摘要 |
The present invention relates to compounds that bind to human vascular endothelial growth factor receptor-2 (VEGFR2) and human angiopoietin-2 (Ang2), and may be useful for treating cancer, especially solid tumors driven by VEGFR2 and Ang2, including gastric, hepatocellular carcinoma, ovarian, colorectal, non-small cell lung, biliary tract, and breast cancers. |
主权项 |
1. A compound, comprising an antibody fused by two linkers to two single chain fragment variable (scFv) polypeptides, wherein:
a) the antibody comprises two identical heavy chains (HCs) and two identical light chains (LCs), wherein each HC comprises a heavy chain variable region (HCVR) whose amino acid sequence is given in SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, or SEQ ID NO: 4, and wherein each LC comprises a light chain variable region (LVCR) whose amino acid sequence is given in SEQ ID NO: 13, SEQ ID NO: 14, or SEQ ID NO: 15, b) the two scFv polypeptides are identical and each comprise an HCVR operably linked to an LCVR, wherein each HCVR has the amino acid sequence given in SEQ ID NO: 21, or SEQ ID NO: 22, and wherein each LCVR has the amino acid sequence given in SEQ ID NO: 23, or SEQ ID NO: 24, and c) the two linkers are identical glycine-rich linkers that each operably link the carboxy-terminus of one HC of the antibody to the amino-terminus of one of the scFv polypeptides. |