US 11,999,800 B2
Bispecific and tetravalent CD137 and FAP molecules for the treatment of cancer
Eric Borges, Biberach (DE); Pankaj Gupta, Scarsdale, NY (US); Daniel Christopher Rowe, Ridgefield, CT (US); Justin M. Scheer, Ridgefield, CT (US); Abdallah Souabni, Vienna (AT); Inigo Tirapu, Vienna (AT); and Joseph Ronald Tumang, Danbury, CT (US)
Assigned to Boehringer Ingelheim International GmbH, Ingelheim am Rhein (DE)
Filed by Boehringer Ingelheim International GmbH, Ingelheim am Rhein (DE)
Filed on May 18, 2021, as Appl. No. 17/323,844.
Claims priority of provisional application 63/037,241, filed on Jun. 10, 2020.
Claims priority of provisional application 63/026,883, filed on May 19, 2020.
Prior Publication US 2021/0363273 A1, Nov. 25, 2021
Int. Cl. C07K 16/40 (2006.01); A61K 39/00 (2006.01); A61P 35/00 (2006.01); C07K 16/28 (2006.01)
CPC C07K 16/40 (2013.01) [A61P 35/00 (2018.01); C07K 16/2878 (2013.01); A61K 2039/507 (2013.01); C07K 2317/31 (2013.01); C07K 2317/565 (2013.01); C07K 2317/622 (2013.01)] 48 Claims
 
1. A bispecific and tetravalent binding molecule having two antigen binding sites that bind specifically to CD137 (4-1BB Ligand Receptor, 4-1BB) and two antigen binding sites that bind specifically to Fibroblast Activation Protein (FAP) wherein each antigen binding site that binds specifically to CD137 (4-1BB Ligand Receptor) is part of an immunoglobulin molecule comprising a heavy chain variable region comprising heavy chain complementarity determining regions (CDRs) comprising the amino acid sequences of SEQ ID NO:295 (CDR1), SEQ ID NO:18 (CDR2) and SEQ ID NO: 9 (CDR3) and a light chain variable region comprising light chain CDRs comprising the amino acid sequences of SEQ ID NO:22 (CDR1), SEQ ID NO:23 (CDR2) and SEQ ID NO:14 (CDR3); and
the antigen binding sites that bind specifically to Fibroblast Activation Protein (FAP) each comprise single chain variable fragments (scFvs) comprising heavy chain CDRs comprising the amino acid sequences of SEQ ID NO:333 (CDR1), SEQ ID NO:144 (CDR2) and SEQ ID NO:145 (CDR3) and light chain CDRs comprising the amino acid sequences of SEQ ID NO:138 (CDR1), SEQ ID NO:139 (CDR2) and SEQ ID NO:140 (CDR3).