Drug intelligence / Profile preview

[99mTc]Tc(CO)3-NOTA-AocNle-CycMSHhex

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

Overview

A radiopharmaceutical imaging agent consisting of a **tricarbonyl technetium-99m ([99mTc]Tc(CO)3) complex chelated by a NOTA ligand** and conjugated to a **lactam-cyclized alpha-melanocyte-stimulating hormone (α-MSH) hexapeptide analog** (AocNle-CycMSHhex). This compound selectively binds to the **melanocortin-1 receptor (MC1R)**, which is highly expressed on melanoma cells. It is designed for **SPECT imaging of melanoma lesions** due to its high tumor uptake, fast urinary clearance, and low kidney accumulation. The drug was developed using Fmoc chemistry and demonstrates MC1R-specific binding with high affinity in vitro (IC50 ~ 0.8 nM). Preclinical studies showed clear visualization of melanoma lesions in mice, highlighting its utility as a **diagnostic radiopharmaceutical** for **melanoma** imaging[1].

Other names
99mTc(CO)3-NOTA-GGNle-CycMSHhex
02

Targets

MC1R (Melanocortin Type 1 Receptor)

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