Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

CHEMBL333687 5-(4-fluorophenyl)-1-[2- [(2R,4R)-4-hydroxy...

Synonyms: SureCN1258955, CHEBI:299976, AC1O5EXB, CTK8E9694, KB-195917, ...

Jacobsen, W. et al., Lilja, J.J. et al., Hermann, M. et al.

Hermann, Bogsrud, Molden, Asberg, Mohebi, Ose, Retterstøl,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of AIDS342648

However, patients with atorvastatin-related myopathy had 2.4-fold and 3.1-fold higher systemic exposures of the metabolites atorvastatin lactone (P<.01) and p-hydroxyatorvastatin (P<.01), respectively, compared with controls [1].

High impact information on AIDS342648

CONCLUSIONS: Grapefruit juice significantly increased serum concentrations of atorvastatin acid, atorvastatin lactone, and active and total HMG-CoA reductase inhibitors, probably by decreasing CYP3A4-mediated first-pass metabolism of atorvastatin in the small intestine [2].

Gene context of AIDS342648

Atorvastatin lactone had a significantly higher affinity to CYP3A4 than the acid (K(m): para-hydroxy atorvastatin, 25.6 +/- 5.0 microM; para-hydroxy atorvastatin lactone, 1.4 +/- 0.2 microM; ortho-hydroxy atorvastatin, 29.7 +/- 9.4 microM; and ortho-hydroxy atorvastatin lactone, 3.9 +/- 0.2 microM) [3].

References

Exposure of atorvastatin is unchanged but lactone and acid metabolites are increased several-fold in patients with atorvastatin-induced myopathy. Hermann, M., Bogsrud, M.P., Molden, E., Asberg, A., Mohebi, B.U., Ose, L., Retterstøl, K. Clin. Pharmacol. Ther. (2006) [Pubmed]
Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. Lilja, J.J., Kivistö, K.T., Neuvonen, P.J. Clin. Pharmacol. Ther. (1999) [Pubmed]
Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Jacobsen, W., Kuhn, B., Soldner, A., Kirchner, G., Sewing, K.F., Kollman, P.A., Benet, L.Z., Christians, U. Drug Metab. Dispos. (2000) [Pubmed]

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