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Rosuvastatin

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
ABCG2* BCRP, MXR 2.02 BCRP-expressing HEK293 vesicles Kitamura, 2008
ABCG2* BCRP, MXR 10.1 MDCK II-BCRP Deng, 2008
SLC10A1 NTCP 65 HeLa-NTCP Ho, 2006
SLC22A8 OAT3 7.4 OAT3-expressing oocytes Windass, 2007
SLCO1A2* OATP1A2, OATP-A 2.6 HeLa-OATP1A2 Ho, 2006
SLCO1B1* OATP1B1, OATP-C, OATP2, LST-1 0.8 HEK293-OATP1B1 Kitamura, 2008
SLCO1B1* OATP1B1, OATP-C, OATP2, LST-1 4 HeLa-OATP1B1 Ho, 2006
SLCO1B1* OATP1B1, OATP-C, OATP2, LST-1 7.3 HeLa-OATP1B1 Ho, 2006
SLCO1B1* OATP1B1, OATP-C, OATP2, LST-1 8.5 OATP1B1-expressing oocytes Simonson, 2004
SLCO1B3* OATP1B3, OATP8 9.8 HeLa-OATP1B3 Ho, 2006
SLCO1B3* OATP1B3, OATP8 14.2 HEK293-OATP1B3 Kitamura, 2008
SLCO2B1 OATP2B1, OATP-B 2.4 HeLa-OATP2B1 Ho, 2006
SLCO2B1 OATP2B1, OATP-B 6.42 HEK293-OATP2B1 Kitamura, 2008

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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
ABCG2 BCRP, MXR Rosuvastatin 15.4 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005

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Clinical Drug-Drug Interactions

DDI Implicated Transporter* Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 ABCG2/OATPs Atazanavir / Ritonavir Rosuvastatin 3.1 7.0 ND ND ND ND Busti, 2008 DDI 1
2 ABCG2/OATPs Cyclosporine Rosuvastatin 5.0 10.6 ND ND ND ND Simonson, 2004 DDI 2
3 ABCG2/OATPs Cyclosporine Rosuvastatin 6.4 18.2 ND ND ND ND Simonson, 2004 DDI 3
4 OATPs Lopinavir / Ritonavir Rosuvastatin 2.1 4.7 ND 0.5 NS yes Kiser, 2008 DDI 4

PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value


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