Supramolecular chemistry is a useful methodology for construction of nano- or micro-sized objects and can significantly contribute to nanotechnology through so-called bottom-up processing. In addition, supramolecular self-assembled structures can mimic some aspects of biological systems. Bio-related functions such as molecular sensing, controlled release, signaling and materials separations have been realized. Supramolecular chemistry is a multidisciplinary field that includes subjects such as molecular design and nanosized materials. In this article recent examples of supramolecular chemistry in the context of biological therapy are introduced and classified into five categories: small supramolecular systems; designer polymers; self-assembled structures; predesigned assemblies; and nanomaterials. Finally, hierarchic organization of supramolecular structures for advanced functions is introduced to illustrate future directions of investigation. We hope that scientists studying therapeutic applications receive inspiration from this review to exploit the opportunities offered by supramolecular chemistry in their respective research areas.