Studies on the biological properties of fullerene C(60) and its derivatives started a decade ago as curiosity-driven studies and are now flourishing as an area of transdisciplinary research. This paper summarizes the results of studies on the biological activity and applications of selected functionalized fullerenes that were published in the last few years. Apart from literature data, we present most of our results of in vitro and in vivo studies with fullerenol C(60)(OH)(24) anti-oxidative and free radical scavenger activities in chemical and biological systems; cytotoxicity against human tumor cell lines; protective effects against various cytotoxic drugs and irradiation; effects on cell cycle and apoptosis, and in vivo radioprotective and cardioprotective effects. The fullerene family of carbon molecules has been a central focus in the emerging fields of nanotechnology and nanomedicine. Fullerenes take an important place in the development of nanobiotechnology and nanomedicine-related products.