Bee Pollen (BP) has many advantageous properties relying on its multitargeting potential, a new tendency in managing many challenging illnesses. In cancer and neurodegeneration, the multiple effects of BP could be of unequaled importance and need further investigation. Although still limited, available data interestingly spotlights some floral sources with promising activities in line with this investigation. Adopting scoping review methodology, we have identified many crucial bioactivities that are widely recognized to individual BP compounds but remain completely untapped in this valuable bee cocktail. A wide range of these compounds have been recently found to be endowed with great potential in modulating pivotal processes in neurodegeneration and cancer pathophysiology. In addition, some ubiquitous BP compounds have only been recently isolated, while the number of studied BPs remains extremely limited compared to the endless pool of plant species worldwide. We have also elucidated that clinical profits from these promising perspectives are still impeded by challenging hurdles such as limited bioavailability of the studied phytocompounds, diversity and lack of phytochemical standardization of BP, and the difficulty of selective targeting in some pathophysiological mechanisms. We finally present interesting insights to guide future research and pave the way for urgently needed and simplified clinical investigations.