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Pharmacokinetics of Rhenium-186 After Administration of Rhenium-186-HEDP to Patients with Bone Metastases

Department of Nuclear Medicine, Center for Hospital Pharmacy, and Oncology Section, Department of Internal Medicine, University Hospital Utrecht, Utrecht, The Netherlands

Correspondence: For reprints contact: J. M. H. de Klerk, MD, Dept. of Nuclear Medicine, University Hospital Utrecht, Room E 02.222, P.O. Box 85500, 3508 GA Utrecht, The Netherlands.

ABSTRACT

The pharmacokinetics of ¹⁸⁶Re-HEDP, a radiopharmaceutical for palliative treatment of metastatic bone pain, was investigated in 11 patients (17 studies) who suffered from metastatic breast or prostate cancer. Half-life times of ¹⁸⁶Re in three blood fractions (whole blood, plasma and plasma water) were 40.1 ± 5.0, 41.0 ± 6.0 and 29.5 ± 6.4 hr, respectively. Time-dependent increase in plasma-protein binding was observed, probably caused by in vivo decomposition of ¹⁸⁶Re-HEDP. Total urinary ¹⁸⁶Re excretion was 69% ± 15%, of which 71% ± 6% was excreted in the first 24 hr after injection. The BSI (i.e., fraction of the skeleton showing scintigraphic evidence of metastatic disease) closely correlated with the fraction of dose non-renally cleared (r = 0.98). This implies that the amount of radioactivity taken up by the skeleton and hence the bone marrow absorbed dose can be predicted from a diagnostic pre-therapy ^99mTc-HDP scintigram. The pharmacokinetic behavior indicates that ¹⁸⁶Re-HEDP has suitable properties to justify its application.

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