The FDA recommends rosuvastatin dosage reductions in Asian patients because pharmacokinetic studies have demonstrated an approximate two-fold increase in median exposure to rosuvastatin in Asian subjects when compared to Caucasian controls. Yet, no explanation for this ethnic difference has been confirmed.
Here we show that rosuvastatin exposure in Asians and Whites does not differ significantly when all subjects are wildtype carriers for both Solute Carrier Organic anion transporter1B1 *1a and ATP Binding Cassette Subfamily G Member 2 c.421 transporters in a two arm, randomized, cross-over rosuvastatin pharmacokinetics study in healthy White and Asian volunteers. For single rosuvastatin doses, AUC0–48 were 92.5(±36.2) and 83.5(±32.2) ng/mL*hr and Cmax were 10.0(±4.1) and 7.6(±3.0) ng/mL for Asians and Whites, respectively. When transporters were inhibited by intravenous rifampin, rosuvastatin AUC0–48 and Cmax also showed no ethnic differences. Our study suggests that both SLCO1B1 and ABCG2 polymorphisms are better predictors of rosuvastatin exposure than ethnicity alone and could be considered in precision medicine dosing of rosuvastatin.
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