Over the past few decades, gold nanomaterials have shown great promise in the field of nanotechnology, especially in medical and biological applications. They have become the most used nanomaterials in those fields due to their several advantageous. However, rod-shaped gold nanoparticles, or gold nanorods (GNRs), have some more unique physical, optical, and chemical properties, making them proper candidates for biomedical applications including drug/gene delivery, photothermal/photodynamic therapy, and theranostics. Most of their therapeutic applications are based on their ability for tunable heat generation upon exposure to near-infrared (NIR) radiation, which is helpful in both NIR-responsive cargo delivery and photothermal/photodynamic therapies. In this review, a comprehensive insight into the properties, synthesis methods and toxicity of gold nanorods are overviewed first. For the main body of the review, the therapeutic applications of GNRs are provided in four main sections: (i) drug delivery, (ii) gene delivery, (iii) photothermal/photodynamic therapy, and (iv) theranostics applications. Finally, the challenges and future perspectives of their therapeutic application are discussed.