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67Ga-DOTA-Lys(ALB)-GGNle-CycMSHhex

Development stage
Unknown
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

67Ga-DOTA-Lys(ALB)-GGNle-CycMSHhex is a **radiolabeled cyclic alpha-melanocyte stimulating hormone (α-MSH) peptide** specifically engineered for **melanoma imaging and potential targeted radionuclide therapy**. It utilizes a DOTA chelator for binding gallium-67, coupled to a cyclic hexapeptide analog of α-MSH via an albumin-binding moiety (Lys(ALB)), aiming to enhance pharmacokinetics by increasing blood retention and tumor targeting[3]. The peptide exhibits **high affinity** for the melanocortin-1 receptor (MC1R), which is highly overexpressed on melanoma cells but has limited expression in normal tissues, facilitating selective tumor imaging. Modifications such as albumin binding can reduce renal uptake and further improve tumor-to-background ratios. Developers have studied variants including 68Ga and 177Lu radiolabels, consistently showing robust melanoma targeting in preclinical models and first-in-human studies[2][3]. The main anticipated indication is the **detection and imaging of metastatic melanoma**, with investigational use for radionuclide therapy.

Other names
67Ga-DOTA-Lys(ALB)-GGNle-CycMSHhex
02

Targets

MC1R (Melanocortin Type 1 Receptor)

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