The proliferation of Virtual Reality-based tools has led to its increased usage in the field of education over the last decades owing to its increasingly realistic simulation and greater control over the 3D simulated environment. The unique features of Virtual Reality (VR) simulation can provide learners with a hazard-free simulated environment allowing limitless failure attempts. Yet, good quality research to verify the effectiveness of VR simulation in training students of the health profession is still lacking. This literature review focuses on the effectiveness of virtual reality-based simulation in enhancing health profession students' empathetic attitude relating to mental illness. Four databases were searched from January 1, 2007 to December 31, 2018. Of 1034 articles identified eligible in the databases, a total of 6 articles have met the criteria for inclusion in this review. Findings suggested that there is a clear relationship between VR simulation and an improvement on users' empathy, attitudes, and knowledge relating to mental Illness. With the unique characteristic of experiential learning of VR simulation, there is a potential development of the VR simulation on empathy and attitude in healthcare education. Also, VR stimulation is found having a larger impact on the users' empathy of users with a healthcare background compared to those without. Future studies should include more in-depth examination on the effect on the specificity of empathy and attitude of people with healthcare background, and in teaching a wider range of mental illnesses such as depression and general anxiety disorder.