The treatment of cancer remains one of the most challenging problems for humanity. Boron neutron capture therapy is a binary approach for cancer treatment that is particularly attractive in treating high-grade gliomas and metastatic brain tumors. Among the types of boron-containing molecules used as boron neutron capture therapy agents, boronated carbohydrate derivatives have received significant attention because of their preferential uptake by growing tumor cells. This review provides a summary of the recent developments in the chemistry of carborane-containing carbohydrates.