Chitosan, derived from chitin, is a biopolymer consisting of arbitrarily distributed β-(1-4)-linked D-glucosamine and N-acetyl-D-glucosamine that exhibits outstanding properties— biocompatibility, biodegradability, non-toxicity, antibacterial activity, the capacity to form films, and chelating of metal ions. Most of these peculiar properties are attributed to the presence of free protonable amino groups along the chitosan backbone, which also gives it solubility in acidic conditions. Moreover, this biopolymer can also be physically modified, thereby presenting a variety of forms to be developed. Consequently, this polysaccharide is used in various fields, such as tissue engineering, drug delivery systems, and cancer treatment. In this sense, this review aims to gather the state-of-the-art concerning this polysaccharide when used as a biomaterial, providing information about its characteristics, chemical modifications, and applications. We present the most relevant and new information about this polysaccharide-based biomaterial’s applications in distinct fields and also the ability of chitosan and its various derivatives to selectively permeate through the cancer cell membranes and exhibit anticancer activity, and the possibility of adding several therapeutic metal ions as a strategy to improve the therapeutic potential of this polymer.