In this chapter, promising dendritic systems are highlighted and theirlimitations are discussed; recent approaches to overcoming these drawbacks are also outlined. Important architectural parameters used torationally design various dendritic materials are provided, while dendritic structure‐related toxicity, biodistribution, cellular uptake, and multivalency are also described in detail. Using several examples, it is shown how dendrimers and dendrons havebeen designed and used as targeted drug delivery vehicles for cancer diagnosis andtreatments in particular. Dendritic materials possessing multifunctionalarchitectures are expected to have a significant impact on the way cancer isprevented, diagnosed, treated, and ultimately cured in the future.