Bone-seeking radiopharmaceuticals play a significant role in the treatment of metastatic pain as an alternative, or in addition, to classic palliative treatment.
Until a few years ago, radionuclides for the management of prostate cancer consisted of several beta-emitting agents, such as strontium (89Sr), phosphorus (32P) and samarium (153Sm) as well as rhenium (186Re and 188Re), which only exhibit a palliative effect in patients with extensive skeletal disease.
Radium (223Ra) dichloride represents a new generation of radiopharmaceuticals, being the first targeted alpha-emitting agent approved, which improves overall survival, postpones skeletal-related events (SREs) and controls bone pain.
Conjugates of bisphosphonates (BP) with macrocyclic chelators open new possibilities in bone-targeted radionuclide imaging and therapy, when labelled with positron and beta-emitting radiometals. [68Ga/177Lu]DOTAZOL appears to be the best leading compound showing fast blood clearance, low uptake in soft tissue and high accumulation in the skeleton.
Prostate-specific membrane antigen (PSMA) is an attractive target for diagnosis and therapy of prostate cancer. 177Lu-PSMA-617 is a new treatment option, which is not solely directed to bone metastases, but also demonstrates “antitumour” activity with limited and well-tolerated side effects.
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