[18F]PRIMATX, a New Positron Emission Tomography Tracer for Imaging of Autotaxin in Lung Tissue and Tumor‐Bearing Mice. (30th July 2019)

• Record Type: Journal Article
• Authors: Briard, Emmanuelle; Joshi, Aniket D.; Shanmukhappa, Shiva; Ilovich, Ohad; Auberson, Yves P.
• Is Part Of: ChemMedChem. Volume 14:Number 16(2019)
• Page Start: 1493
• Page End: 1502
• Publication Date: 2019-07-30
• Subjects: enzymes -- fibrosis -- fluorinated ligands -- imaging agents -- oncology; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201900297
• Languages: English
• ISSNs: 1860-7179

Abstract

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 [ 18 F]( R, E )‐3‐(4‐chloro‐2‐((5‐methyl‐2 H ‐tetrazol‐2‐yl)methyl)phenyl)‐1‐(4‐((5‐(2‐fluoroethoxy)pyridin‐2‐yl)methyl)‐2‐methylpiperazin‐1‐yl)prop‐2‐en‐1‐one ([ 18 F]PRIMATX, [ 18 F]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. Abstract : PRIMATX is a novel PET tracer for imaging the secreted enzyme autotaxin (ATX). It proved sensitive to fibrosis‐associated ATX expression in fibrotic lung tissue from idiopathic pulmonary fibrosis patients, and allows the detection of ATX‐expressing melanoma tumors in living mice with a good signal‐to‐noise ratio. This study provides a potential diagnostic tool for clinical development, and confirms the relevance of ATX for this purpose.