UNLABELLED: 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. CONCLUSION: 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.
UNLABELLED: 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. CONCLUSION: 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: Marcus Franz; Monika Matusiak-Brückner; Petra Richter; Katja Grün; Barbara Ziffels; Dario Neri; Hansjörg Maschek; Uwe Schulz; Alexander Pfeil; Christian Jung; Hans R Figulla; Jan Gummert; Alexander Berndt; André Renner Journal: J Mol Histol Date: 2014-05-03 Impact factor: 2.611
Authors: Luigi Aloj; Laura D'Ambrosio; Michela Aurilio; Anna Morisco; Ferdinando Frigeri; Corradina Caraco'; Francesca Di Gennaro; Gaetana Capobianco; Leonardo Giovannoni; Hans D Menssen; Dario Neri; Antonio Pinto; Secondo Lastoria Journal: Eur J Nucl Med Mol Imaging Date: 2014-01-17 Impact factor: 9.236