After a quarter of century of rapid technological advances, research has revealed the complexity of cancer, a disease intimately related to the dynamic transformation of the genome. However, the full understanding of the molecular onset of this disease is still far from achieved and the search for mechanisms of treatment will follow closely. It is here that Nanotechnology enters the fray offering a wealth of tools to diagnose and treat cancer. It is indisputable that the use of gold nanocarriers has been gaining momentum as vectors for therapy and diagnostic strategies, combining the AuNPs’ ease of functionalization with numerous biomolecules, high loading capacity and fast uptake by target cells. In fact, over the last decade nearly 12.000 research papers focusing on multifunctional gold nanocarriers have been published in peer-reviewed journals. Some of the described nanosystems will most likely revolutionize our understanding of biological mechanisms and push forward the clinical practice through their integration in future diagnostics platforms. Nevertheless, very little gave fruitful results in order to improve a bench-to-bedside approach to translational research. On the basis of theoretical and experimental results obtained so far are we or not at the point: from bench to bedside and back again? As you will see, the answers to this question are complex, but one thing is clear: Translation into clinics is a tortuous and difficult path. Here, we provide a critical review about the available multifunctional gold nanocarriers for in vitro application and in vivo cancer targeting on nanodiagnostics and therapy.