	US 12,479,919 B2
	Anti-CTLA4 and anti-PD-1 bifunctional antibody, pharmaceutical composition thereof and use thereof
Baiyong Li, Guangdong (CN); Yu Xia, Guangdong (CN); Zhongmin Maxwell Wang, Guangdong (CN); and Peng Zhang, Guangdong (CN)
Assigned to Akeso Pharmaceuticals, Inc., Guangzhou (CN)
Filed by Akeso Pharmaceuticals, Inc., Guangdong (CN)
Filed on Dec. 16, 2022, as Appl. No. 18/067,669.
Application 18/067,669 is a continuation of application No. 16/327,076, granted, now 11,578,128, previously published as PCT/CN2017/098466, filed on Aug. 22, 2017.
Claims priority of application No. 201610705624.2 (CN), filed on Aug. 23, 2016.
Prior Publication US 2024/0010728 A1, Jan. 11, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 16/28 (2006.01); A61K 39/395 (2006.01); A61P 7/06 (2006.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01); C07K 16/46 (2006.01); C12N 15/62 (2006.01); G01N 33/577 (2006.01); G01N 33/68 (2006.01); A61K 39/00 (2006.01)

CPC C07K 16/2818 (2013.01) [A61K 39/395 (2013.01); A61P 7/06 (2018.01); A61P 35/00 (2018.01); A61P 35/02 (2018.01); C07K 16/46 (2013.01); C07K 16/468 (2013.01); C12N 15/62 (2013.01); G01N 33/577 (2013.01); G01N 33/68 (2013.01); A61K 2039/505 (2013.01); C07K 2317/24 (2013.01); C07K 2317/31 (2013.01); C07K 2317/622 (2013.01); C07K 2317/76 (2013.01); C07K 2317/92 (2013.01); G01N 2333/70521 (2013.01)]

22 Claims

1. A bispecific antibody, comprising:

an immunoglobulin comprising a heavy chain and a light chain,

wherein the heavy chain comprises a first heavy chain variable region comprising heavy chain complementarity determining region (HCDR) 1 of SEQ ID NO: 29, HCDR2 of SEQ ID NO: 30, and HCDR3 of SEQ ID NO: 31, and a heavy chain constant region,

wherein the light chain comprises a first light chain variable region comprising light chain complementarity determining region (LCDR) 1 of SEQ ID NO: 32, LCDR2 of SEQ ID NO: 33, and LCDR3 of SEQ ID NO:34, and a light chain constant region,

wherein a C-terminus of the heavy chain is attached to at least one single-chain antibody via a first linker fragment,

wherein the at least one single-chain antibody comprises,

(i) a second heavy chain variable region comprising HCDR1 of SEQ ID NO: 35, HCDR2 of SEQ ID NO: 36, and HCDR3 of SEQ ID NO: 37, and a second light chain variable region comprising LCDR1 of SEQ ID NO: 38, LCDR2 of SEQ ID NO: 39, and LCDR3 of SEQ ID NO: 40;

(ii) a second heavy chain variable region comprising HCDR1 of SEQ ID NO: 35, HCDR2 of SEQ ID NO: 41, and HCDR3 of SEQ ID NO: 37, and a second light chain variable region comprising LCDR1 of SEQ ID NO: 38, LCDR2 of SEQ ID NO: 39, and LCDR3 of SEQ ID NO: 40; or

(iii) a second heavy chain variable region comprising HCDR1 of SEQ ID NO: 42, HCDR2 of SEQ ID NO: 43, and HCDR3 of SEQ ID NO: 44, and a second light chain variable region comprising LCDR1 of SEQ ID NO: 45, LCDR2 of SEQ ID NO: 46, and LCDR3 of SEQ ID NO: 47.