Molecular radiopharmaceuticals based on bioconjugates of chelators with peptides and proteins have had significant clinical impact in diagnosis and treatment of several types of cancers. In the 1990s, indium-111 and yttrium-90 labelled chelator-peptide/protein conjugates established the clinical utility of these radiopharmaceuticals for receptor-targeted g-scintigraphy imaging and systemic radiotherapy. Second generation bioconjugates based on peptides targeting the somatostatin II receptor and the prostate specific membrane antigen are now widely used for management of neuroendocrine and prostate cancer respectively. These bioconjugates are typically radiolabelled with gallium-68 for imaging of target receptor expression with Positron Emission Tomography, and the b --emitter, lutetium-177 for targeted radiotherapy. Innovations in radioisotope technology and biomolecular therapies are likely to drive the future clinical development of radiopharmaceuticals based on radiometals. New chelator-peptide and chelator-protein bioconjugates will underpin nuclear medicine advances in molecular imaging and radiotherapy.

Radiotracers labelled with technetium-99m (99mTc) enable accessible diagnostic imaging of disease, provided that radiotracer preparation is simple. Whilst 99mTc radiopharmaceuticals for imaging perfusion are routinely prepared from kits, and regularly...

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