Over the last two decades, advancements in nanomaterials and nanoscience have paved the path for the emergence of nano-medical convergence science, significantly impacting healthcare. In our review, we highlight how these advancements are applied in various biomedical technologies such as drug delivery systems, bio-imaging for diagnostic and therapeutic purposes. Recently, novel inorganic nanohybrid drugs have been developed, combining multifunctional inorganic nanomaterials with therapeutic agents (known as inorganic medicinal nanoarchitectonics). These innovative drugs are actively utilized in cutting-edge medical treatments, including targeted anti-cancer therapy, photo and radiation therapy, and immunotherapy. This review provides a detailed overview of the current development status of inorganic medicinal nanoarchitectonics and explores potential future directions in their advancements.