16D3

16D3 (also known as iVR1) is a synthetic hexapeptide that acts as a selective antagonist of Vascular Endothelial Growth Factor Receptor 1 (VEGFR1). Identified through phage display technology, 16D3 binds to the extracellular domain of VEGFR1, specifically blocking the interaction with its natural ligands, such as VEGF-A and Placental Growth Factor (PlGF). This inhibition prevents VEGFR1 phosphorylation and downstream signaling pathways that drive tumor angiogenesis, the recruitment of pro-tumorigenic monocyte-macrophages, and the stabilization of blood vessels by mural cells. Preclinical studies have demonstrated that 16D3 effectively reduces tumor growth and metastasis in colorectal cancer models, particularly when used in combination with chemotherapy like irinotecan. Additionally, it has shown potent anti-angiogenic activity in models of choroidal neovascularization, suggesting potential therapeutic utility in ocular diseases such as wet age-related macular degeneration.

Other names

inhibitor of VEGFR1