Therapeutic radiopharmaceuticals

Ercan M., Caglar M.

CURRENT PHARMACEUTICAL DESIGN, vol.6, no.11, pp.1085-1121, 2000 (SCI-Expanded) identifier

  • Publication Type: Article / Review
  • Volume: 6 Issue: 11
  • Publication Date: 2000
  • Doi Number: 10.2174/1381612003399833
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1085-1121
  • Hacettepe University Affiliated: Yes


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 mm's 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 <0.1 mu 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 an spared from radiation effects.