Autism spectrum disorder is a developmental disability affecting 1 in every 59 newborns and causes significant morbidity while exact pathophysiology is unclear. Recent hypothesis includes vasopressin in patients with ASD while vasopressin receptor antagonists including balovaptan appears to be promising option for treatment especially in ASD patients with high functionality. In this study, our aim is to describe recent developments in vasopressin receptor antagonists involving ASD treatment which have potential for future clinical implementation.