T-0901317, also known as T-1317; TO-091317; TO 901317, is a liver X receptor (LXR) agonist. T-0901317 inhibits development of atherosclerosis in LDL receptor-deficient mice. T-0901317 significantly reduced the atherosclerotic lesions in LDLR(-/-) mice without affecting plasma total cholesterol levels. T-0901317 increased expression of ATP binding cassette A1 in the lesions in LDLR(-/-) mice as well as in mouse peritoneal macrophages. T-0901317 also significantly induced cholesterol efflux activity in peritoneal macrophages. T-0901317 may be useful therapeutic agents for the treatment of atherosclerosis.