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Elacridar (GF120918)

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
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.027 Colchicine MDCK II-MDR1 Rautio, 2006
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.39 Digoxin Caco-2 Tang, 2002
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.44 Digoxin MDCK-MDR1 Tang, 2002
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.18 Digoxin MDCKII-MDR1 Keogh, 2006
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.055 Digoxin MDCK II-MDR1 Rautio, 2006
ABCG2 BCRP, MXR Elacridar (GF120918) 0.31 Mitoxantrone HEK293-BCRP Ahmed-Belkacem, 2005
ABCB1 MDR1, P-gp Elacridar (GF120918) 0.043 Vinblastine MDCK II-MDR1 Rautio, 2006

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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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