A common type of cancer treatment is chemotherapy, which involves using anticancer chemicals to kill cancerous cells. Despite all advances in chemotherapy, this method still has undesired side effects on healthy cells and suffers from nonspecific targeting. Dendrimers are nanoparticles capable of delivering drugs, DNA, and RNA to tumor cells without harming normal cells, so they have been utilized extensively in targeted cancer treatment. A dendrimer is a highly branched polymeric macromolecule with excellent physicochemical properties, intramolecular cavities, and easy surface modification. These structures can be applied as anticancer drug carriers through the entrapment of drugs in their internal voids or binding to the functional groups on their surface. In addition, further surface modifications, such as targeting ligands, can increase selectivity, delivery, and biocompatibility. This review will briefly summarize dendrimer’s history and focus on dendrimer-based nanotherapeutics for cancer therapy. In a nutshell, functionalized dendrimers are presented here as potential drug and gene carriers for cancer treatment.