Inhibition of intestinal cholesterol absorption by ezetimibe in humans

  • Sudhop T
  • Lutjohann D
  • Kodal A
 et al. 
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Background - Ezetimibe has been shown to inhibit cholesterol absorption in animal models, but studies on cholesterol absorption in humans have not been performed thus far. Methods and Results - The effect of ezetimibe (10 mg/d) on cholesterol absorption and synthesis, sterol excretion, and plasma concentrations of cholesterol and noncholesterol sterols was investigated in a randomized, double-blind, placebo-controlled, crossover study in 18 patients with mild to moderate hypercholesterolemia. Treatment periods lasted 2 weeks with an intervening 2-week washout period. Fractional cholesterol absorption rates averaged 49.8±13.8% on placebo and 22.7±25.8% on ezetimibe, indicating a reduction of 54% (geometric mean ratio; P

Author-supplied keywords

  • Cholesterol absorption
  • Cholesterol synthesis
  • Ezetimibe
  • Lathosterol
  • Plant sterols

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  • Thomas Sudhop

  • Dieter Lutjohann

  • Annette Kodal

  • Diane L. Tribble

  • Sukrut Shah

  • Inna Perevozskaya

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