Since less cholesterol is absorbed, less of it is delivered to the liver. Zetia binds to NPC1L1 and blocks the absorption of cholesterol and plant sterols in the intestine. Yolanda is a passionate medical writer who loves to help people understand how health and different treatments work. Inhibits sterol transporter at brush border and, consequently, intestinal absorption of cholesterol, which in turn decreases delivery of cholesterol to the liver and reduces hepatic cholesterol stores. Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. 12.1 Mechanism of Action. Mechanism of Action. Ezetimibe has a unique mechanism of action compared to other classes of lipid-lowering agents. 2 It inhibits the absorption of dietary and biliary cholesterol decreasing the intestinal absorption by 54%. Peak plasma time: 4-12 hr (parent drug); 1-2 hr (metabolite) Ezetimibe does not, however, affect triglyceride absorption. Yolanda. NPC1L1 (Niemann-Pick C1-Like 1) is a protein that transports sterols and cholesterol across the gut lining and absorbs them in the body [15, 16, 17]. Mechanism of Action. Absorption. Bioavailability: Variable. ZETIA is an inhibitor of intestinal cholesterol (and related phytosterol) ... 12.1 Mechanism of Action 12.2 Pharmacodynamics 12.3 Pharmacokinetics 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility 13.2 Animal Toxicology and/or Pharmacology . After graduating in Pharmacy in Australia, she moved to Italy to study the Mediterranean way of life and continue learning about health and medicine. In a 2-week clinical study in 18 hypercholesterolemic patients, ZETIA inhibited intestinal cholesterol absorption by 54%, compared with placebo.