Intrigued and inspired by the intricacy of natural architectures which display various morphologies, researchers seek to develop artificial counterparts in order to replicate, and thereby harness, their function for diverse applications. In particular, well‐defined nanoparticles with various morphologies are of great interest for biomedical research. The impact of morphologically discrete nanoparticles upon the development of nanomedicine is significant, gaining increasing attention for its potential to provide a new avenue for the development of future therapeutic technologies. This progress report discusses adaptive morphologies based on block copolymers as platforms for therapeutic and smart drug delivery applications, including design rationale and controlling the morphology of polymeric nanoparticles. The proof‐of‐concept studies on influence of shapes of nanoparticles on their anticancer effects in vitro and in vivo are addressed.