Cyclodextrins (CDs) are cyclic oligosaccharides of natural origin composed of a-(1,4) linked glucopyranose subunits. They possess a cone-like supramolecular structure expressing a lipophilic cavity and a hydrophilic external surface that allows spontaneous inclusion complexation of 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, while CDs have been especially widely utilized as pharmaceutical excipients and drug carriers in the pharmaceutical field. Nowadays, a growing amount of evidence is demonstrating that CDs may represent a highly efficient tool in the development of useful therapies based on their lipid-extracting action. Several research groups all over the world are investigating their potential as active pharmaceutical ingredients (APis) for the prevention and treatment of various medical conditions like atherosclerosis, dyslipidaemia, obesity, diabetes, neurodegenerative diseases, cancer, in vitro fertilization etc. Sugammadex is the first approved CD-based drug for reversal of neuromuscular blockade induced by rocuronium or vecuronium 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 the improvement of quality of life of patients with a broad spectrum of diseases. This review briefly summarizes the recent and future applications of CD as potential new APis in modern medicine.