Authors: Ercan, M.T.; Caglar, M.

Source: Current Pharmaceutical Design, Volume 6, Number 11, 1 July 2000 , pp. 1085-1121(37)

Publisher: Bentham Science Publishers

Abstract:

A variety of radiopharmaceuticals have been introduced for the internal therapy of malignant and inflammatory lesions in nuclear medicine. In order to destroy the disseased tissues radionuclides with high linear energy transfer (LET) such as beta, alpha, Auger or low energy conversion electron emitters are needed. The range of beta particles is in mms so they are effective for large tumors. The range of alpha particles is short, only a few cell diameters. Thus, they are effective in treating circulating malignant cells and micrometastases. The range of Auger and conversion electrons is than0.1 micro m. They are very effective in cell killing when they are carried across cell membrane into the nucleus to damage DNA. Appropriate ions, molecules and particles are labelled with such radionuclides and used as radiopharmaceuticals in many different applications. For an effective dose to be delivered high target to non target ratios must be attained. Monoclonal antibodies to specific antigens expressed on tumor cells have been developed to increase the uptake by malignant tissues by specific accumulation. Radiolabelled peptides such as somatostatin, small molecules such as metaiodo-benzylguanidine (MIBG) and many different nano-and micro-particles have been investigated. The effectiveness of therapy can be increased by direct locoregional administration of the radiopharmaceutical. This way the radiation effects are confined locally and the normal tissues are spared from radiation effects.

Keywords: Radiopharmaceuticals; Malignant; Inflammatory lesions; Linear energy transfer; Micrometastases; Monoclonal antibodies; Internal radionuclide therapy; Radionuclides; Carrier molecules; Ions; Magnetically enhanced radionuclide therapy; Iodide; Beta emitters; Strontium 89 85 chloride; Samarium 153 EDTMP; Alpha emitters; Meta iodobenzylguanidine; Tumor associated antigen; Human antimouse antibody; Targeting vascular bed; Peptide receptor radionuclide therapy; Hepatocellular carcinoma; Thymidine analogs; Hydroxyapatite; Carbohydrates

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612003399833

Publication date: 2000-07-01

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• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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