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actinium Ac 225-DOTA-MTI-201
- Development stage
- Unknown
- Lead developer
- Modulation Therapeutics
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
actinium Ac 225-DOTA-MTI-201 (also known as 225Ac-MTI-201) is a targeted alpha-particle radiopharmaceutical therapy developed by Modulation Therapeutics in collaboration with West Virginia University and Moffitt Cancer Center. It consists of a cyclic beta-hairpin peptidomimetic ligand that selectively targets the melanocortin-1 receptor (MC1R), conjugated via a DOTA chelator to the alpha-emitting radionuclide actinium-225 (225Ac). MC1R is highly overexpressed on the surface of uveal and cutaneous melanoma cells but has limited expression in normal tissues. Upon binding to MC1R, the radioconjugate is rapidly internalized, delivering highly localized, high-energy alpha radiation directly to the cancer cells, inducing lethal double-strand DNA breaks while sparing surrounding healthy tissues. actinium Ac 225-DOTA-MTI-201 is currently in Phase I clinical development for the treatment of metastatic uveal melanoma.
- Other names
- Actinium-225-labeled DOTA-conjugated peptideActinium225-labeled DOTA-conjugated peptideActinium 225-labeled DOTA-conjugated peptide
02
Targets
MC1R (Melanocortin Type 1 Receptor)
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