Human health is considered the most important goal of all. The use of different materials in biomedical applications, such as pharmacy (drug delivery systems), regenerative medicine (implantable biomaterials, wound dressings), and biomedical or tissue engineering (cell scaffolds), is of the utmost importance right now. Therefore, the development of new organic–inorganic biomaterials is currently the hot topic. Zeolites and zeolite imidazolate frameworks (ZIFs) belong to different chemical groups but their structural similarity and superior properties place them among the most interesting materials that could be used for various biomedical applications. Despite their properties, the application of these materials in the aforementioned fields of study is quite new and requires further research and systematisation. The following work reviews the most recent applications of zeolites and ZIFs in the biomedical field with the strongest emphasis on the polymer/zeolite or polymer/ZIFs composites or hybrid biomaterials. In addition, the application of such systems as drug carriers and in the regenerative medicine, especially in the treatment of osteoporosis, is described and summarized. Moreover, the discussion of antimicrobial and anticancer mechanisms of zeolite/ZIF-based biomaterials was included. The presented literature review clearly shows that zeolites/ZIFs loaded biomaterials are becoming a good alternative to already existing therapeutic routes as advanced healthcare materials. Some remarks on the challenges and future prospects in terms of stability-instability, stimuli-responsive materials, and toxicity are also presented. Therefore, this work is a tale of zeolites and ZIFs on the quest to find the ideal biomaterial for biomedical applications. The question is: will they succeed? Let us find out.