177Lu-NMG2

177Lu-NMG2 is a radiolabeled peptidomimetic and minigastrin analog developed for the targeted imaging and therapy of tumors overexpressing the cholecystokinin-2 receptor (CCK2R), such as medullary thyroid cancer (MTC) and small cell lung cancer (SCLC). It is a derivative of the clinical-stage compound PP-F11N, modified by the substitution of a specific amide bond with a 1,4-disubstituted 1,2,3-triazole bioisostere at the Tyr12-Gly13 position. This structural modification is designed to enhance receptor affinity and improve tumor-targeting properties. The molecule consists of the beta-emitting radionuclide lutetium-177 complexed by a DOTA chelator, linked to a peptide sequence containing a hexa-D-glutamate moiety for enhanced metabolic stability. Preclinical evaluations have shown that 177Lu-NMG2 exhibits high tumor uptake, slow tumor washout, and favorable tumor-to-kidney ratios, making it a promising candidate for peptide receptor radionuclide therapy (PRRT).

Other names

177Lu-labeled NMG 2triazolominigastrin analog