AbstractMacrocyclic supramolecular materials play an important role in encapsulating anticancer drugs to improve the anticancer efficiency and reduce the toxicity to normal tissues through host‐guest interactions. Among them, pillar[n]arenes, as an emerging class of supramolecular macrocyclic compounds, have attracted increasing attention in drug delivery and drug‐controlled release due to their high biocompatibility, excellent host‐guest chemistry, and simplicity of modification. In this review, we summarize the research progress of pillar[n]arene‐based supramolecular nanodrug delivery systems (SNDs) in recent years in the field of tumor therapy, including drug‐controlled release, imaging diagnostics and therapeutic modalities. Furthermore, the opportunities and major limitations of pillar[n]arene‐based SNDs for tumor therapy are discussed.