title: [(18)F]VM4-037 MicroPET Imaging and Biodistribution of Two In Vivo CAIX-Expressing Tumor Models.
abstract: OBJECTIVE
  [(18)F]VM4-037 was recently developed as a positron emission tomography (PET) tracer for the detection of carbonic anhydrase IX (CAIX), a tumor-specific protein upregulated under hypoxic conditions. In this study, the accumulation of [(18)F]VM4-037 was determined in two CAIX-expressing preclinical human tumor models.
  
  
  METHODS
  U373 and HT29 tumor-bearing animals were injected with [(18)F]VM4-037 and underwent microPET imaging up to 4 h post-injection (p.i.). Biodistribution throughout the different organs was assessed at 2 and 4 h p.i. using gamma counting.
  
  
  RESULTS
  MicroPET imaging showed high [(18)F]VM4-037 uptake in the abdominal region, and biodistribution revealed high radioactivity in the kidney, ileum, colon, liver, stomach, and bladder. Although high CAIX expression was confirmed in both tumor models, tumor uptake assessed with microPET and biodistribution experiments was comparable to background tissues.
  
  
  CONCLUSIONS
  In this study, [(18)F]VM4-037 does not specifically accumulate in CAIX-expressing tumors, indicating that the tracer is not suitable for the detection of CAIX.
authors.affiliation: Department of Radiation Oncology (MaastRO Lab), GROW-School for Oncology and Developmental Biology, Maastricht University Medical Centre, UNS 50/23, PO Box 616, 6200 MD, Maastricht, The Netherlands. sarah.peeters@maastrichtuniversity.nl.
authors.forename: Sarah G J A
authors.initials: SG
authors.lastname: Peeters
authors.affiliation: Department of Radiation Oncology (MaastRO Lab), GROW-School for Oncology and Developmental Biology, Maastricht University Medical Centre, UNS 50/23, PO Box 616, 6200 MD, Maastricht, The Netherlands.
authors.forename: Ludwig
authors.initials: L
authors.lastname: Dubois
authors.affiliation: Department of Radiation Oncology (MaastRO Lab), GROW-School for Oncology and Developmental Biology, Maastricht University Medical Centre, UNS 50/23, PO Box 616, 6200 MD, Maastricht, The Netherlands.
authors.forename: Natasja G
authors.initials: NG
authors.lastname: Lieuwes
authors.affiliation: Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1117, PO Box 7057, 1081 HV, Amsterdam, The Netherlands.
authors.forename: Dennis
authors.initials: D
authors.lastname: Laan
authors.affiliation: Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1117, PO Box 7057, 1081 HV, Amsterdam, The Netherlands.
authors.forename: Martien
authors.initials: M
authors.lastname: Mooijer
authors.affiliation: Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1117, PO Box 7057, 1081 HV, Amsterdam, The Netherlands.
authors.forename: Robert C
authors.initials: RC
authors.lastname: Schuit
authors.affiliation: Neurofarba Department, Sezione di Scienze Farmaceutiche and Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Vullo
authors.affiliation: Neurofarba Department, Sezione di Scienze Farmaceutiche and Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
authors.affiliation: Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1117, PO Box 7057, 1081 HV, Amsterdam, The Netherlands.
authors.forename: Jonas
authors.initials: J
authors.lastname: Eriksson
authors.affiliation: Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1117, PO Box 7057, 1081 HV, Amsterdam, The Netherlands.
authors.forename: Albert D
authors.initials: AD
authors.lastname: Windhorst
authors.affiliation: Department of Radiation Oncology (MaastRO Lab), GROW-School for Oncology and Developmental Biology, Maastricht University Medical Centre, UNS 50/23, PO Box 616, 6200 MD, Maastricht, The Netherlands.
authors.forename: Philippe
authors.initials: P
authors.lastname: Lambin
mesh_terms: D000951:Antigens, Neoplasm / Q000378:metabolism*; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases / Q000378:metabolism*; D045744:Cell Line, Tumor; D004151:Dipeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D057054:Molecular Imaging / Q000379:methods*; D009369:Neoplasms / Q000378:metabolism / Q000473:pathology*; D049268:Positron-Emission Tomography / Q000379:methods*; D013449:Sulfonamides / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: C000598170:3-(4-(2-fluoroethoxy)phenyl)-2-(3-methyl-2-(4-((2-sulfamoylbenzo(d)thiazol-6-yloxy)methyl)-1H-1,2,3-triazol-1-yl)butanamido)propanoic acid; D000951:Antigens, Neoplasm; D004151:Dipeptides; D013449:Sulfonamides; C089226:CA9 protein, human; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases
keywords: Biodistribution; CAIX; PET imaging; Preclinical; [18F]VM4-037