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Co\u2010administration or sequential administration of selected drugs whose mechanism of action complement the properties of radionuclide therapy may provide a pharmacological basis to potentially overcome some of the limitations of radiopharmaceutical therapy and may enhance clinical efficacy by additive or synergistic cytotoxic effects. The rational design and evaluation of novel radiopharmaceutical\u2013drug combinations and optimization of dosage and administration schedules, within the complex context of individualized multimodal cancer treatment, requires a multidisciplinary approach, principally including clinical pharmacology. 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