Glioblastoma (GBM) is the most aggressive malignant brain tumor in adults. Cholesterol is an essential component of cells,and the synthesis, transport and metabolism of cholesterol play important roles in the occurrence and development of tumors. Cholester-ol homeostasis-related regulators such as niemann-pick-like C-type protein (NPC1) and sterol O-acyltransferase (SOAT1), have recentlybecome potential new drug intervention targets for tumor therapy. The study elaborates the possible therapeutic effects of small-mole- cule drugs targeting cholesterol homeostasis in GBM.