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Sirolimus

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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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 Sirolimus 1.53 Basal activity High Five insect cell crude membranes Pawarode, 2007
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Sirolimus 6.49 Bromsulphthalein HEK-OATP1B1 Oswald, 2010
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Sirolimus 1.1 Demethylphalloin HEK293 cells Fehrenbach, 2003
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Sirolimus 0.22 Estradiol-17beta-glucuronide HEK-OATP1B1 Farasyn, 2019
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Sirolimus 0.65 Estrone sulfate HEK-OATP1B1 Farasyn, 2019
SLCO1B3 OATP1B3, OATP8 Sirolimus 1.3 Mycophenolic acid 7-O-glucuronide HEK293-OATP1B3 Farasyn, 2019
ABCB1 MDR1, P-gp Sirolimus 1.3 Rhodamine 123 Caco-2 cells Wacher, 2002
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Sirolimus 0.32 Rosuvastatin HEK-OATP1B1 Farasyn, 2019

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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