title: PET imaging with small-molecule tyrosine kinase inhibitors: TKI-PET.
abstract: The discovery and increased understanding of tumor targets has led to the development and approval of 12 small molecule tyrosine kinase inhibitors (TKIs). Despite tremendous efforts in TKI development, treatment efficacies with these therapeutics are still too low and improvements require a personalized medicine approach. Positron emission tomography (PET) with radiolabeled TKIs (TKI-PET) is a tracking, quantification and imaging method, which provides a unique understanding of the behavior of these drugs in vivo and of the interaction with their target(s). In this article we provide an overview of tracer synthesis and development because each TKI requires a tailor made approach. Moreover, we describe current preclinical work and the first proof-of-principle clinical studies on the application of TKI-PET, illustrating the potential of this approach for improving therapy efficacy and personalized cancer treatment.
authors: Department of Nuclear Medicine and PET Research, VU University Medical Center, Amsterdam, The Netherlands. p.slobbe@vumc.nl
authors: Paul
authors: P
authors: Slobbe
authors: Alex J
authors: AJ
authors: Poot
authors: Albert D
authors: AD
authors: Windhorst
authors: Guus A M S
authors: GA
authors: van Dongen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002986:Clinical Trials as Topic; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D049268:Positron-Emission Tomography / Q000379:methods*; D057285:Precision Medicine / Q000379:methods; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D019275:Radiopharmaceuticals; D011505:Protein-Tyrosine Kinases