The availability of radiopharmaceuticals to depict primary malignant pheochromocytoma and its metastases has markedly changed the approach to these unusual cancers. Whole body screening afforded by scintigraphy allows remote tumor involvement to be identified and provides staging information necessary to guide subsequent therapy. The avid accumulation by malignant pheochromocytoma of some radiopharmaceuticals used for scanning has shown promise in therapeutic trials. In this paper, we discuss radiopharmaceuticals presently employed in malignant pheochromocytoma for both diagnostic and therapeutic uses and potential future compounds that may find their way into clinical practice in the approach to these and other related neoplasms.