Dosimetry and pharmacokinetics of [ 177 Lu]Lu-satoreotide tetraxetan in patients with progressive neuroendocrine tumours
European Journal of Nuclear Medicine and Molecular Imaging(2024)
摘要
Purpose To evaluate the dosimetry and pharmacokinetics of the novel radiolabelled somatostatin receptor antagonist [ 177 Lu]Lu-satoreotide tetraxetan in patients with advanced neuroendocrine tumours (NETs). Methods This study was part of a phase I/II trial of [ 177 Lu]Lu-satoreotide tetraxetan, administered at a median cumulative activity of 13.0 GBq over three planned cycles (median activity/cycle: 4.5 GBq), in 40 patients with progressive NETs. Organ absorbed doses were monitored at each cycle using patient-specific dosimetry; the cumulative absorbed-dose limits were set at 23.0 Gy for the kidneys and 1.5 Gy for bone marrow. Absorbed dose coefficients (ADCs) were calculated using both patient-specific and model-based dosimetry for some patients. Results In all evaluated organs, maximum [ 177 Lu]Lu-satoreotide tetraxetan uptake was observed at the first imaging timepoint (4 h after injection), followed by an exponential decrease. Kidneys were the main route of elimination, with a cumulative excretion of 57–66% within 48 h following the first treatment cycle. At the first treatment cycle, [ 177 Lu]Lu-satoreotide tetraxetan showed a median terminal blood half-life of 127 h and median ADCs of [ 177 Lu]Lu-satoreotide tetraxetan were 5.0 Gy/GBq in tumours, 0.1 Gy/GBq in the bone marrow, 0.9 Gy/GBq in kidneys, 0.2 Gy/GBq in the liver and 0.8 Gy/GBq in the spleen. Using image-based dosimetry, the bone marrow and kidneys received median cumulative absorbed doses of 1.1 and 10.8 Gy, respectively, after three cycles. Conclusion [ 177 Lu]Lu-satoreotide tetraxetan showed a favourable dosimetry profile, with high and prolonged tumour uptake, supporting its acceptable safety profile and promising efficacy. Trial registration NCT02592707. Registered October 30, 2015.
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关键词
[177Lu]Lu-satoreotide tetraxetan,Somatostatin receptor antagonist,Neuroendocrine tumours,Dosimetry,Pharmacokinetics,Systemic radionuclide therapy
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