Phase 0 Microdosing PET Study Using the Human Mini Antibody F16SIP in Head and Neck Cancer Patients

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 I-124, 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: I-124-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 I-124-F16SIP. Conclusion: Performing a microdosing immuno-PET study appeared feasible and demonstrated adequate bioavailability and selective tumor targeting of I-124-F16SIP. The results of this study justify further clinical exploration of I-124-F16SIP-based therapies.