177Lu-FVIIai

177Lu-FVIIai is a tissue factor (TF)-targeted radionuclide therapy consisting of the beta-emitting radioisotope lutetium-177 (177Lu) conjugated to an active site-inhibited version of recombinant human Factor VIIa (FVIIai). Tissue factor is a transmembrane glycoprotein that is frequently overexpressed in various solid tumors, including pancreatic cancer, where it contributes to tumor progression, metastasis, and angiogenesis. FVIIai acts as a high-affinity targeting ligand for TF; however, because its active site is chemically inhibited, it does not trigger the extrinsic coagulation pathway, thereby minimizing the risk of systemic thrombosis. Upon binding to TF on the surface of cancer cells, the 177Lu payload delivers localized ionizing radiation, leading to DNA double-strand breaks and tumor cell death. Preclinical studies in pancreatic cancer xenograft models have demonstrated that 177Lu-FVIIai can significantly inhibit tumor growth and improve survival. The agent was developed through a collaboration involving Minerva Imaging, the Technical University of Denmark, and the University of Copenhagen.

Other names

lutetium-177 labeled active site inhibited factor VIIalutetium177 labeled active site inhibited factor VIIalutetium 177 labeled active site inhibited factor VIIa177Lu-labeled FVIIai