Vascular endothelial growth factor pathway inhibitor (null)

Vascular endothelial growth factor pathway inhibitors are a diverse group of therapeutic agents designed to block signaling through the vascular endothelial growth factor system—a key regulator responsible for new blood vessel formation (angiogenesis) under both normal physiological conditions and pathological states such as cancer. These therapies work by either neutralizing soluble forms of VEGF proteins or inhibiting their cell-surface receptors' activity—most notably receptor tyrosine kinases like VEGFR2. By disrupting these signals, they suppress tumor neovascularization required for solid tumor progression and metastasis. They are widely used across oncology indications—including colorectal cancer, renal cell carcinoma—and ophthalmology indications such as age-related macular degeneration. However, because they interfere with essential processes in healthy tissues too, their use is associated with significant cardiovascular and renal toxicities requiring careful management.

Other names

Anti-VEGF therapyVEGF inhibitorAnti–vascular endothelial growth factor therapyVSP inhibitor (VEGF signaling pathway inhibitor)

Mechanisms for drugs targeting this pathway include: Monoclonal antibodies binding to and neutralizing circulating VEGF ligands (e.g., bevacizumab); Antibody fragments binding selectively to isoforms of VEGF-A (e.g., ranibizumab); Soluble decoy receptors trapping multiple forms of VEGFs and placental growth factors ("VEGF trap," e.g., aflibercept); Small molecule inhibitors blocking intracellular tyrosine kinase activity of the receptors, especially on endothelial cells involved in angiogenesis (e.g., sunitinib, sorafenib).