Fluvastatin Pathway


Fluvastatin inhibits cholesterol synthesis via the mevalonate pathway by inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase is the enzyme responsible for the conversion of HMG-CoA to mevalonic acid, the rate-limiting step of cholesterol synthesis by this pathway. Fluvastatin bears a chemical resemblance to the reduced HMG-CoA reaction intermediate that is formed during catalysis. Fluvastatin was the first synthetically-prepared HMG-CoA reductase inhibitor. Although similar to lovastatin, simvastatin, and pravastatin, it has a shorter half-life, no active metabolites, extensive protein binding, and minimal CSF penetration. Cholesterol biosynthesis accounts for approximately 80% of cholesterol in the body; thus, inhibiting this process can significantly lower cholesterol levels.

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References

  1. Lescol/Lescol XL. (2009). [Electronic version]. e-CPS. Retrieved June 30, 2009.
  2. Reszka, A.A., & Rodan, G.A. (2003). Bisphosphonate mechanism of action. Current Rheumatology Reports, 5(1), 65-74. PMID: 12590887
  3. Schmidt, E.B., & Larsen, M.L. (2004). HMG-CoA-reductase-inhibitors. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 460-463). Berlin, Germany: Springer.