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[177Lu]Lu-DOTA-MGS5
- Development stage
- Unknown
- Lead developer
- Erasmus MC
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
[177Lu]Lu-DOTA-MGS5 is a **radiolabeled minigastrin analog** designed for **peptide receptor radionuclide therapy (PRRT)** targeting the **cholecystokinin-2 receptor (CCK2R)**, which is overexpressed in several cancers including medullary thyroid carcinoma (MTC), small cell lung cancer (SCLC), and other neuroendocrine tumors. The agent consists of a minigastrin-derived peptide (MGS5) conjugated via DOTA chelator to the **beta-emitting isotope Lutetium-177 (177Lu)**. It delivers targeted radiation by binding specifically to CCK2R-expressing tumor cells, which results in localized cytotoxicity. Preclinical studies and preliminary clinical dosimetry indicate high **receptor affinity**, excellent **radiochemical purity** (>98%), favorable **biodistribution** (notably high and persistent tumor uptake, low background), and manageable toxicity profile, supporting its clinical development for PRRT in advanced, CCK2R-positive malignancies[1][2][3].
- Other names
- DOTA-MGS5DOTA-MGS-5DOTA-MGS 5Lu-177 DOTA-MGS5Lu177 DOTA-MGS5Lu 177 DOTA-MGS5
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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