We conducted an investigator-initiated, prospective, two arm, crossover, randomized, controlled trial to evaluate the pharmacogenomic effect of drug transporters on rosuvastatin pharmacokinetics in Asian and White healthy volunteers. Recruitment was from the general public in the San Francisco/Bay area from November 2014 to July 2015. Each participant provided written informed consent.
Subjects were block randomly assigned to receive either an oral 20mg rosuvastatin tablet (
Crestor®, AstraZeneca, Wilmington, DE) first or an oral 20mg rosuvastatin tablet immediately following a 30-min intravenous infusion of rifampin (
Rifadin®, Sanofi-Aventis, Bridgewater, NJ) 600 mg in 10 ml sterile normal saline at a rate of 20 mg/min. The two periods were separated by at least a 7-day washout and all subjects completed both periods. To eliminate a food effect, subjects fasted from 8 hours prior to rosuvastatin dosing to 3 hours post dosing and standardized meals were provided. Venous blood samples (8 mL each) were collected into K3-EDTA tubes at t=0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 9, 12, 24, 32, 48 hours post dosing. Blood was centrifuged within 30 min at 4 °C and aliquot plasma samples were stored at −80 °C until bioanalysis.
Wu H.F., Hristeva N., Chang J., Liang X., Li R., Frassetto L, & Benet L.Z. (2017). Rosuvastatin pharmacokinetics in Asian and White subjects wild-type for both OATP1B1 and BCRP under control and inhibited conditions. Journal of pharmaceutical sciences, 106(9), 2751-2757.