Metal–organic frameworks (MOFs), a burgeoning class of coordination polymers, have garnered significant attention due to their outstanding structure, porosity, and stability. They have been extensively studied in catalysis, energy storage, water harvesting, selective gas separation, and electrochemical applications. Recent advancements in post-synthetic strategies, surface functionality, and biocompatibility have expanded the application scope of MOFs, particularly in various biomedical fields. Herein, we review MOF-based nanomaterials bioimaging nanoplatforms in magnetic resonance imaging, computed tomography, and fluorescence imaging. MOFs serve as the foundation for biosensors, demonstrating efficiency in sensing H₂O₂, tumor biomarkers, microRNA, and living cancer cells. MOF-based carriers are well designed in drug delivery systems and anticancer treatment therapies. Additionally, we examine the challenges and prospects of MOFs in surface modification, release of metal ions, and interaction with intracellular components, as well as their toxicity and long-term effects.