Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin.

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Citation

Pasanen MK, Fredrikson H, Neuvonen PJ, Niemi M

Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin.

Clin Pharmacol Ther. 2007 Dec;82(6):726-33. doi: 10.1038/sj.clpt.6100220. Epub 2007 May 2.

PubMed ID
17473846 [ View in PubMed
]
Abstract

Thirty-two healthy volunteers with different SLCO1B1 genotypes ingested a 20 mg dose of atorvastatin and 10 mg dose of rosuvastatin with a washout period of 1 week. Subjects with the SLCO1B1 c.521CC genotype (n=4) had a 144% (P<0.001) or 61% (P=0.049) greater mean area under the plasma atorvastatin concentration-time curve from 0 to 48 h (AUC(0-48 h)) than those with the c.521TT (n=16) or c.521TC (n=12) genotype, respectively. The AUC(0-48 h) of 2-hydroxyatorvastatin was 100% greater in subjects with the c.521CC genotype than in those with the c.521TT genotype (P=0.018). Rosuvastatin AUC(0-48 h) and peak plasma concentration (Cmax) were 65% (P=0.002) and 79% (P=0.003) higher in subjects with the c.521CC genotype than in those with the c.521TT genotype. These results indicate that, unexpectedly, SLCO1B1 polymorphism has a larger effect on the AUC of atorvastatin than on the more hydrophilic rosuvastatin.

DrugBank Data that Cites this Article

Drugs
Drug Interactions
DrugsInteraction
Rosuvastatin
Cyclosporine
The serum concentration of Rosuvastatin can be increased when it is combined with Cyclosporine.