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Lu-DOTA-RM2
- Development stage
- Unknown
- Lead developer
- Lantheus
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
Lu-DOTA-RM2 is a radiopharmaceutical composed of the GRPR (gastrin-releasing peptide receptor) antagonist peptide RM2, conjugated with DOTA and labeled with the beta-emitting radioisotope Lutetium-177. It is designed for targeted radiotherapy of cancers that overexpress GRPR, such as prostate and breast cancer. The mechanism involves high-affinity binding to GRPR on tumor cells, delivering localized radiation to induce cytotoxicity while sparing most normal tissues due to rapid clearance from non-target organs. Preclinical and early clinical studies have shown high tumor uptake, favorable dosimetry, and promising safety profiles. Lu-DOTA-RM2 is being developed as part of a theranostic pair alongside 68Ga-DOTA-RM2 for diagnostic imaging[1][4][6].
- Other names
- RM2 (when referring to the radiolabeled peptide)DOTA-conjugated RM2
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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