US 11,939,381 B2
Bispecific antibodies targeting immune checkpoints
Stephen J. Demarest, San Diego, CA (US); Yiqing Feng, Carmel, IN (US); Juqun Shen, San Diego, CA (US); Yang Shen, Scarsdale, NY (US); and Stephanie Marie Truhlar, Carlsbad, CA (US)
Assigned to Eli Lilly and Company, Indianapolis, IN (US)
Appl. No. 17/258,348
Filed by Eli Lilly and Company, Indianapolis, IN (US)
PCT Filed Jul. 12, 2019, PCT No. PCT/US2019/041517
§ 371(c)(1), (2) Date Jan. 6, 2021,
PCT Pub. No. WO2020/018354, PCT Pub. Date Jan. 23, 2020.
Claims priority of provisional application 62/799,274, filed on Jan. 31, 2019.
Claims priority of provisional application 62/700,525, filed on Jul. 19, 2018.
Prior Publication US 2021/0292416 A1, Sep. 23, 2021
Int. Cl. C07K 16/28 (2006.01); A61K 39/00 (2006.01)
CPC C07K 16/2818 (2013.01) [C07K 16/2878 (2013.01); A61K 2039/505 (2013.01); C07K 2317/31 (2013.01); C07K 2317/34 (2013.01); C07K 2317/75 (2013.01); C07K 2317/76 (2013.01); C07K 2317/92 (2013.01)] 20 Claims
 
1. An antibody that antagonizes human PD-1 (SEQ ID NO:25) and agonizes human CD137 (SEQ ID NO:26), comprising a first and second heavy chain and a first and second light chain, wherein each chain comprises a variable region and a constant region, and wherein:
a) the first heavy chain of the antibody comprises a complementarity-determining region 1 (CDR1) having the amino acid sequence of SEQ ID NO:1, a complementarity-determining region 2 (CDR2) having the amino acid sequence of SEQ ID NO:2, and a complementarity-determining region (CDR3) having the amino acid sequence of SEQ ID NO:3;
b) the first light chain of the antibody comprises a CDR1 having the amino acid sequence of SEQ ID NO:7, a CDR2 having the amino acid sequence of SEQ ID NO:8, and a CDR3 having the amino acid sequence of SEQ ID NO:9;
c) the second heavy chain of the antibody comprises a CDR1 having the amino acid sequence of SEQ ID NO:13, a CDR2 having the amino acid sequence of SEQ ID NO:14, and a CDR3 having the amino acid sequence of SEQ ID NO:15; and
d) the second light chain of the antibody comprises a CDR1 having the amino acid sequence of SEQ ID NO:19, a CDR2 having the amino acid sequence of SEQ ID NO:20, and a CDR3 having the amino acid sequence of SEQ ID NO:21.