Nanomaterials with controlled physical, chemical, and biological characteristics can be used for the therapy of the specific causes of the diseases. There are several ways to develop new materials in nanometer scale. Mainly, top‐down and bottom‐up approaches are the two major techniques to produce nanomaterials. Depending on the application area, either one or both of these approaches can be used to develop materials that can be used in studying pathophysiology of diseases and their diagnosis and therapy. Especially, bioinspired and biomimetic strategies yield products that can replace or accommodate activities of the natural biomolecules. Nevertheless, for effective diagnosis and therapy of diseases, it is almost crucial to first understand the molecular reasons behind disease development. The nanomaterials can be also used in regenerative medicine applications. Although there have been extensive advances in developing nanomaterials for biomedical purposes, only few of them have been translated into clinics.