[18F]PRIMATX,a New Positron Emission Tomography Tracer for Imaging of Autotaxin in Lung Tissue and Tumor-Bearing Mice |
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| Authors: | Dr Emmanuelle Briard Dr Aniket D Joshi Dr Shiva Shanmukhappa Dr Ohad Ilovich Dr Yves P Auberson |
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| Affiliation: | 1. Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Novartis Pharma AG, Klybeckstrasse 141, 4057 Basel, Switzerland;2. Clinical and Translational Imaging, Novartis Pharmaceuticals, 45 Sidney Street, 1203K, Cambridge, MA, 01239 USA;3. Discovery and Investigative Safety, Preclincial Safety, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA, 01239 USA;4. inviCRO, LLC, 27 Dry Dock Avenue, 7th Floor West, Boston, MA, 02210 USA |
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| Abstract: | Autotaxin (ATX) is a secreted enzyme with tissue levels associated with tissue injury, which increase during wound healing and chronic fibrotic diseases. We selected 18F](R,E)-3-(4-chloro-2-((5-methyl-2H-tetrazol-2-yl)methyl)phenyl)-1-(4-((5-(2-fluoroethoxy)pyridin-2-yl)methyl)-2-methylpiperazin-1-yl)prop-2-en-1-one (18F]PRIMATX, 18F] 2 ), a tracer for positron emission tomography, to image ATX expression in vivo. It successfully differentiates expression levels in lung tissue samples from idiopathic pulmonary fibrosis patients, and allows the detection of ATX-expressing tumors in living mice, confirming its potential for development as a clinical imaging agent. |
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| Keywords: | enzymes fibrosis fluorinated ligands imaging agents oncology |
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