In vivo drug interaction studies involving rosuvastatin and sulfasalazine indicating at least partial contribution by BCRP

ObjectObject DoseaPrecipitantPrecipitant Therapeutic ClassPrecipitant Dosea% Change in AUCbReference
Sulfasalazine2-g SDCurcuminFood products2-g SD220Kusuhara et al., 2012
500-mg SDPantoprazoleProton pump inhibitors40-mg SD83cAdkison et al., 2010
100-μg SDCurcuminFood products2-g SD83Kusuhara et al., 2012
Rosuvastatin10 mg QD × 10 daysCyclosporineImmunosuppressants75 to 200 mg BID (stable dose for at least 2 mo)610dSimonson et al., 2004
10-mg SDAtazanavir + ritonavirProtease inhibitors300 mg atazanavir + 100 mg ritonavir QD × 6 days210Busti et al., 2008
20 mg QD × 7 daysLopinavir + ritonavirProtease inhibitors400 mg lopinavir + 100 mg ritonavir BID × 7 days110Kiser et al., 2008
10-mg SDEltrombopagPlatelet-stimulating agents75 mg QD × 5 days55Allred et al., 2011
10-mg SDElvitegravir + cobicistatAIDS treatments150 mg elvitegravir + 150 mg cobicistat QD × 10 days40Custodio et al., 2014
10-mg SDTipranavir + ritonavirProtease inhibitors500 mg tipranavir + 200 mg ritonavir BID × 11 days37Pham et al., 2009
  • BID, twice daily; QD, once daily; SD, single dose.

  • a The route of administration was oral in all cases.

  • b Values were extracted from the Drug Interaction Database and calculated as the change in mean AUC values.

  • c AUC change observed with 421A/C genotype and was not statistically different from control.

  • d Change in AUC was calculated using healthy historical controls.