Abstract: Retinoic acid-related orphan receptor γt (RORγt), a member of the nuclear receptor family, is known as orphan nuclear receptor due to absence of recognizable natural ligands. Studies have shown that RORγt plays a significant role in the occurrence and development of inflammation and autoimmune diseases by regulating the differentiation of helper T cells 17 (Th17) and the expression of various cytokines. RORγt inhibitors, including antagonists and inverse agonists, can suppress the development of inflammation and autoimmune diseases. This review summarizes the structure and function of RORγt and its role in related inflammation and autoimmune diseases regulated by Th17, and provides a comprehensive overview of the development, clinical application and challenges of small molecule RORγt inhibitors in recent years, in order to offer some valuable insights for the development of small molecule RORγt inhibitors.