177Lu-NMG-1

177Lu-NMG-1 is a radiolabeled peptidomimetic analog of the minigastrin derivative PP-F11N, developed for the diagnosis and therapy of tumors overexpressing the cholecystokinin-2 receptor (CCK2R). It features a structural modification where a specific amide bond in the peptide backbone is replaced by a 1,4-disubstituted 1,2,3-triazole as a metabolically stable bioisostere. While part of a series of novel minigastrins (NMGs) designed to improve tumor-targeting properties, NMG-1 demonstrated lower receptor affinity (IC50 of 22.8 nM) and reduced cellular internalization compared to the clinical candidate PP-F11N in preclinical in vitro assays. It is primarily investigated for potential applications in medullary thyroid cancer (MTC) and small cell lung cancer (SCLC).

Other names

[177Lu]Lu-NMG-1