Title : Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide.

Pub. Date : 2006 Mar

PMID : 16447051






3 Functional Relationships(s)
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1 Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide. Pioglitazone cytochrome P450 family 2 subfamily C member 8 Homo sapiens
2 OBJECTIVE: Pioglitazone, a thiazolidinedione antidiabetic, inhibits cytochrome P450 (CYP) 2C8 and CYP3A4 enzymes in vitro. Pioglitazone cytochrome P450 family 2 subfamily C member 8 Homo sapiens
3 CONCLUSIONS: Pioglitazone does not increase the plasma concentrations of repaglinide, indicating that the inhibitory effect of pioglitazone on CYP2C8 and CYP3A4 is very weak in vivo, probably due to its extensive plasma protein binding. Pioglitazone cytochrome P450 family 2 subfamily C member 8 Homo sapiens