Biodistribution data

In spite of these promising results, the tumor uptake of 9°Y-SU015 is still relatively low (around 1.5% ID/g at 24 h post injection). The biodistribution data in the c-neu Oncomouse model also show that a small part of 9°Y-SU015 is excreted via the hepatobiliary route. The radioactivity levels in blood, kidney, and liver are relatively high, which makes 9°Y-SU015 less than ideal as a new therapeutic radiopharmaceutical for the treatment of solid tumors. 

Table 3.7 gives the biodistribution data of DOTATATE in two groups of Swiss mice those that received the radiopharmaceutical obtained at a molar peptide to radionuclide ratio of 0.54, and those that received the agent obtained at a molar peptide to radionuclide ratio of 2.73. 

The analytical forms used to represent biodistribution data in the most precise and convenient way are ... 

On the basis of the biodistribution data, the estimated absorbed dose to the HRSl tumour from 15 mCi of Lu-DOTATATE in multiple dose therapy was 225.32 rad/mCi (60.89 mGy/MBq). 

TABLE 14.8. ABSORBED DOSES DETERMINED FROM Lii-DOIATATE BIODISTRIBUTION DATA IN RATS... 

The biodistribution data show that Lu-DOTATATE is more stable and has better uptake than l-DOTATATE, and that the CLl of Lu-DOTATATE is three times that of I-DOTATATE. The biodistribution studies carried out in rats bearing tumours overexpressing somatostatin receptors show that Lu-DOTATATE has specific uptake and binds to the tumour with adequate stability. Tlie adrenal gland and pancreas were determined to be dose limiting organs. 

LUNGU, V, BAICULESCU, S., CHIPER, D., NICULAE, D., DANAILA, L., Mathematical modelling correlated to MIRD for calculation absorbed dose from animal biodistribution data , Nat. Conf. Phys., Bucharest, 2005. 

Several authors reported the use of a so-called morpholino (MORE), a commercially available synthetic oligomer for pretargeting application (Liu et al. 2002, 2004). A construct of MAG3 and cMORF was found to be effective in a mouse tumor model. Biodistribution data indicated high uptake in the tumor and low uptake in the normal tissues (Liu et al. 2002). 

The potential utility of Ga-complex as a PET radiotracer was evaluated in mice with micro-PET [139]. Five minutes after tail vein injection of the Ga-complex, a greater net uptake in the brain of knockout mice was detected when compared with that of the wild-type mice, what is consistent with the biodistribution data obtained with the Ga-complex. Although the complex has been reeognized as a transport substrate of Pgp, the authors are cautiously optimistic regarding its applicability in SPECT and PET imaging for in vivo assessment of Pgp activity. Issues related with radiation dosimetry and radiolabeling require additional experimentation. 

Correlations of Physico-Chemical and Biological Properties with in Vivo Biodistribution Data for Platinum-195 m -Labeled Chloroammineplatinum(II) Complexes... 

Empirical Correlations of Biodistribution Data with Physicochemical and Biological Properties... 

We have previously published on the detailed biodistribution of tritium-labeled 5nm dendrimers with neutral and positive-charged surface. This was the first quantitative biodistribution data on dendrimers in tumor model systems, and we found that both dendrimers cleared rapidly from blood, and localized to... 

The anion is clearly not as active as the neutral compound but the result is noteworthy. In principle, the trend in activities in this series may be related to differing cellular absorption with subsequent different intracellular concentrations or to different reactivity with the proposed target molecule. Studies have shown that some of these complexes such as K2PtCl4 [12], rran5-[PtCl2(NH3)2] [13] and [Pt(dien)Cl]+ [14] do inhibit DNA synthesis, and indeed all bind to DNA (see Chapter 1) they are not unreactive but the inhibition does not lead to an antitumour effect. Biodistribution data in vivo have correlated the activity and toxicity of... 

Comparison of biodistribution data for the general series [PtCl (am)4 ] ,... 

J. D. Hoeschele, T. A. Butler, and J. A. Roberts Correlations of Physico-Chemical and Biological Properties with In Vivo Biodistribution Data for Platinum-195m-Labelled Chloroammineplatinum(II) Complexes (Inorganic Chemistry in Biology and Medicine, ACS Symposium Series v. 140, Ed. A. E. Martell) p. 181. ACS, Washington (1980). 

Unless the elimination and biodistribution data could not be obtained in this very interesting model, were are able to conclude that the iodine deficiency seems to accelerate the iodide absorption and to slow the iodide elimination, resulting in a higher biodisponibility than in normal animals. 

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