Given the more widespread use of conventional imaging techniques such as magnetic resonance imaging or computed tomography, recent years have witnessed an increased rate of incidental findings in the adrenal gland and those adrenal masses can be either of benign or malignant origin. In this regard, routinely conducted morphological imaging cannot always reliably distinguish between cancerous and noncancerous lesions. As such, those incidental adrenal masses trigger further diagnostic work-up, including molecular functional imaging providing a non-invasive read-out on a sub-cellular level. For instance, [¹⁸F]FDG positron emission tomography (PET) as a marker of glucose consumption has been widely utilized to distinguish between malignant vs benign adrenal lesions. In addition, more adrenal cortex-targeted radiotracers for PET or single photon emission computed tomography have entered the clinical arena, e.g., Iodometomidate or IMAZA, which are targeting CYP11B enzymes, or Pentixafor identifying CXCR4 in adrenal tissue. All these tracers are used for diagnosing tumors deriving from the adrenal cortex. Furthermore, radiolabeled MIBG, DOPA, and DOTATOC/-TATE are radiotracers that are quite helpful in detecting pheochromocytomas originating from the adrenal medulla. Of note, after having quantified the retention capacities of the target in-vivo, such radiotracers have the potential to be used as anti-cancer therapeutics by using their therapeutic equivalents in a theranostic setting. The present review will summarize the current advent of established and recently introduced molecular image biomarkers for investigating adrenal masses and highlight its transformation beyond providing functional status towards image-guided therapeutic approaches, in particular in patients afflicted with adrenocortical carcinoma.