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225Ac-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-MC1RL-DOTA is a targeted alpha-particle therapy (TAT) consisting of the alpha-emitting radionuclide actinium-225 (225Ac) conjugated to a melanocortin 1 receptor (MC1R) specific ligand (MC1RL) via a DOTA chelator. MC1R is highly expressed in approximately 94% of uveal melanomas and is also prevalent in cutaneous melanomas, while remaining absent in most normal tissues, providing a high therapeutic index. The agent delivers high-linear energy transfer (LET) alpha radiation to the tumor site, causing lethal double-strand DNA breaks. Preclinical studies have demonstrated high radiochemical purity, stability in human serum, and significant tumor growth delay or complete remission in mouse models of uveal and cutaneous melanoma with minimal systemic toxicity.
- Other names
- 225Ac-MC1RL
02
Targets
MC1R (Melanocortin Type 1 Receptor)
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