title: Phase 0 microdosing PET study using the human mini antibody F16SIP in head and neck cancer patients.
abstract: The aim of this microdosing phase 0 clinical study was to obtain initial information about pharmacokinetics, biodistribution, and specific tumor targeting of the antitenascin-C mini antibody F16SIP.
  
  
  METHODS
  Two milligrams of F16SIP, labeled with 74 MBq of (124)I, were intravenously administered to patients with head and neck cancer (n = 4) scheduled for surgery 5-7 d later. Immuno-PET scans were acquired at 30 min and 24 h after injection. For pharmacokinetic analysis, blood samples were taken at different time points after infusion. Tissue uptake was extracted from whole-body PET scans. In addition, ex vivo radioactivity measurements of blood and of biopsies from the surgical specimens were performed.
  
  
  RESULTS
  (124)I-F16SIP was well tolerated. Uptake was visible mainly in the liver, spleen, kidneys, and bone marrow and diminished over time. Tumor uptake increased over time, with all 4 tumors visible on 24-h PET images. The tumor-to-blood ratio was 7.7 ± 1.7 at the time of surgery. Pharmacokinetic analysis revealed good bioavailability of (124)I-F16SIP.
  
  
  CONCLUSIONS
  Performing a microdosing immuno-PET study appeared feasible and demonstrated adequate bioavailability and selective tumor targeting of (124)I-F16SIP.The results of this study justify further clinical exploration of (124)I-F16SIP-based therapies.
authors: Department of Otolaryngology/Head and Neck Surgery, VU University Medical Center, Amsterdam, The Netherlands.
authors: Derrek A
authors: DA
authors: Heuveling
authors: Remco
authors: R
authors: de Bree
authors: Danielle J
authors: DJ
authors: Vugts
authors: Marc C
authors: MC
authors: Huisman
authors: Leonardo
authors: L
authors: Giovannoni
authors: Otto S
authors: OS
authors: Hoekstra
authors: C René
authors: CR
authors: Leemans
authors: Dario
authors: D
authors: Neri
authors: Guus A M S
authors: GA
authors: van Dongen
mesh_terms: D000328:Adult; D000368:Aged; D000911:Antibodies, Monoclonal / Q000493:pharmacokinetics; D002294:Carcinoma, Squamous Cell / Q000098:blood supply / Q000000981:diagnostic imaging* / Q000378:metabolism; D006258:Head and Neck Neoplasms / Q000098:blood supply / Q000000981:diagnostic imaging* / Q000378:metabolism; D006801:Humans; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D008297:Male; D008875:Middle Aged; D009389:Neovascularization, Pathologic / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography / Q000379:methods*; D017434:Protein Structure, Tertiary; D011829:Radiation Dosage; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D019063:Tenascin / Q000737:chemistry / Q000276:immunology* / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D000911:Antibodies, Monoclonal; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D019063:Tenascin