NT4-methotrexate

NT4-methotrexate (NT4-MTX) is a preclinical peptide-drug conjugate (PDC) consisting of the tetra-branched neurotensin-derived peptide NT4 conjugated to the cytotoxic folate antagonist methotrexate (MTX). Developed by SetLance and researchers at the University of Siena, NT4-methotrexate is designed to selectively target cancer cells by binding to sulfated glycosaminoglycans (sGAGs), particularly heparan sulfate, and low-density lipoprotein receptor-related proteins (LRP1 and LRP6) on tumor cell membranes. Upon binding, the conjugate is internalized, delivering methotrexate intracellularly to inhibit dihydrofolate reductase (DHFR), thereby bypassing drug resistance mechanisms such as those mediated by the loss of the reduced folate carrier (RFC). It has demonstrated significant tumor growth reduction in preclinical xenograft models of colorectal, breast, and bladder cancers.

Other names

NT4-MTX conjugateNT-4-MTX conjugateNT 4-MTX conjugateNT4-conjugated methotrexateNT-4-conjugated methotrexateNT 4-conjugated methotrexatemethotrexate-conjugated NT4