Drug intelligence / Profile preview

175Lu-DOTA-PSMA-GUL

Development stage
Preclinical
Lead developer
Cellbion
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

175Lu-DOTA-PSMA-GUL is a stable isotope-labeled analog of the therapeutic radiopharmaceutical 177Lu-DOTA-PSMA-GUL, designed for the treatment of prostate cancer. It serves as a non-radioactive surrogate used in pharmacokinetic and biodistribution studies to facilitate precise quantification via liquid chromatography-tandem mass spectrometry (LC-MS/MS). The molecule comprises a glutamate-urea-lysine (GUL) targeting moiety that specifically binds to Prostate-Specific Membrane Antigen (PSMA), which is highly overexpressed in prostate adenocarcinoma cells. The GUL domain is linked to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator complexed with a stable lutetium-175 ion. Preclinical evaluations in rat models have demonstrated that the compound exhibits a multi-exponential plasma decline with a short elimination half-life and is primarily excreted through the renal system, with significant accumulation in the kidneys and prostate.

Other names
Lutetium-175-DOTA-PSMA-GULLutetium175-DOTA-PSMA-GULLutetium 175-DOTA-PSMA-GULStable lutetium-labeled PSMA-targeted ligand
02

Targets

PSMA (Prostate-specific membrane antigen)

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