IP Library › Granted Patent US 12685781
Granted Patent B2
US 12685781 · App. 17/668,904 · Granted Jul 21, 2026

Anti-HER3 antibody-drug conjugate

Inventors: Thore Hettmann (Martinsried, DE); Reimar Abraham (Martinsried, DE); Sabine Blum (Martinsried, DE); Suguru Ueno (Tokyo, JP)
Assignees: Daiichi Sankyo Company, Limited; Daiichi Sankyo Europe GmbH
A61K47/6849A61K47/68037A61K47/6889A61P35/00G06T11/23G06T11/60G06T13/80G06T11/10G06T2200/24
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Quick Facts
Patent No.
US 12685781
App. No.
17/668,904
Granted
Jul 21, 2026
Kind
B2
Abstract

To provide an antitumor drug having excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER3 antibody via a linker having a structure represented by the formula: -L 1 -L 2 -L P -NH—(CH 2 )n 1 -L a -(CH 2 )n 2 -C(═O)— or -L 1 -L 2 -L P - (the anti-HER3 antibody is connected to the terminal of L 1 , the antitumor compound is connected to the carbonyl group of —(CH 2 )n 2 -C(═O)— moiety or the C terminal of L P , with the nitrogen atom of the amino group at position 1 as a connecting position).

Claims (57)

1 . An antibody-drug conjugate, wherein a linker and an antitumor compound represented by any one of the following formulae and anti-HER3 antibody are connected:

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-GGFG 

-NH-CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-GGFG 

-NH-CH 2 CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-GGFG 

-NH-CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-GGFG 

-NH-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 590)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-DGGFG 

-NH-CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 590)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-DGGFG 

-NH-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-GGFG

-NH-CH 2 CH 2 -O-CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-NH-CH 2 CH 2 -O-

CH 2 CH 2 -O-CH 2 CH 2 -C(═O)-GGFG 

-NH-CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-NH-CH 2 CH 2 -O-

CH 2 CH 2 -O-CH 2 CH 2 -O-CH 2 CH 2 -O-CH 2 CH 2 -C(=O)-GGFG 

-NH-CH 2 CH 2 -C(═O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-NH-CH 2 CH 2 -O-

CH 2 CH 2 -O-CH 2 CH 2 -O-CH 2 CH 2 -O-CH 2 CH 2 -C(=O)-GGFG 

-NH-CH 2 CH 2 CH 2 -C(=O)-(NH-DX),

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-GGFG 

-(NH-DX),

(SEQ ID NO: 590)

-(Succinimid-3-yl-N)-CH 2 CH 2 -C(═O)-DGGFG 

-(NH-DX), or

(SEQ ID NO: 585)

-(Succinimid-3-yl-N)-CH 2 CH 2 CH 2 CH 2 CH 2 -C(═O)-GGFG 

-(NH-DX)

wherein

-(Succinimid-3-yl-N)- has a structure represented by the following formula:

which is connected to the antibody at position 3 thereof and is connected to a methylene group in the linker structure containing this structure on the nitrogen atom at position 1, and (NH-DX) represents a group represented by the following formula:

wherein the nitrogen atom of the amino group at position 1 is the connecting position.

2 . The antibody-drug conjugate according to claim 1 , wherein an average number of units of the drug-linker structure conjugated per antibody is in a range of from 2 to 8.

3 . The antibody-drug conjugate according to claim 1 , wherein an average number of units of the drug-linker structure conjugated per antibody is in a range of from 3 to 8.

4 . A drug containing the antibody-drug conjugate according to claim 1 or a salt thereof.

5 . A pharmaceutical composition containing the antibody-drug conjugate according to claim 1 or a salt thereof as an active component, and a pharmaceutically acceptable formulation component.

6 . The antibody-drug conjugate according to claim 1 , wherein the antibody comprises the CDRH1 to CDRH3 and CDRL1 to CDRL3 of U1-49, U1-53, U1-59, U1-7 or U1-9 in the heavy and light chains, respectively.

7 . A pharmaceutical composition comprising the antibody-drug conjugate according to claim 6 , a salt thereof as an active ingredient, and a pharmaceutically acceptable formulation ingredient.

8 . The antibody-drug conjugate according to claim 1 , wherein the antibody comprises the heavy chain variable region and the light chain variable chain of U1-49, U1-53, U1-59, U1-7 or U1-9 on the heavy and light chains, respectively.

9 . The antibody-drug conjugate according to claim 1 , wherein the antibody comprises the amino acid sequences represented by SEQ ID Nos: 42 and 44, SEQ ID Nos: 54 and 56, SEQ ID Nos: 70 and 72, SEQ ID Nos: 92 and 94, or, SEQ ID Nos: 96 and 98, in the heavy and light chains, respectively.

10 . The antibody-drug conjugate according to claim 1 , wherein the antibody comprises the amino acid sequences represented by SEQ ID Nos: 583 and 584 in the heavy and light chains, respectively.

11 . The antibody-drug conjugate according to claim 1 , wherein the antibody comprises the light chain of SEQ ID NO: 584 and the heavy chain of SEQ ID NO: 583, wherein the lysine residue at the carboxyl terminus of the heavy chain is absent.