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Bifunctional bisphosphonate complexes for the diagnosis and therapy of bone metastases

This paper describes a new type of radiolabelled bisphosphonate conjugate for improved imaging and palliation of bone metastasis. We used a rational design approach to give higher affinity and selectivity for bone than the conventional SPECT bone imaging agent, 99mTc-MDP. We extended this to a therapeutic analogue (Torres, Bioconjugate Chem. 2010). The molecules have further impact by their binding to iron oxide and other nanomaterials, hence radiolabelling them to generate bi- and tri-modal imaging agents (Torres, Angew. Chem, 2011 & Bioconjugate Chem, 2011). We have begun a clinical trial of these agents for sentinel node detection.