Drug intelligence / Profile preview

DOTA-CycMSH

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

Overview

DOTA-CycMSH is a **radiolabeled peptide drug** that combines a DOTA chelator (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) with a cyclized α-melanocyte-stimulating hormone (α-MSH) analog[3]. It is designed to target the **melanocortin 1 receptor (MC1R)**, which is highly expressed on melanoma cells. Upon radiolabeling, such as with ^225Ac, ^111In, ^67Ga, or ^177Lu, DOTA-CycMSH functions either as a diagnostic imaging agent or as a targeted radiotherapeutic for melanoma[1][3]. Its mechanism relies on high-affinity, receptor-mediated binding to MC1R, rapid internalization into melanoma cells, and prolonged tumor retention, enabling selective imaging and/or therapy[1][3].

Other names
DOTA-modified cyclized α-melanocyte-stimulating hormoneDOTA-CycMSH
02

Targets

MC1R (Melanocortin Type 1 Receptor)

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