Over the past decade, there has been a rising interest in the use of carboranes as a potential pharmacophoric moiety in the development of new drugs for the treatment of various types of cancer. The unique physical and chemical properties of carboranes make their use attractive in drug development. In several instances, the inclusion of carboranes into a drug structure has increased the agent's binding affinity, potency, or bioavailability. The purpose of this review is to highlight applications of carboranes to the medicinal chemistry of cancer.