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Radiopharmaceuticals for Radionuclide Therapy
Published in Michael Ljungberg, Handbook of Nuclear Medicine and Molecular Imaging for Physicists, 2022
Meltem Ocak, Emre Demirci, Jessie R. Nedrow, Rebecca Krimins
In numerous studies, a response rate of 40–97 per cent with a mean of 70 per cent has been reported. The quality of life of the patients also improved, and a significant decrease in analgesic consumption has been noted. A mild bone marrow toxicity is noted in most the patients. The platelet and white blood cell (WBC) counts have been decreased to the lowest levels in 3–5 weeks but recover in 6–8 weeks after therapy. For the repeated treatments, the main dose-limiting toxicity is bone marrow suppression [73]. Overall, 153Sm–EDTMP has been successfully used for pain control for more than three decades.
Management of bone pain
Published in Nigel Sykes, Michael I Bennett, Chun-Su Yuan, Clinical Pain Management, 2008
Samarium (153Sm) is available as an alternative to strontium. This is conjugated with a phosphonate compound ethylene diamine tetraline tetramethyline phosphonic acid (EDTMP) and thereby preferentially taken up after intravenous administration into sites of bone remineralization. It is a beta particle emitter with an average energy of 233 KeV and a range of 3 mm in soft tissue. In addition, samarium produces low energy gamma rays at 103 KeV which gives the advantage that it can be imaged using a gamma camera, as shown in Figure 20.6. Administration is by single intravenous injection and formal phase I and II dose escalation studies33[III] have shown optimal effect at a dose of 1 mCi/kg. It has been evaluated in randomized placebo-controlled double-blind trials34[II] and found to have a demonstrable analgesic effect in hormone-resistant prostate cancer and breast cancer. Transient myelosuppression is seen from radiation dose to the bone marrow, which is rarely of clinical consequence and multiple doses of samarium at eight-week intervals have been described.
Radiolanthanides in Nuclear Medicine
Published in Astrid Sigel, Helmut Sigel, Metal Ions in Biological Systems, 2004
Frank Rösch, Eva Forssell-Aronsson
Multidentate chelates are needed to form complexes because in vivo dissociation of the radiolanthanide from the chelate invariably results in bone and liver uptake. While for many applications this uptake is undesirable since it leads to non-specific irradiation of these (presumably) non-target tissues, for the palliative therapy of disseminated bone metastases, the radiolanthanide accumulation on the hydroxyapatite structure is desired. Therefore, ligands with intermediate complex formation constants are selected or ligands, that tender an additional binding capacity to hydroxyapatite. In analogy to known 99mTc complexes with substituted phosphonates, substituted amine-methylene phosphonic acids such as EDTMP (ethylenediaminetetramethylene phosphonic acid), DOTMP (1,4,7,10-cyclododecyl-tetraaminetetramethylene phosphonic acid), and DTPMP (diethylenetriaminepentamethylene phosphonic acid) have been investigated for the radiolanthanides. [153Sm]EDTMP has become commercially available, while for the application of 166Ho, due to its lower specific activity, the kinetically inert ligand DOTMP was discussed [14].
Comparative studies on the potential use of 177Lu-based radiopharmaceuticals for the palliative therapy of bone metastases
Published in International Journal of Radiation Biology, 2020
Hesham M. H. Zakaly, Mostafa Y. A. Mostafa, Darya Deryabina, Michael Zhukovsky
Next, ethylene diamine tetramethylene phosphonate (EDTMP), another osteotropic drug, is considered. EDTMP is a therapeutic agent currently used in combination with the 153Sm radionuclide. EDTMP preparation forms a compound with 177Lu that has stability of more than 98% (Chakraborty, Das, Banerjee, et al. 2008). This fact will be taken into account when calculating the dose loads on organs and tissues.