Cyclodextrins (CDs) are cyclic oligosaccharides of natural origin composed of alfa-(1,4) linked glucopyranose subunits. They possess a cone-like supramolecular structure expressing a lipophilic cavity and a hydrophilic external surface that allows to spontaneously complex poorly soluble compounds in an aqueous environment. As a result of molecular complexation phenomena CDs are widely used in many fields, including cosmetic and food industries, and especially have been widely utilized as pharmaceutical excipients and drug carriers in the pharmaceutical field. Nowadays, several research groups all over the world are investigating their potential as active pharmaceutical ingredients (APIs) for the treatment of various illnesses (atherosclerosis, dyslipidemia, obesity, diabetes, neurodegenerative diseases, cancer, in vitro fertilization etc.). Sugammadex is first cyclodextrin approved as drug for reversal of neuromuscular blocade induced by rocuronium or veruconium in adults. It provides rapid and predictable reversal of neuromuscular blockade with little adverse reactions. Due to sugammadex effectiveness and safety profile it is expected that CD-based molecules will be developed further and contribute to improvement of quality of life of patients with a broad spectrum of diseases. The aim of this review is to briefly summarize the recent and future applications of cyclodextrins in pharmaceutics as new APIs.