title: PET radiopharmaceuticals for imaging integrin expression: tracers in clinical studies and recent developments.
abstract: Noninvasive determination of integrin expression has become an interesting approach in nuclear medicine. Since the discovery of the first 18F-labeled cyclic RGD peptide as radiotracer for imaging integrin αvβ3 expression in vivo, there have been carried out enormous efforts to develop RGD peptides for PET imaging. Moreover, in recent years, additional integrins, including α5β1 and αvβ6 came into the focus of pharmaceutical radiochemistry. This review will discuss the tracers already evaluated in clinical trials and summarize the preliminary outcome. It will also give an overview on recent developments to further optimize the first-generation compounds such as [18F]Galacto-RGD. This includes recently developed 18F-labeling strategies and also new approaches in 68Ga-complex chemistry. Furthermore, the approaches to develop radiopharmaceuticals targeting integrin α5β1 and αvβ6 will be summarized and discussed.
authors.affiliation: Department of Nuclear Medicine, Innsbruck Medical University, Anichstraße 35, 6020 Innsbruck, Austria.
authors.forename: Roland
authors.identifier: 0000-0002-4665-7433
authors.initials: R
authors.lastname: Haubner
authors.affiliation: Molecular Imaging and Radiochemistry, Department of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, 91054 Erlangen, Germany.
authors.forename: Simone
authors.initials: S
authors.lastname: Maschauer
authors.affiliation: Molecular Imaging and Radiochemistry, Department of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, 91054 Erlangen, Germany.
authors.forename: Olaf
authors.identifier: 0000-0003-0247-3656
authors.initials: O
authors.lastname: Prante
mesh_terms: D003952:Diagnostic Imaging; D019788:Fluorodeoxyglucose F18; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000737:chemistry / Q000302:isolation & purification*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals; D014018:Tissue Distribution
chemical_list: D039302:Integrin alphaVbeta3; D019275:Radiopharmaceuticals; D019788:Fluorodeoxyglucose F18