UNLABELLED: We conducted the first-in-human study of (18)F-fluoroethyl triazole [Tyr(3)] octreotate ((18)F-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 (18)F-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 (18)F-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 (18)F-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.
UNLABELLED: We conducted the first-in-human study of (18)F-fluoroethyl triazole [Tyr(3)] octreotate ((18)F-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 (18)F-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 (18)F-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 (18)F-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.
Authors: Ksenia Lisova; Maxim Sergeev; Susan Evans-Axelsson; Andreea D Stuparu; Seval Beykan; Jeffrey Collins; Jason Jones; Michael Lassmann; Ken Herrmann; David Perrin; Jason T Lee; Roger Slavik; R Michael van Dam Journal: Nucl Med Biol Date: 2018-04-20 Impact factor: 2.408
Authors: Verena I Böhmer; Wiktor Szymanski; Keimpe-Oeds van den Berg; Chantal Mulder; Piermichele Kobauri; Hugo Helbert; Dion van der Born; Friederike Reeβing; Anja Huizing; Marten Klopstra; Douwe F Samplonius; Ines F Antunes; Jürgen W A Sijbesma; Gert Luurtsema; Wijnand Helfrich; Ton J Visser; Ben L Feringa; Philip H Elsinga Journal: Chemistry Date: 2020-07-21 Impact factor: 5.236
Authors: Jason M Tarkin; Christopher Wall; Deepa Gopalan; Luigi Aloj; Roido Manavaki; Tim D Fryer; Eric O Aboagye; Martin R Bennett; James E Peters; James H F Rudd; Justin C Mason Journal: Circ Cardiovasc Imaging Date: 2020-05-28 Impact factor: 7.792
Authors: Suraiya R Dubash; Nicholas Keat; Kasia Kozlowski; Chris Barnes; Louis Allott; Diana Brickute; Sam Hill; Mickael Huiban; Tara D Barwick; Laura Kenny; Eric O Aboagye Journal: Eur J Nucl Med Mol Imaging Date: 2020-03-02 Impact factor: 9.236