US 12,138,315 B2
Anti-CD37 antibody-drug conjugate
Tomoko Terauchi, Tokyo (JP); Yuji Shinjo, Tokyo (JP); Hajime Sugawara, Tokyo (JP); Yusuke Shuchi, Tokyo (JP); and Riki Goto, Tokyo (JP)
Assigned to DAIICHI SANKYO COMPANY, LIMITED, Tokyo (JP)
Filed by DAIICHI SANKYO COMPANY, LIMITED, Tokyo (JP)
Filed on Jan. 12, 2024, as Appl. No. 18/411,436.
Application 18/411,436 is a continuation of application No. PCT/JP2022/038604, filed on Oct. 17, 2022.
Claims priority of application No. 2021-170114 (JP), filed on Oct. 18, 2021.
Prior Publication US 2024/0165254 A1, May 23, 2024
Int. Cl. A61K 47/68 (2017.01); A61P 35/00 (2006.01)
CPC A61K 47/6849 (2017.08) [A61K 47/68037 (2023.08); A61K 47/6889 (2017.08); A61P 35/00 (2018.01)] 46 Claims
OG exemplary drawing
 
1. An antibody-drug conjugate wherein an anti-CD37 antibody is conjugated to a drug-linker structure represented by any one formula selected from the group consisting of the following formulas (a) to (f):
-(Succinimid-3-yl-N)—CH2CH2—C(═O)-GGFG-NH—CH2CH2CH2—C(═O)—(NH-DX),  (a)
-(Succinimid-3-yl-N)—CH2CH2CH2CH2CH2—C(═O)-GGFG-NH—CH2CH2CH2—C(═O)—(NH-DX),  (b)
-(Succinimid-3-yl-N)—CH2CH2CH2CH2CH2—C(═O)-GGFG-NH—CH2—O—CH2—C(═O)—(NH-DX),  (c)
-(Succinimid-3-yl-N)—CH2CH2CH2CH2CH2—C(═O)-GGFG-NH—CH2CH2—O—CH2—C(═O)—(NH-DX),  (d)
-(Succinimid-3-yl-N)—CH2CH2—C(═O)—NH—CH2CH2O—CH2CH2O—CH2CH2—C(═O)-GGFG-NH—CH2CH2CH2—C(═O)—(NH-DX), and  (e)
-(Succinimid-3-yl-N)—CH2CH2—C(═O)—NH—CH2CH2O—CH2CH2O—CH2CH2O—CH2CH2O—CH2CH2—C(═O)-GGFG-NH—CH2CH2CH2—C(═O)—(NH-DX),  (f)
wherein
-(Succinimid-3-yl-N)— has a structure represented by the following formula:

OG Complex Work Unit Chemistry
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,
GGFG represents an amino acid sequence consisting of glycine-glycine-phenylalanine-glycine linked through peptide bonds,
—(NH-DX) is a group represented by the following formula:

OG Complex Work Unit Chemistry
with the nitrogen atom of the amino group at position 1 as a connecting position,
and the anti-CD37 antibody comprises
a light chain variable region comprising the amino acid sequence at positions 21 to 128 in the light chain full-length amino acid sequence shown in SEQ ID NO: 2 and
a heavy chain variable region comprising the CDRH1 consisting of SEQ ID NO: 22; the CDRH2 consisting of SEQ ID NO: 23; and the CDRH3 consisting of SEQ ID NO: 24.