2008-07-01
Molecular imaging of reduced renal uptake of radiolabelled [DOTA 0,Tyr3]octreotate by the combination of lysine and Gelofusine in rats
Publication
Publication
NuklearMedizin , Volume 47 - Issue 3 p. 110- 115
Aim: In peptide receptor radionuclide therapy (PRRT) using radiolabelled somatostatin analogues, kidney uptake of radiolabelled compound is the major dose-limiting factor. We studied the effects of Gelofusine (20 mg) and lysine (100 mg) and the combination of both after injection of therapeutic doses of radiolabelled [DOTA0,Tyr3]octreotate (60 MBq 111In or 555 MBq 177Lu labelled to 15 μg peptide) in male Lewis rats. Methods: Kidney uptake was measured by single photon emission computed tomography (SPECT) scans with a four-headed multi-pinhole camera (NanoSPECT) at 24 h, 5 and 7 days p. i. and was quantified by volume of interest analysis. For validation the activity concentration in the dissected kidneys was also determined ex vivo using a gamma counter and a dose calibrator. Results: Gelofusine and lysine both reduced kidney uptake of [ 177Lu-DOTA0,Tyr3]octreotate significantly by about 40% at all time points. The combination of Gelo - fusine and lysine resulted in a 62% inhibition of kidney uptake (p < 0.01 vs. lysine alone). A weak but significant dose-response relationship for Gelofusine, but not for lysine, was found. In a study with [111In-DOTA0,Tyr 3]octreotate, conclusions drawn from NanoSPECT data were confirmed by biodistribution data. Conclusions: We conclude that rat kidney uptake of radiolabelled somatostatin analogues can be monitored for a longer period in the same animal using animal SPECT. Gelofusine and lysine had equal potential to reduce kidney uptake of therapeutic doses of [177Lu-DOTA 0,Tyr3]octreotate. The combination of these compounds caused a significantly larger reduction than lysine or Gelofusine alone and may therefore offer new possibilities in PRRT. The NanoSPECT data were validated by standard biodistribution experiments.
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doi.org/10.3413/nukmed-0069, hdl.handle.net/1765/74667 | |
NuklearMedizin | |
Organisation | Department of Nuclear Medicine |
Rolleman, E., Bernard, B., Breeman, W., Forrer, F., de Blois, E., Hoppin, J., … de Jong, M. (2008). Molecular imaging of reduced renal uptake of radiolabelled [DOTA 0,Tyr3]octreotate by the combination of lysine and Gelofusine in rats. NuklearMedizin, 47(3), 110–115. doi:10.3413/nukmed-0069 |