Carbon nanotubes (CNT) are allotropes of carbon with a cylindrical nanostructure. They have recently aroused great interests as drug carriers, but their pharmacokinetic profiles which determine their potentials in clinical application are yet to be fully understood. Therefore, this overview attempts to outline the processes of absorption, distribution, metabolism and excretion (ADME) that govern the pharmacokinetics of CNT. In addition, the molecular mechanisms of intracellular internalization and drug release are also discussed.