Introduction: Boron-containing compounds (BCCs) are attractive chemical entities in drug development. Some of these compounds have been used in the treatment of human disease, and studies on their pharmacodynamics suggest that they employ multiple forms of activity. However, less is known about the pharmacokinetic profile of these molecules. Areas covered: The herein compiled reported data is presented in accordance with the classical ADME' system for identifying the scope of BCCs in the respective fields. Our analysis suggests that these compounds have several distinct ways to move within the human body, and that the specific structural features of each molecule account for its distinct pharmacokinetic profile. These insights should be useful for designing BCCs with a desired effect. Expert opinion: Increasing knowledge about the pharmacokinetics of BCCs is providing a broader understanding about the design of new release systems and potential drugs, as well as probable protein transporters that could be related to key roles in physiological processes. These transporters may be involved in sodium transport, hormone release and regulation of the cell cycle. The shared features among groups of BCCs are being identified in order to apply these insights to the design of advantageous compounds.