Accelerator mass spectrometry (AMS) has emerged as an important analytical tool in biomedical and pharmaceutical research. Its sensitivity (up to attomole, 10-18 levels), precision, low sample requirements and the ability to trace a biomarker over a prolonged period of time are valuable attributes. Metabolomic, kinetic, toxicokinetic and dosimetric studies of various chemical molecules, at environmental exposure levels and physiologically relevant doses, using radioisotopes (e.g. 14C, 3H, 26Al and 41Ca) are possible. AMS has contributed significantly to the understanding of DNA-adduct formation in carcinogenesis and is finding new uses in the changing drug development paradigm where more researchers are turning to biomarkers to predict functional and clinical outcomes in patients. Microdosing and first-in-human studies are also breakthroughs spearheaded by the innovative use of AMS. Recent advances see AMS driven into fields of phytochemical and nutritional research as well as clinical diagnosis and disease state monitoring. As a result of the high initial costs and forbidding size, developments in equipment miniaturization and enhanced sample throughput seek to overcome these barriers. AMS is expected to present new and exciting opportunities in biomedical research as its breadth of applications continues to expand. This article provides an insight into the pharmaceutical and biomedical applications of AMS.