Abstract
PurposeThe radiolabelled somatostatin analogue [177Lu]Lu-DOTA-EB-TATE binds to albumin via Evans blue, thereby increasing the residence time in the blood and potentially allowing more therapeutic agent to be absorbed into the target tissue during peptide receptor radionuclide therapy. It was tested in selected patients whether the substance is superior to [177Lu]Lu-DOTA-TOC.MethodsActivity kinetics in organs and tumours after [177Lu]Lu-DOTA-EB-TATE and [177Lu]Lu-DOTA-TOC were compared intraindividually in five patients with progressive somatostatin receptor-positive disease scheduled for radionuclide therapy.ResultsIn comparison to [177Lu]Lu-DOTA-TOC, tumour doses per administered activity were higher for [177Lu]Lu-DOTA-EB-TATE in 4 of 5 patients (median ratio: 1.7; range: 0.9 to 3.9), kidney doses (median ratio: 3.2; range: 1.6 to 9.8) as well as spleen doses (median ratio: 4.7; range 1.2 to 6.2) in all patients, and liver doses in 3 of 4 evaluable patients (median ratio: 4.0; range: 0.7 to 4.9). The tumour to critical organs absorbed dose ratios were higher after [177Lu]Lu-DOTA-TOC in 4 of 5 patients.ConclusionsPrior to a treatment with [177Lu]Lu-DOTA-EB-TATE, it should be assessed individually whether the compound is superior to established substances.
Highlights
High expression of somatostatin receptors allows for imaging and peptide receptor radionuclide therapy (PRRT) of neoplasms using radiolabelled somatostatin analogues like 90Yand 177Lu-labelled [DOTA0,Tyr3]-octreotate (DOTA-TATE) or -octreotide (DOTA-TOC) [1,2,3,4]
As a further optimization of PRRT, octreotate bound to Evans blue (DOTA-EB-TATE) has recently been introduced [8]
This report presents the results of intraindividual comparisons of activity kinetics in organs and tumours after intravenous administration of both [177Lu]Lu-DOTA-EB-TATE and [177Lu]Lu-DOTA-TOC in patients with progressive somatostatin receptor positive malignancies
Summary
High expression of somatostatin receptors allows for imaging and peptide receptor radionuclide therapy (PRRT) of neoplasms using radiolabelled somatostatin analogues like 90Yand 177Lu-labelled [DOTA0,Tyr3]-octreotate (DOTA-TATE) or -octreotide (DOTA-TOC) [1,2,3,4]. A major problem regarding the tumour absorbed dose in PRRT with DOTA-TATE or DOTA-TOC, is the rapid elimination of the active compound from the blood stream [6, 7], eventually leading to insufficient tumour uptake and poorer clinical outcome. As a further optimization of PRRT, octreotate bound to Evans blue (DOTA-EB-TATE) has recently been introduced [8]. Evans blue reversibly binds to endogenous albumin, retains octreotate in the blood, and extends the effective plasma half-life of the radiolabelled vector considerably. Since somatostatin receptors are still able to bind octreotate held by Evans blue, achievable tumour uptake and absorbed dose might be significantly increased and result in outcomes that are
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