Among the numerous nanomedicine formulations, dendrimers have emerged as original, efficient, carefully assembled, hyperbranched, polymeric nanoparticles based on synthetic monomers. Dendrimers are used either as nanocarriers of drugs or as drugs themselves. When used as drug carriers, dendrimers are considered ‘best-in-class agents’, modifying and enhancing the pharmacokinetic and pharmacodynamic properties of the active entities encapsulated or conjugated with the dendrimers. When used as drugs themselves, dendrimers represent a novel category of “first-in-class” drugs. The purpose of this original review is to analyse the different strategies involved in the development, application, and impact of dendrimers as drugs. We examine a selection of nanoparticles that use multifunctional elements and demonstrate clinical multifunctionality, and we extend these principles to applications in dendrimer nanomedicine design. Finally, for practical consideration, the concepts of vertical and diagonal translation are introduced as potential strategies to facilitate dendrimer development.