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177Lu-NMG3
- Development stage
- Preclinical
- Lead developer
- Paul Scherrer Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
177Lu-NMG3 is a radiopharmaceutical peptidomimetic designed for the targeted imaging and peptide receptor radionuclide therapy (PRRT) of tumors overexpressing the cholecystokinin-2 receptor (CCK2R), such as medullary thyroid cancer (MTC) and small cell lung cancer (SCLC). It is a structural analog of the clinical candidate PP-F11N, modified by the substitution of two amide bonds with metabolically stable 1,4-disubstituted 1,2,3-triazoles at the DGlu10-Ala11 and Tyr12-Gly13 positions. These bioisosteric replacements enhance the compound's binding affinity for CCK2R and improve its pharmacokinetic profile, resulting in higher tumor uptake and prolonged retention compared to earlier minigastrin derivatives. The molecule consists of a DOTA chelator complexed with the beta-emitting radioisotope Lutetium-177, conjugated to a modified minigastrin peptide sequence.
- Other names
- 177Lu-labeled NMG3triazolominigastrin 3triazolominigastrin3triazolominigastrin-3[177Lu]Lu-NMG3
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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