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Iodine-131-Labeled Diphosphonates for Palliative Treatment of Bone Metastases: II. Preliminary Clinical Results with Iodine-131 BDP3

Klinikum der Universität Heidelberg and Universitätskliniken Homburg/Saar, West Germany

Correspondence: For reprints contact: M. Eisenhut, PhD, Klinikum der Universität Heidelberg, Zentrum Radiologie, Forschungsgruppe Strahlenklinik, Im Neuenheimer Feld 328, D-6900 Heidelberg, FRG.

ABSTRACT

The kinetics, dosimetry, and response of iodine-131 -amino-(4-hydroxybenzylidene)-diphosphonate ([¹³¹I]BDP3) treatment were investigated with patients who had pain symptoms from bone metastases of various primary carcinoma. The blood clearance of [¹³¹I] BDP3 was rapid. More than 90% disappeared from the blood pool at 2 hr after injection. The excretion of the activity occurred solely through the kidneys and mean total-body retention at 48 hr was 48.6%. The urinary activity showed a metabolite which must be formed by an in vivo cleavage reaction of a phosphorus-carbon bond. The uptake of in vivo cleaved [¹³¹I] iodide in the unblocked thyroid was 0.5%. The effective half-life of [¹³¹I]BDP3 in metastatic bone (median 182 hr; range 177–205 hr) proved to be longer than in unaffected areas (145 hr; 140–165 hr). Palliative therapies were performed with 18 patients. They received doses ranging between 6 and 48 mCi [¹³¹I]BDP3. The response was 44% complete pain relief, 6% substantial pain relief, 22% minimal improvement, and 28% no change. The duration of response ranged between 1 and 8 wk.

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