The difficulty of achieving targeted drug delivery following administration of currently marketed anticancer therapeutics is a still a concern. Metallic nanoparticles (NPs) developed through nanotechnology breakthroughs appear to be promising in this regard. Research studies pertaining to gold NPs have indicated their promising applicability in cancer diagnosis, drug delivery and therapy. These NPs have also recently paved the path for precise drug delivery and site-specific targeting. Our review paper thus highlights the scope and impact of biogenetically generated gold nanoparticles (NPs) in cancer therapy. In a critical, constructive, and methodical manner, we compare the advantages offered by gold NPs over other metal NPs. Moreover, we also focus on novel ‘greener’ strategies that have been recently explored for the preparation of gold NPs and shed light on the disadvantages of conventional NP synthesis routes. Future prospects pertaining to the use of gold NPs in oncotherapy and domains that require further investigation are also addressed.