The purpose of this study is to provide a critical reflection on the direction of pharmacological moral education in the era of transhumanism. In other words, it is intended to examine a method to improve moral ability through pharmacological methods, which is one of the methods to improve human morality. The pharmacological approach has a deep connection with the phenomenon of medicalization or biomedicalization in theory, but the recent biomedicalization approach focuses on improving moral life beyond the purpose of treatment, and biotechnology. This is because the technology that was oriented towards nature or things has now turned to human beings, but it is necessary to pay attention to the effect of technology in relation to the phenomenon of biomedicalization. For this reason, this study tried to examine how the medicalization and biomedicalization of pharmacology first colonized the fields of mental health and happiness education, and what limitations were expressed. We will examine whether these limitations can have certain technical limitations as they are connected in the realm of moral improvement and virtue reinforcement. Not only that, but also ethically, it reveals that the trend of pharmacological human improvement research, which focuses on the importance and role of emotions in moral judgment, has one-sided limitations. I wanted to suggest what the limitations are. Although the boundary between treatment and improvement is unclear through advanced science and technology, it is suggested that the pursuit of improvement as well as treatment has considerable limitations. In the end, it was emphasized that the pharmacological approach in transhumanism’s moral improvement project did not yet elevate the moral action ability of human beings. In other words, it was suggested that there is a need to properly try traditional moral education through a virtue education approach.