Drug intelligence / Profile preview

225Ac-scrambled-MC1RL-DOTA

Development stage
Preclinical
Lead developer
H. Lee Moffitt Cancer Center & Research Institute
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

225Ac-scrambled-MC1RL-DOTA is a radiolabeled control peptide used in preclinical research for targeted alpha-particle therapy. It consists of the alpha-emitting radionuclide Actinium-225 (225Ac) chelated by DOTA and conjugated to a scrambled sequence of the melanocortin 1 receptor (MC1R) ligand (MC1RL). In studies evaluating 225Ac-MC1RL-DOTA for the treatment of uveal and cutaneous melanoma, this scrambled version serves as a negative control to demonstrate that the therapeutic efficacy of the lead compound is dependent on specific binding to the MC1R receptor. It was developed by researchers at the H. Lee Moffitt Cancer Center & Research Institute in collaboration with Wake Forest University and West Virginia University.

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