Drug intelligence / Profile preview

copper-64-diacetyl-bis(N4-methylthiosemicarbazone)

Development stage
Phase 2
Lead developer
Linqmed
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Copper-64-diacetyl-bis(N4-methylthiosemicarbazone)** is a radiopharmaceutical compound primarily developed for imaging and therapy of hypoxic tumors. The compound, also called 64Cu-ATSM, is a copper-64-labeled bis(thiosemicarbazone) complex that selectively accumulates in hypoxic cells within solid tumors due to its redox chemistry and membrane permeability. Once internalized in hypoxic cells, 64Cu-ATSM undergoes reduction and is trapped, enabling selective PET imaging of hypoxic regions as well as targeted radiotherapy. Mechanistically, hypoxia-selectivity is conferred by the electronic structure of the ligand, which influences redox behavior and cell retention. Radiotoxicity is mediated both by β-decay and emission of Auger electrons, especially when copper-64 localizes near nuclear DNA[2][3][4][5][6]. The developer of 64Cu-ATSM as an imaging and therapeutic agent is Washington University School of Medicine, with early contributions from Fukui Medical University.

Other names
copper(II)-diacetyl-bis(N4-methylthiosemicarbazone)Cu(II)ATSM64Cu-ATSMcopper-64-ATSMcopper64-ATSMcopper 64-ATSM64Cu-diacetyl-bis(N4-methylthiosemicarbazone)

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