The Role of Bone-Seeking Radionuclides in the Palliative Treatment of Patients with Painful Osteoblastic Skeletal Metastases

Abstract

Targeted bone-seeking radionuclides are underutilized in the treatment of painful diffuse osteoblastic metastases. Several new agents are in active clinical investigation, and the pending approval of the first alpha-emitting radionuclide (223Ra) may offer a new class of agents that provide greater efficacy and less toxicity than those currently available for routine clinical use.

Medical Treatment of Breast Cancer Bone Metastasis: From Bisphosphonates to Targeted Drugs

“…Uncontrolled systemic disease, asemptomatic bone metastasis less than three bone metastasis sites, pure osteolytic metastasis, poor bone marrow reserve and less than 60 days of life expectancy are relative contraindications of radionuclide therapy. Absolute contraindications are spinal cord compression, high risk of fracture or pathologic fracture of weight bearing bone, renal failure, pregnancy and breast feeding (Tomblyn, 2012). Strontium-89 hydrochloride (Sr-89), samarium-153 lexidronam (Sm-153) and rhenium-186 hydroxyethylidenediphosphonate (Re-186) are approved radiopharmaceuticals for radionuclide therapy.…”

“…Transient myelosuppression is the most common toxicity. Generally thrombocytopenia is experienced, significant neutropenia and anemia develops less than thrombocytopenia (Tomblyn, 2012). There was a debate about combined use of bisphosphonate and radionuclides.…”

Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

“…For example, the decay of 125 I has been shown to lead to the deposition of a very high dose (≈10 9 cGy/decaying atom) in the immediate vicinity (≈2 nm 3 ) of the decay site and a sharp and significant drop in the energy deposited (from ≈10 9 to ≈10 6 cGy) as a function of increasing distance (few nanometres) from the decaying 125 I atom (Kassis, 2011). For example, when 125 I is localized within the cytoplasm, the survival curve is of the low LET type and the number of decays needed to reduce survival is ≈80 times that of DNA-incorporated 125 I (Kassis, 2011 (Abbasi, 2012(Abbasi, , 2011Argyrou et al, 2013a;Bączyk, 2011;Bryan et al, 2009;Chakraborty et al, 2008;Daha et al, 2010;Das et al, 2009;Harrison et al, 2013;Lewington, 2005;Máthé et al, 2010;Neves et al, 2005;Nilsson et al, 2013bNilsson et al, , 2007Nilsson et al, , 2005aNilsson et al, , 2005bPandit-Taskar et al, 2014;Ramdahl et al, 2013;Sartor, 2004;Simón et al, 2012;Sivaprasad and Rajagopal, 2012;Tomblyn, 2012;Vigna et al, 2011;Volkert and Hoffman, 1999;Wang et al, 2011). Despite the growing number of radionuclides investigated for treatment of bone metastases, the use of 89 Sr and 153 Sm still accounts for the bulk of radiopharmaceutical bonetargeted therapeutics in the clinical context and the majority of the review articles available in the literature focus on those two radionuclides.…”

Production and quality control 177Lu (NCA)—DOTMP as a potential agent for bone pain palliation

“…Low‐energy β ‐ emitting radionuclides, such as 177 Lu, 153 Sm, 175 Yb, and 186 Re, are used for palliation of bone pain, whereas radionuclides with higher energies including 166 Ho, 90 Y, and 188 Re are recommended for bone marrow ablation. Sometimes, the carrier and radionuclide are one and the same (as 32 P and 89 Sr) because of their similarity to the elemental composition of bone 17 , 18 , 19 , 20 , 21 …”