Radiolanthanides in endoradiotherapy: an overview

Abstract

Endoradiotherapy (targeted radionuclide therapy) is a systemic approach, involving a radiolabeled targeting vector with a well characterized biochemical strategy to selectively deliver a cytotoxic level of radiation to a disease site on a cellular/molecular level. The group of radiolanthanides has been considered both for imaging and therapy over many years. Some radiolanthanides have been and are increasingly applied for therapeutic purposes. However, the clinical use of endoradiotherapeuticals containing radiolanthanides requires a complex and interdisciplinary approach. It involves, among other factors, the choice of the most suitable lanthanide radionuclide (in terms of nuclear decay parameters such as type and energy of the particles emitted, half-life, decay products etc.); the identification of the most promising production route; the determination of the relevant production parameters such as excitation functions, nuclear reaction yields, radionuclidic purities, specific activities etc.; the chemical isolation of the radiolanthanide produced from the target material (except the (n, γ) production route); the synthesis of the labelling precursor, and labelling of the precursor and the chemical purification and isolation of the labelled radiotherapeutical, ready for i.v. injection; and finally the investigation of pharmacological targeting parameters of the labelled radiotherapeutical in vitro and in vivo (animal experiments).