In the past few years, there has been an unprecedented development of gold nanomaterials (AuNMs) for potential clinical applications. Owing to their advantageous physical, chemical, and biological properties, AuNMs have attracted great attention in the nanomedicine arena for applications in biological sensing, biomedical imaging, drug delivery, and photothermal therapy. Their tunable size, shape, and surface characteristics coupled with excellent biocompatibility render them ideal candidates for translation from bench-top to bedside. This review summarizes the recent research on the applications of AuNM with a focus on biomedical diagnostics and therapeutics. The bio-interaction of these NM with cells and their in vivo responses are presented. After reviewing these potential applications, future challenges and prospects are discussed and the suitability of how AuNMs are used as effective tools in clinical medicine is assessed.