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Topotecan

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
ABCC4 MRP4 1.66 HepG2-MRP4 Tian, 2006
SLC47A2 MATE2K 60 HEK293-MATE2K Tanihara, 2007
SLC47A1 MATE1 70 HEK293-MATE1 Tanihara, 2007
ABCB1 MDR1, P-gp 78.3 Caco-2 Li, 2008
ABCB1 MDR1, P-gp 102 MDCK II-MDR1 Li, 2008
ABCG2 BCRP, MXR 213 MDCK II-BCRP Li, 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
SLC22A2 OCT2 Topotecan 61 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Wittwer, 2013
SLC47A1 MATE1 Topotecan 1.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC47A2 MATE2K Topotecan 8.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013

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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 ABCB1/ABCG2 Elacridar (GF120918) Topotecan 2.4 2.8 ND ND NS ND Kruijtzer, 2002 DDI 1

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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