PT - JOURNAL ARTICLE AU - Suraiya R. Dubash AU - Nicholas Keat AU - Paola Mapelli AU - Frazer Twyman AU - Laurence Carroll AU - Kasia Kozlowski AU - Adil Al-Nahhas AU - Azeem Saleem AU - Mickael Huiban AU - Ryan Janisch AU - Andrea Frilling AU - Rohini Sharma AU - Eric O. Aboagye TI - Clinical Translation of a Click-Labeled <sup>18</sup>F-Octreotate Radioligand for Imaging Neuroendocrine Tumors AID - 10.2967/jnumed.115.169532 DP - 2016 Aug 01 TA - Journal of Nuclear Medicine PG - 1207--1213 VI - 57 IP - 8 4099 - http://jnm.snmjournals.org/content/57/8/1207.short 4100 - http://jnm.snmjournals.org/content/57/8/1207.full SO - J Nucl Med2016 Aug 01; 57 AB - We conducted the first-in-human study of 18F-fluoroethyl triazole [Tyr3] octreotate (18F-FET-βAG-TOCA) in patients with neuroendocrine tumors (NETs) to evaluate biodistribution, dosimetry, and safety. Despite advances in clinical imaging, detection and quantification of NET activity remains a challenge, with no universally accepted imaging standard. Methods: Nine patients were enrolled. Eight patients had sporadic NETs, and 1 had multiple endocrine neoplasia type 1 syndrome. Patients received 137–163 MBq (mean ± SD, 155.7 ± 8 MBq) of 18F-FET-βAG-TOCA. Safety data were obtained during and 24 h after radioligand administration. Patients underwent detailed whole-body PET/CT multibed scanning over 4 h with sampling of venous bloods for radioactivity and radioactive metabolite quantification. Regions of interest were defined to derive individual and mean organ residence times; effective dose was calculated with OLINDA 1.1. Results: All patients tolerated 18F-FET-βAG-TOCA with no adverse events. Over 60% parent radioligand was present in plasma at 60 min. High tumor (primary and metastases)-to-background contrast images were observed. Physiologic distribution was seen in the pituitary, salivary glands, thyroid, and spleen, with low background distribution in the liver, an organ in which metastases commonly occur. The organs receiving highest absorbed dose were the gallbladder, spleen, stomach, liver, kidneys, and bladder. The calculated effective dose over all subjects (mean ± SD) was 0.029 ± 0.004 mSv/MBq. Conclusion: The favorable safety, imaging, and dosimetric profile makes 18F-FET-βAG-TOCA a promising candidate radioligand for staging and management of NETs. Clinical studies in an expanded cohort are ongoing to clinically qualify this agent.