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FL-091 is a novel small-molecule radioligand vector designed to target neurotensin receptor 1 (NTSR1) positive solid tumors. Overexpression of NTSR1 is associated with the progression of several cancers, including colorectal, breast, pancreatic, and head and neck cancers. FL-091 binds to NTSR1 with high affinity and acts as an antagonist. Its radioisotope complexes—most notably Lutetium-177 (177Lu-FL-091) and Actinium-225 (225Ac-FL-091)—demonstrate improved in vivo biodistribution profiles compared to other NTSR1-targeting agents, resulting in higher tumor uptake and faster clearance from normal tissues. Preclinical studies have shown that these properties translate into superior anti-tumor activity across multiple xenograft models without significant toxicity or weight loss in treated animals. The drug is being developed as a radionuclide drug conjugate for the treatment of various NTSR1-positive cancers[1][2][3][4][5][8].
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