Zeolitic Imidazolate Frameworks (ZIFs) are a type of metal-organic framework (MOF) composed of imidazole ligands and zinc ions. They have been identified as a promising platform for developing theranostics, including nanocarriers for drug delivery and fluorescent molecules. ZIF materials are suitable matrices for encapsulating enzymes, medicinal molecules, and nanoparticles due to their high biocompatibility. Moreover, these compounds are susceptible to degradation in acidic conditions or in the presence of competing ligands, rendering them a valuable basis for constructing sensitive theranostic systems. ZIF showed identical physiochemical characteristics, which facilitated the evaluation of size-dependent biological components of the organisms. ZIFs exhibit potential for diverse biological applications such as bioimaging, biosensing, drug delivery, and theranostic. This review will focus on the biomedical applications of ZIFs, including biosensing, drug delivery, bioimaging, and theranostic applications.