Radiopharmaceuticals for targeted radiotherapy of cancer

Abstract

Targeted radiotherapy is the administration of a radiolabelled molecule designed to deliver therapeutic doses of radiation to malignant tumours with high specificity. Radionuclides that are used to label radiopharmaceuticals for cancer therapy generally decay by particle emission, i.e., α, ^-, ⁺, Auger or conversion electrons. Bifunctional chelators have been designed to attach metal radionuclides to biological molecules that target tumours. Four types of targeted radiotherapy agents are discussed: small molecules, carrier particles, receptor-targeted agents and pre-targeting agents. Human trials of targeted radiotherapy for radiolabelled somatostatin analogues and pre-targeting agents are encouraging. This review focuses on selected disclosures in the patent literature, primarily between 1993 and 1999, for radionuclide production, bifunctional chelators and radiopharmaceuticals, which may prove successful in the development of future agents for cancer radiotherapy.

• bifunctional chelators
• pre-targeting
• radioimmunotherapy
• targeted radiotherapy
• tumour receptors