antibody comprises
(i) a heavy chain variable region comprising the complementarity-determining regions (CDRs) CDR-H1 having the amino acid sequence of SEQ ID NO: 1, CDR-H2 having the amino acid sequence of SEQ ID NO: 2 and CDR-H3 having the amino acid sequence of SEQ ID NO: 3, and
(ii) a light chain variable region comprising the complementarity-determining regions (CDRs) CDR-LI having the amino acid sequence of SEQ ID NO: 4, CDR-L2 having the amino acid sequence of SEQ ID NO: 5 and CDR-L3 having the amino acid sequence of SEQ ID NO: 6,
wherein the conjugate is not a conjugate represented by the following formula:

OG Complex Work Unit Chemistry
wherein (i) AB represents an antibody, the antibody comprising a heavy chain variable region having the amino acid sequence of SEQ ID NO: 10 and a light chain variable region having the amino acid sequence of SEQ ID NO: 12, y represents an average number of units of the drug-linker structure conjugated to the antibody per itself, and the antibody is conjugated to a drug linker represented by the above formula by a thioether bond, or (ii) AB represents an antibody, the antibody comprising a heavy chain having the amino acid sequence of SEQ ID NO: 22 or a variant thereof in which one amino acid has been removed from the C-terminus and a light chain having the amino acid sequence of SEQ ID NO: 16, y represents an average number of units of the drug-linker structure conjugated to the antibody per itself, and the antibody is conjugated to a drug linker represented by the above formula by a thioether bond.