drug_type
RELEVANT_DRUG
intervention_type
Radiopharmaceutical (therapeutic)
drug_description
MC1R-targeted peptide radiopharmaceutical delivering alpha-particle therapy via 212Pb decay (212Pb→212Bi/212Po) to induce short-range, high-LET DNA double-strand breaks in melanoma cells; administered IV approximately every 8 weeks as mono- or combination therapy.
nci_thesaurus_concept_id
C199480
nci_thesaurus_preferred_term
Lead Pb 212-VMT01
nci_thesaurus_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.
drug_mesh_term
Radiopharmaceuticals
drug_category
RADIOPEPTIDE CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
MC1R-targeted peptide (VMT01) delivers the alpha-emitting radionuclide 212Pb (decaying via 212Bi/212Po) to MC1R-expressing tumor cells, producing short-range, high-LET alpha radiation that induces clustered DNA double-strand breaks and tumor cell death.
drug_name
[212Pb]VMT01
nct_id_drug_ref
NCT05655312