RT Journal Article SR Electronic T1 Phase 0 Microdosing PET Study Using the Human Mini Antibody F16SIP in Head and Neck Cancer Patients JF Journal of Nuclear Medicine JO J Nucl Med FD Society of Nuclear Medicine SP 397 OP 401 DO 10.2967/jnumed.112.111310 VO 54 IS 3 A1 Derrek A. Heuveling A1 Remco de Bree A1 Danielle J. Vugts A1 Marc C. Huisman A1 Leonardo Giovannoni A1 Otto S. Hoekstra A1 C. René Leemans A1 Dario Neri A1 Guus A.M.S. van Dongen YR 2013 UL http://jnm.snmjournals.org/content/54/3/397.abstract AB 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 124I, 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: 124I-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 124I-F16SIP. Conclusion: Performing a microdosing immuno-PET study appeared feasible and demonstrated adequate bioavailability and selective tumor targeting of 124I-F16SIP.The results of this study justify further clinical exploration of 124I-F16SIP-based therapies.