2022
DOI: 10.3390/molecules27185831
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Dosimetry of [212Pb]VMT01, a MC1R-Targeted Alpha Therapeutic Compound, and Effect of Free 208Tl on Tissue Absorbed Doses

Abstract: [212Pb]VMT01 is a melanocortin 1 receptor (MC1R) targeted theranostic ligand in clinical development for alpha particle therapy for melanoma. 212Pb has an elementally matched gamma-emitting isotope 203Pb; thus, [203Pb]VMT01 can be used as an imaging surrogate for [212Pb]VMT01. [212Pb]VMT01 human serum stability studies have demonstrated retention of the 212Bi daughter within the chelator following beta emission of parent 212Pb. However, the subsequent alpha emission from the decay of 212Bi into 208Tl results i… Show more

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Cited by 4 publications
(3 citation statements)
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“…On the other hand, the impact from free 208 Tl is also very minimal. The recoiled free 208 Tl from alpha emission of 212 Bi results in 0.03% and 0.09% increase in the absorbed dose to the red marrow and the kidneys, respectively [ 55 ]. In general, free 208 Tl results in less than 1.2% absorbed dose in any organ or tissue [ 55 ].…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…On the other hand, the impact from free 208 Tl is also very minimal. The recoiled free 208 Tl from alpha emission of 212 Bi results in 0.03% and 0.09% increase in the absorbed dose to the red marrow and the kidneys, respectively [ 55 ]. In general, free 208 Tl results in less than 1.2% absorbed dose in any organ or tissue [ 55 ].…”
Section: Discussionmentioning
confidence: 99%
“…The recoiled free 208 Tl from alpha emission of 212 Bi results in 0.03% and 0.09% increase in the absorbed dose to the red marrow and the kidneys, respectively [ 55 ]. In general, free 208 Tl results in less than 1.2% absorbed dose in any organ or tissue [ 55 ]. In the micro-SPECT imaging study, the Bioemtech Gamma-Eye SPECT Imaging system had energy range of 30–500 keV.…”
Section: Discussionmentioning
confidence: 99%
“…Isothermal titration calorimetry (ITC) experiments confirmed the stability of the 212 Bi daughter radionuclide in the PSC chelator to >95% at 2 h after radiolabeling. Importantly, the contribution of free 208 Tl to the total body dose was shown to be negligible [20]. The optimization of the radiochemical labeling procedure included steps to overcome the loss of activity due to several purification steps: The freshly eluted activity from the 224 Ra/ 212 Pb generator is partitioned into Pb resin 10-12%, waste ~2%, and product 84-86%.…”
Section: Radiochemistrymentioning
confidence: 99%