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188Re(CO)3-dipicolylamine-alendronate : a new bisphosphonate conjugate for the radiotherapy of bone metastases

This paper reports the synthesis and biological evaluation of a new beta-emitting radionuclide-bisphosphonate complex designed to improve efficacy (by improved design), cost and availability to patients (by utilising the Re-188 generator) of radionuclide therapy for bone metastases, especially in prostate cancer. The work confirmed the chemical structure and showed that the bisphosphonate group was freely available to bind to bone mineral more effectively than previous bisphosphonate derivatives. Imaging in mice showed that the compound delivered more of the radionuclide to bone, with longer retention, than the previous standard Re-188-HEDP, giving higher radiation dose to bone and less to non-target tissues.