NT4-5FdU

NT4-5FdU is a preclinical peptide-drug conjugate (PDC) consisting of the tetra-branched peptide NT4 conjugated to 5-fluorodeoxyuridine (5FdU, also known as floxuridine), a fluoropyrimidine chemotherapy agent. Developed by researchers at the University of Siena and its spinout SetLance, the NT4 peptide carrier is derived from the sequence of human neurotensin and acts as a tumor-selective delivery vehicle. It achieves cancer selectivity by binding to sulfated glycosaminoglycans (specifically heparan sulfate proteoglycans) and endocytic low-density lipoprotein receptor-related proteins (LRP1 and LRP6) overexpressed on cancer cell membranes. Upon binding, the conjugate is internalized, releasing the cytotoxic 5FdU payload which inhibits thymidylate synthase to disrupt DNA synthesis. In preclinical models, NT4-5FdU has demonstrated significant reduction of tumor growth in xenografts of colorectal cancer, pancreatic adenocarcinoma, and urinary bladder cancer compared to unconjugated 5FdU.

Other names

NT4-5-fluorodeoxyuridineNT-4-5-fluorodeoxyuridineNT 4-5-fluorodeoxyuridineNT4-floxuridineNT-4-floxuridineNT 4-floxuridinetetrabranched NT(8-13)-betaAla-K(PEG-5-fluorodeoxyuridine)