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Development and Estimation of Human Dosimetry of a New 47Sc-Risedronate for Radiopharmaceutical Application.

Bisphosphonate risedronate (2-(3-pyridinyl)-1-hydroxyethane diphosphonic acid) was radiolabeled with scandium-47 (47Sc) as potential therapeutic radiopharmaceutical for skeletal metastases. Its time-dependent biodistribution in mice was measured and its human dosimetry was derived. The labelling process was performed at 95 °C for 30 min. The stability of the radio-conjugate was tested in human serum at 37 °C and its biodistribution was studied in balb/c mice. The radiochemical yield of ≥90% was obtained corresponding to a specific activity of 277 MBq/mg. The radio-conjugate showed good stability in human serum up to 48 h. A high bone uptake by 48 h post-injection was achieved, which suggests that 47Sc-risedronate may be therapeutically beneficial for the palliation of painful bone metastasis. The estimated absorbed dose coefficient and the time-integrated activity coefficient (ã (rs, TD)) in the bone were 1.35 mGy/MBq and 31.04 (Bq-h/Bq), respectively. The absorbed doses to non-osseous normal organs were much lower than that to the bone.