At present, the pharmacological mechanism of the three main drugs for the treatment of atherosclerosis, 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase inhibitors, Niemann-pick C1-like protein 1 (NPC1L1) inhibitors, and proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, is mainly to reduce cholesterol through affecting the synthesis, absorption, and degradation of cholesterol, respectively. Here, NPC1L1 is linked to atherosclerosis.