Pentavalent rhenium-188 dimercaptosuccinic acid for targeted radiotherapy: synthesis and preliminary animal and human studies.

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    • Abstract:
      Abstract. Pentavalent rhenium-188 dimercaptosuccinic acid [[sup 188]Re(V)DMSA] is a beta-emitting analogue of [sup 99m]Tc(V)DMSA, a tracer that is taken up in a variety of tumours and bone metastases. The aim of this study was to develop the kit-based synthesis of the agent on a therapeutic scale, to assess its stability in vivo, and to obtain preliminary biodistribution and dosimetry estimates, prior to evaluation of its potential as a targeted radiotherapy agent. The organ distribution of [sup 188]Re in mice was determined 2 h alter injection of 3 MBq [sup 188]Re(V)DMSA prepared from eluate from a [sup 188]W/[sup 188]Re generator. Three patients with cancer of the prostate and three with cancer of the bronchus, all with bone metastases confirmed with a standard [sup 99]mTc-hydroxymethylene diphosphonate ([sup 99]mTc-HDP) scan, were given 370 MBq [sup 188]Re(V)DMSA and imaged at 3 h and 24 h using the 155-kev gamma-photon (15%). Blood and urine samples were collected to determine clearance and to analyse the speciation of [sup 188]Re. Organ residence times were estimated from the scans, and used to estimate radiation doses using MIRDOSE 3. In mice, [sup 188]Re(V)DMSA was selective for bone and kidney. In patients, it showed selectivity for bone metastases (particularly those from prostate carcinoma) and kidney, but uptake in normal bone was not significantly greater than in surrounding soft tissues. Of the normal tissues the kidneys received the highest radiation dose (0.5-1.3 mGy/MBq). The images... [ABSTRACT FROM AUTHOR]
    • Abstract:
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