Abstract
The development and subsequent clinical uses of radioiodinated meta-iodobenzylguanidine (MIBG) represent a good example of truly molecular targeting avant la letter. The credit for this goes to Prof. William Beierwaltes, whose group at the University of Michigan in Ann Arbor in the 1960s studied and developed tracers for the adrenal cortex, medulla, and heart. After working with 14C-epinephrine for neuroblastoma (1967) and 14C-dopamine for pheochromocytoma (1973) initially [1], they switched to radioiodinated bretylium analogs and quaternary ammonium derivatives for imaging. Don Wieland synthesized and compared 125I-labelled ortho-, para-, and metaisomers of iodobenzylguanidine and was the first to describe imaging of the dog’s adrenal medulla using 131I-para-iodobenzylguanidine (1980); in 1981, Sisson et al. reported imaging of pheochromocytoma in humans using 131I-MIBG. The downside was that 131I-MIBG was a poor tracer for cardiac imaging and that initial attempts to image other neuroendocrine tumors (NETs) showed false-negative results.
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Hoefnagel, C.A. (2014). Tumors of the Adrenergic System: Imaging and Therapy. In: Hodler, J., von Schulthess, G.K., Kubik-Huch, R.A., Zollikofer, C.L. (eds) Diseases of the Abdomen and Pelvis 2014–2017. Springer, Milano. https://doi.org/10.1007/978-88-470-5659-6_32
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