The therapeutic potential of carbohydrates has been well demonstrated by the number of carbohydrate-based compounds, either synthetic, semi-synthetic or from natural sources for the treatment of disease states such as bacterial and viral infections, cancer or diabetes, to name only a few. The discovery of bioactive carbohydrates and their development toward a further pharmaceutical application involve interdisciplinarity studies bridging chemistry, biology, and pharmaceutical/medical sciences, such as carbohydrate chemistry, biochemistry, glycobiology, drug design, microbiology and oncology. The biological profile of these molecules arises by a variety of mechanisms, many of them relying on the interference with carbohydrate-dependent events, including the inhibition of carbohydrate-acting enzymes, inhibition of carbohydrate-protein or carbohydrate-carbohydrate interactions, interaction with biologically relevant carbohydrate-based structures or inhibition of their biosynthesis. Carbohydrate-based molecules offer additional important benefits which further enhances their pharmaceutical and biomedical interest, namely their polyfunctionalized nature and stereochemistry, which enable for a fine tuning and modulation of the biological and pharmacokinetic properties, their hydrophilicity, biocompatibility, and low toxicity. The articles included in this Research Topic illustrate how well carbohydrates may provide and contribute to ground-breaking therapeutic solutions, using novel carbohydrate chemistry strategies.