Carbon nanotubes were introduced in the 21st century into biomedicine for the delivery of therapeutic, diagnostic and imaging agents. CNTs are unique one-dimensional structures having fascinating physical, mechanical and chemical properties and also drug loading properties. Ease in cellular uptake allows them to be explored for a wide range of applications in biology and medicine. This current review is an informative compiling of the origin of CNTs, and how CNTs are used in different aspects of biomedicine including drug delivery and cancer treatment, bio-sensing, biomedical imaging, and tissue engineering. The current review also focuses on the pharmacokinetics, toxicity, and metabolism of CNTs and discusses the potential advantages and obstacles associated with biomedical applications.