Organ distribution studies of lutetium-177 in mouse

Müller, W.; Linzner, U.; Schäffer, Eva

doi:10.1016/0047-0740(78)90087-6

Cited by 18 publications

(9 citation statements)

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“…All key organs treated with 177 Lu-tetulomab had lower absorbed doses than those found by Fisher et al [39] where no serious adverse effects were observed in the patients. For all organs the absorbed doses of 177 Lu-tetulomab were well below the 15 Gy limit suggested by Winter et al (2009) for 90 Y-ibritumomab [37].…”

Section: Resultsmentioning

confidence: 53%

“…The extrapolations from the last time point of the activity vs. time curves to infinity represented between 2 and 11 % of the total area under the curve. The data was compared with clinical dosimetry data of 90 Y-tiuexetan-ibritumomab (15 MBq/kg) from Fisher et al [39] and of 177 Lu-cG250 (2,405 GBq/m 2 ) from Stillebroer et al [36], which is equivalent to approximately 60 MBq/kg for a patient with 1.79 m 2 surface area and 70 kg bodyweight. …”

Section: Resultsmentioning

confidence: 99%

“…The uptake in bone was explained by the similarity between the ions 177 Lu +3 and Ca +2 that are involved in hydroxiapatite formation. Muller et al [39] found that the biological half-lives of 177 Lu was around 5 days for soft tissues while it was 50 days for skeleton. Given the low concentration of activity found in femur and skull in the biodistribution studies of 177 Lu-tetulomab, 177 Lu does not seem to detach from the tetraxetan chelator to a significant degree after injection.…”

Section: Discussionmentioning

confidence: 99%

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Biodistribution and Dosimetry of 177Lu-tetulomab, a New Radioimmunoconjugate for Treatment of Non-Hodgkin Lymphoma

Repetto-Llamazares

Larsen

Mollatt

et al. 2013

CRP

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The biodistribution of the anti-CD37 radioimmunoconjugate 177Lu-tetraxetan-tetulomab (177Lu-DOTA-HH1) was evaluated. Biodistribution of 177Lu-tetraxetan-tetulomab was compared with 177Lu-tetraxetan-rituximab and free 177Lu in nude mice implanted with Daudi lymphoma xenografts. The data showed that 177Lu-tetulomab had a relevant stability and tumor targeting properties in the human lymphoma model. The half-life of 177Lu allowed significant tumor to normal tissue ratios to be obtained indicating that 177Lu-tetraxetan-tetulomab could be suitable for clinical testing. The biological and effective half-life in blood was higher for 177Lu-tetraxetan-tetulomab than for 177Lu-tetraxetan-rituximab. The biodistribution of 177Lu-tetraxetan-tetulomab did not change significantly when the protein dose was varied from 0.01 to 1 mg/kg. Dosimetry calculations showed that the absorbed radiation doses to normal tissues and tumor in mice were not significantly different for 177Lu-tetraxetan-tetuloma b and 177Lu-tetraxetan-rituximab. The absorbed radiation doses were extrapolated to human absorbed radiation doses. These extrapolated absorbed radiation doses to normal tissues for 177Lu-tetraxetan-tetulomab at an injection of 40 MBq/kg were significantly lower than the absorbed radiation doses for 15 MBq/kg Zevalin, suggesting that higher tumor radiation dose can be reached with 177Lu-tetraxetan-tetulomab in the clinic.

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Section: Resultsmentioning

confidence: 53%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Biodistribution and Dosimetry of 177Lu-tetulomab, a New Radioimmunoconjugate for Treatment of Non-Hodgkin Lymphoma

Repetto-Llamazares

Larsen

Mollatt

et al. 2013

CRP

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“…Although the amount of free 177 Lu is ≤0.5%, there are reports on its incorporation in the skeleton [5,6,8]. Therefore, preclinical experiments were performed to obtain detailed morphological information.…”

Section: Discussionmentioning

confidence: 99%

“…Muller et al reported in a study with mice that 60% of the injected dose (ID) of 177 LuCl 3 is incorporated in the skeleton at 48 h p.i. [5,6]. Li et al reported the stability of 177 Lu-DTPA in vitro in serum [4].…”

Section: Introductionmentioning

confidence: 99%

The addition of DTPA to [177Lu-DOTA0,Tyr3]octreotate prior to administration reduces rat skeleton uptake of radioactivity

Breeman

Wansem

Bernard

et al. 2003

Eur J Nucl Med Mol Imaging

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Peptide receptor-targeted radionuclide therapy is nowadays also being performed with DOTA-conjugated peptides, such as [DOTA(0),Tyr(3)]octreotate, labelled with radionuclides like (177)Lu. The incorporation of (177)Lu is typically >/=99.5%; however, since a total patient dose can be as high as 800 mCi, the amount of free (177)Lu(3+) (= non-DOTA-incorporated) can be substantial. Free (177)Lu(3+) accumulates in bone with unwanted irradiation of bone marrow as a consequence. (177)Lu-DTPA is reported to be stable in serum in vitro, and in vivo it has rapid renal excretion. Transforming free Lu(3+) to Lu-DTPA might reroute this fraction from accumulation in bone to renal clearance. We therefore investigated: (a) the biodistribution in rats of (177)LuCl(3), [(177)Lu-DOTA(0),Tyr(3)]octreotate and (177)Lu-DTPA; (b) the possibilities of complexing the free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate to (177)Lu-DTPA prior to intravenous injection; and (c) the effects of free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate, in the presence and absence of DTPA, on the biodistribution in rats. (177)LuCl(3) had high skeletal uptake (i.e. 5% ID per gram femur, with localization mainly in the epiphyseal plates) and a 24-h total body retention of 80% injected dose (ID). [(177)Lu-DOTA(0),Tyr(3)]octreotate had high and specific uptake in somatostatin receptor-positive tissues, and 24-h total body retention of 19% ID. (177)Lu-DTPA had rapid renal clearance, and 24-h total body retention of 4% ID. Free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate could be complexed to (177)Lu-DTPA. Accumulation of (177)Lu in femur, blood, liver and spleen showed a dose relation to the amount of free (177)Lu(3+), while these accumulations could be normalized by the addition of DTPA. After labelling [DOTA(0),Tyr(3)]octreotate with (177)Lu the addition of DTPA prior to intravenous administration of [(177)Lu-DOTA(0),Tyr(3)]octreotate is strongly recommended.

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The Radiopharmaceutical Science of Monoclonal Antibodies and Peptides for Imaging and Targeted In Situ Radiotherapy of Malignancies

Reilly

2010

Pharmaceutical Sciences Encyclopedia

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Radiolabeled monoclonal antibodies (mAbs) and peptides offer the opportunity for molecular imaging of tumors in order to probe their phenotypic properties. Various strategies are being used for labeling these biomolecules with single gamma‐photon‐emitters or positron‐emitters for single‐photon emission computerized tomography (SPECT) and positron‐emission tomography (PET) imaging, respectively. This article focuses on the radiopharmaceutical science that provides the foundation for these biomolecules, mAbs and peptides, for targeting radionuclides to tumors.

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Organ distribution studies of lutetium-177 in mouse

Cited by 18 publications

References 4 publications

Biodistribution and Dosimetry of 177Lu-tetulomab, a New Radioimmunoconjugate for Treatment of Non-Hodgkin Lymphoma

Biodistribution and Dosimetry of 177Lu-tetulomab, a New Radioimmunoconjugate for Treatment of Non-Hodgkin Lymphoma

The addition of DTPA to [177Lu-DOTA0,Tyr3]octreotate prior to administration reduces rat skeleton uptake of radioactivity

The Radiopharmaceutical Science of Monoclonal Antibodies and Peptides for Imaging and Targeted In Situ Radiotherapy of Malignancies

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