N4-CO-Re(Arg11)CCMSH

N4-CO-Re(Arg11)CCMSH is a synthetic, cyclic melanotropin peptide analogue designed for molecular imaging and targeted radionuclide therapy in melanoma. It is based on the core structure of cyclic [Cys, Cys, Glu, His, Arg, Ser, His, Phe, Arg, Trp, Arg]-α-melanocyte-stimulating hormone (α-MSH) variant, with cyclization through rhenium (Re) coordination and chemical modification at the N-terminus with an N4-CO group for improved stability and radiolabeling. The drug is radiolabeled with technetium-99m (for SPECT imaging) and demonstrates tumor selectivity by targeting melanocortin 1 receptor (MC1R), which is highly expressed on melanoma cells. Key mechanistic features include strong internalization and retention in MC1R-positive tumor cells and rapid clearance from non-target tissues. The agent is investigated for use as a diagnostic and potentially therapeutic radiopharmaceutical for melanoma. Primary developer cited is the Biochemistry Department, University of Missouri, with lead researcher Thomas P. Quinn.

Other names

N4-CO-Re(Arg11)CCMSH