Tumor-associated carbohydrate antigens (TACAs) have been described as a novel class of targets for anticancer therapy. Based on the multiple biological effects associated with them, inhibition of TACA signaling could directly impact on cancer growth, invasion, and metastasis. Besides, it can restore the recognition of tumors by the immune system, for example, by diminishing activity of checkpoint inhibitors. Due to their abundance on cancer cells, TACAs represent interesting targets for prophylactic and therapeutic vaccination strategies, as well as for immunotherapy. This chapter summarizes the current knowledge on cancer-related glycans and how they can be used as diagnostic or therapeutic targets. Moreover, novel therapeutic modalities including antibody-drug conjugates, bispecific T cell engagers, and CAR T/NK cells that are explored in preclinical or early clinical studies against these targets will be described and analyzed.