With advances in nanotechnology, various new drug delivery systems (DDSs) have emerged and played a key role in the diagnosis and treatment of cancers. Over the last two decades, gold nanocages (AuNCs) have been attracting considerable attention because of their outstanding properties. This review summarizes current advancements in endogenous, exogenous, and dual/multi-stimuli responsive AuNCs in drug delivery. This review focuses on the properties, clinical translation potential, and limitations of stimuli-responsive AuNCs for cancer diagnosis and treatment.