With the rapid development of nanotechnology, stimuli‐responsive nanomaterials have provided an alternative for designing controllable drug delivery systems due to their spatiotemporally controllable properties. As a new type of porous material, metal–organic frameworks (MOFs) have been widely used in biomedical applications, especially drug delivery systems, owing to their tunable pore size, high surface area and pore volume, and easy surface modification. Here, recent progress in MOF‐based stimuli‐responsive systems is presented, including pH‐, magnetic‐, ion‐, temperature‐, pressure‐, light‐, humidity‐, redox‐, and multiple stimuli‐responsive systems for the delivery of anticancer drugs. The remaining challenges and suggestions for future directions for the rational design of MOF‐based nanomedicines are also discussed.

Metal–organic frameworks (MOFs), also known as coordination polymers, have attracted extensive research interest in the past few decades due to their unique physical structures and potentially vast applications. In this review, we outline the recent progress in the synthesis, functionalization and applications of MOFs in biomedicine, mainly focusing on two promising, yet challenging areas, i.e., drug delivery and biosensing applications. A major challenge is the proper functionalization of MOFs with demanding properties suitable for biomedical applications. Extensive studies on MOFs in biomedicine have led to substantial progress in the control of key properties of MOFs such as toxicity, size and shape, and biological stability. Due to their flexible composition, pore size and easy functionalization properties, MOFs can be utilized as key components for the development of various functional systems, and their applications in drug delivery and biosensing are reviewed. Future trends and perspectives in these research areas are also outlined.

It is of utmost urgency to achieve effective and safe anticancer treatment with the increasing mortality rate of cancer. Novel anticancer drugs and strategies need to be designed for enhanced therapeutic efficacy. Fenton- and Fenton-like reaction-based chemodynamic therapy (CDT) are new strategies to enhance anticancer efficacy due to their capacity to generate reactive oxygen species (ROS) and oxygen (O₂). On the one hand, the generated ROS can damage the cancer cells directly. On the other hand, the generated O₂ can relieve the hypoxic condition in the tumor microenvironment (TME) which hinders efficient photodynamic therapy, radiotherapy, etc. Therefore, CDT can be used together with many other therapeutic strategies for synergistically enhanced combination therapy. The antitumor applications of Fenton- and Fenton-like reaction-based nanomaterials will be discussed in this review, including: (iþ) producing abundant ROS in-situ to kill cancer cells directly, (ii) enhancing therapeutic efficiency indirectly by Fenton reaction-mediated combination therapy, (iii) diagnosis and monitoring of cancer therapy. These strategies exhibit the potential of CDT-based nanomaterials for efficient cancer therapy.