VEGF-Trap is a high-affinity VEGF blocker with potent antitumor effects. It is a soluble decoy receptor created by fusing the first three Ig domains of VEGF receptor 1 (VEGFR1) to the constant region of human IgG1. However, this fusion protein has poor in vivo pharmacokinetic properties. Researchers engineered a more effective VEGF-Trap by modifying the protein to reduce its positive charge and improve its pharmacokinetic profile. The resulting VEGF-Trap R1R2 has a significantly longer half-life and higher affinity for VEGF, making it more effective at blocking VEGF signaling. VEGF-Trap R1R2 effectively suppresses tumor growth and vascularization in vivo, resulting in stunted and almost completely avascular tumors. It is more effective than other VEGF blockers, such as monoclonal antibodies targeting the VEGF receptor. VEGF-Trap R1R2 also shows promise in treating various cancers and other diseases involving pathological angiogenesis, such as diabetic retinopathy and psoriasis. The VEGF-Trap R1R2 was tested in various in vitro and in vivo experiments, including binding assays, phosphorylation assays, and tumor growth experiments. It showed high affinity for VEGF and effectively blocked VEGF-induced phosphorylation of VEGFR2 and cell proliferation. In tumor growth experiments, VEGF-Trap R1R2 significantly inhibited the growth of various tumor cell lines, including melanoma, rhabdomyosarcoma, and glioma. VEGF-Trap R1R2 was also tested in acute hypotension experiments, where it effectively blocked VEGF-induced hypotension. It showed superior pharmacodynamic performance compared to the parental VEGF-Trap. Additionally, it was compared to a monoclonal antibody targeting VEGFR2, and it showed similar efficacy at much lower concentrations. The VEGF-Trap R1R2 is composed of entirely human sequences, which may reduce the risk of immunogenicity in human patients. It binds to all species of VEGF tested, making it a versatile reagent for use in various experimental animal models. The VEGF-Trap R1R2 is currently in human clinical trials for several different types of cancer.VEGF-Trap is a high-affinity VEGF blocker with potent antitumor effects. It is a soluble decoy receptor created by fusing the first three Ig domains of VEGF receptor 1 (VEGFR1) to the constant region of human IgG1. However, this fusion protein has poor in vivo pharmacokinetic properties. Researchers engineered a more effective VEGF-Trap by modifying the protein to reduce its positive charge and improve its pharmacokinetic profile. The resulting VEGF-Trap R1R2 has a significantly longer half-life and higher affinity for VEGF, making it more effective at blocking VEGF signaling. VEGF-Trap R1R2 effectively suppresses tumor growth and vascularization in vivo, resulting in stunted and almost completely avascular tumors. It is more effective than other VEGF blockers, such as monoclonal antibodies targeting the VEGF receptor. VEGF-Trap R1R2 also shows promise in treating various cancers and other diseases involving pathological angiogenesis, such as diabetic retinopathy and psoriasis. The VEGF-Trap R1R2 was tested in various in vitro and in vivo experiments, including binding assays, phosphorylation assays, and tumor growth experiments. It showed high affinity for VEGF and effectively blocked VEGF-induced phosphorylation of VEGFR2 and cell proliferation. In tumor growth experiments, VEGF-Trap R1R2 significantly inhibited the growth of various tumor cell lines, including melanoma, rhabdomyosarcoma, and glioma. VEGF-Trap R1R2 was also tested in acute hypotension experiments, where it effectively blocked VEGF-induced hypotension. It showed superior pharmacodynamic performance compared to the parental VEGF-Trap. Additionally, it was compared to a monoclonal antibody targeting VEGFR2, and it showed similar efficacy at much lower concentrations. The VEGF-Trap R1R2 is composed of entirely human sequences, which may reduce the risk of immunogenicity in human patients. It binds to all species of VEGF tested, making it a versatile reagent for use in various experimental animal models. The VEGF-Trap R1R2 is currently in human clinical trials for several different types of cancer.