Published in:
01-05-2015 | Image of the Month
[177Lu]Lutetium-labelled PSMA ligand-induced remission in a patient with metastatic prostate cancer
Authors:
Clemens Kratochwil, Frederik L. Giesel, Matthias Eder, Ali Afshar-Oromieh, Martina Benešová, Walter Mier, Klaus Kopka, Uwe Haberkorn
Published in:
European Journal of Nuclear Medicine and Molecular Imaging
|
Issue 6/2015
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Excerpt
The prostate-specific membrane antigen (PSMA) shows intense overexpression in the majority of prostate cancers (PCa) [
1]. A Glu-urea-Lys motif has been found to bind with high affinity to the catalytic domain of PSMA [
2]. Following conjugation to the chelator HBED-CC, a
68Ga-labelled PSMA ligand (
68Ga-DKFZ-11) has been derived as a novel PET tracer [
3]. Since PSMA is internalized after binding of a ligand [
4], it is also an excellent target for systemic radionuclide therapy. Consequently, a
131I-labelled PSMA ligand (
131I-MIP-1095) demonstrated favourable tumour-targeting properties and promising antitumour efficacy [
5]. However, clinical application of
131I causes a high radiation burden and is hampered by complex regulations in most countries. Therefore,
177Lu is considered to be preferable for targeted radionuclide therapy. The novel theranostic drug
177Lu-DKFZ-617 is a DOTA derivative of the Glu-urea-Lys motif. The chelator is conjugated via an aromatic linker that further improves tumour accumulation while simultaneously reducing kidney uptake. …