Chemotherapy is widely recognized as an effective approach for treating cancer due to its ability to eliminate cancer cells using chemotherapeutic drugs. However, traditional chemotherapy suffers from various drawbacks, including limited solubility and stability of drugs, severe side effects, low bioavailability, drug resistance, and challenges in tracking treatment efficacy. These limitations greatly hinder its widespread clinical application. In contrast, supramolecular chemotherapy, which relies host–guest interactions, presents a promising alternative by offering highly efficient and minimally toxic anticancer drug delivery. In this review, we provide an overview of recent advancements in supramolecular chemotherapy based on host–guest interactions. We emphasize the significant role it plays in guiding cancer therapy. Drawing on a wealth of cutting‐edge research, we aim to present a timely and valuable resource for individuals interested in the field of supramolecular chemotherapy or cancer therapy. Furthermore, we aspire to contribute to progression of the field of supramolecular chemotherapy toward clinical application.This article is protected by copyright. All rights reserved