Bispecific Antibodies Anti-VEGF and Anti-PD-1 and Their Uses

Claims

Bispecific antibodies containing an anti-VEGF binding region conjugated to an anti-PD-1 binding region and uses thereof for cancer treatment.

1. A bispecific binding protein, characterized in that it comprises one or more anti-VEGF binding regions and one or more anti-PD-1 binding regions.

32. A pharmaceutical composition, characterized in that it comprises the bispecific binding protein of claim 1 and a pharmaceutically acceptable excipient.

50. A bispecific binding protein, characterized in that it comprises one or more anti-VEGF binding regions and one or more anti-PD-1 binding regions, wherein the bispecific binding protein comprises a single-chain variable fragment (scFv) comprising an anti-VEGF binding region and an anti-PD-1 binding region, and an anti-VEGF light chain, wherein the anti-VEGF light chain forms a complex with the scFv, wherein: (a) the scFv comprises an anti-VEGF heavy chain region, a first linker, an anti-PD-1 heavy chain variable region, a second linker, and an anti-PD-1 light chain region, wherein: (i) the anti-VEGF heavy chain region comprises an anti-VEGF heavy chain variable region comprising the sequence shown in SEQ ID No. 3 linked at its C-terminal end to a heavy chain constant region comprising the sequence shown in the SEQ ID No. 51;(ii) the first connector comprises the sequence shown in SEQ ID No. 57, wherein the first connector joins the C-terminal end of the anti-VEGF heavy chain region to the anti-PD-1 heavy chain variable region; (iii) the anti-PD-1 heavy chain variable region comprises the sequence shown in SEQ ID No. 54; (iv) the second connector comprises the sequence shown in SEQ ID No. 58, wherein the second connector joins the C-terminal end of the anti-PD-1 heavy chain variable region to the anti-PD-1 light chain region; and (v) the anti-PD-1 light chain region optionally comprises the sequence shown in SEQ ID No. 53, wherein the scFv comprises the sequence shown in SEQ ID No. 61;and (b) the anti-VEGF light chain comprises a variable region of the anti-VEGF light chain comprising the sequence shown in SEQ ID No. 4 joined at its C-terminal end to a constant region of the light chain comprising the sequence shown in SEQ ID No. 52.;