3-Hydroxy-3-methylglutaryl Coenzyme A Reductase Inhibitors

  • D. R. Illingworth
  • E. B. Schmidt
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 109)


Delineation of the mechanisms responsible for the maintenance of cholesterol homeostasis in humans has provided a sound scientific basis for the development of drugs which act to inhibit key enzymes in the pathway of cholesterol biosynthesis. In humans, the majority of cholesterol which is transported in plasma lipoproteins is derived from de novo synthesis rather than from dietary sources (Brown and Goldstein 1986). Conversion of 3-hydroxy-3methylglutaryl coenzyme A (HMG-CoA) to mevalonic acid by the enzyme HMG-CoA reductase is the rate-limiting enzyme in cholesterol biosynthesis and is subject to metabolic regulation. Other enzymes, including HMG-CoA synthase and squalene synthase, are also subject to metabolic regulation.


Reductase Inhibitor Familial Hypercholesterolemia Familial Hypercholesterolemia Mevalonic Acid Bile Acid Sequestrant 
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© Springer-Verlag Berlin Heidelberg 1994

Authors and Affiliations

  • D. R. Illingworth
  • E. B. Schmidt

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