ABSTRACT: Cancer is one of the significant threats to human life. Although various latest technologies are currently available to treat cancer, it still accounts for millions of death each year worldwide. Thus, creating a need for more developed and novel technologies to combat this deadly condition. Nanoparticles-based cancer therapeutics have offered a promising approach to treat cancer effectively while minimizing adverse events. Among various nanoparticles, nanogold (AuNPs) are biocompatible and have proved their efficiency in treating cancer because they can reach tumors via enhanced permeability and retention effect. The size and shape of the AuNPs are responsible for their diverse therapeutic behavior. Thus, to modulate their therapeutic values, the AuNPs can be synthesized in various shapes, such as spheres, cages, flowers, shells, prisms, rods, clusters, etc. Also, attaching AuNPs with single or multiple targeting agents can facilitate the active targeting of AuNPs to the tumor tissue. The AuNPs have been much explored for photothermal therapy (PTT) to treat cancer. In addition to PTT, AuNPs-based nanoplatforms have been investigated for combinational multimodal therapies in the last few years, including photodynamic therapy, chemotherapy, radiotherapy, immunotherapy, etc., to ablate cancer cells. Thus, the present review focuses on the recent advancements in the functionalization of AuNPs-based nanoconstructs for cancer imaging and therapy using combinatorial multimodal approaches to treat various cancers.