Definition

A radioconjugate composed of the melanocyte-stimulating hormone receptor (MSHR; melanocortin-1 receptor; MC1R; melanin-activating peptide receptor; melanotropin receptor)-targeting peptide, VMT01, conjugated to the alpha-emitting radioisotope lead Pb 212, with potential antineoplastic activity. Upon administration, lead Pb 212-VMT01 targets and binds to MC1R-expressing tumor cells. This allows for the specific delivery of a cytotoxic dose of alpha radiation to MC1R-expressing tumor cells. MC1R, a G protein-coupled receptor expressed by melanocytes that binds to melanocortins, is involved in regulating mammalian skin and hair color. It is upregulated on the surface of metastatic melanoma cells.