14 / 56
Ramucirumab (IMC-1121B):
A Fully Human VEGF Receptor-2 Antagonist
•
Isolated from phage display library of human Fab fragments from non-immunized
donors
1
•
Fully human anti-VEGFR-2 IgG
1
monoclonal antibody
1
•
High affinity (KD = 50 pM)
1
•
Blocks VEGF binding to VEGFR-2
•
(IC
50
= 0.8 nM)
1
1
. Lu D et al.
J Biol Chem
.2003;278(44):43496-43507.
2. Miao H-Q et al.
Biochem Biophys Res Commun.
2006;345:438-445
.
3.Zhu Z et al.
Leukemia
. 2003;17:604-611
.
•
Biochemical and anti-tumor effects
–
Inhibits ligand-dependent VEGFR-2 activation and signaling
1
–
Inhibits proliferation and migration of human endothelial cells
2
–
Direct anti-tumor effect in NOD-SCID mice inoculated with VEGFR-2
+
HL60 leukemic cells
3