Title : In Vitro Evidence of Potential Interactions between CYP2C8 and Candesartan Acyl-β-D-glucuronide in the Liver.

Pub. Date : 2021 Apr

PMID : 33446524






4 Functional Relationships(s)
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1 Taken together, these data suggest that candesartan acyl-beta-D-glucuronide is actively transported by OATPs into hepatocytes, and drug-drug interactions may occur with coadministration of candesartan and CYP2C8 substrates including paclitaxel as a result of the inhibition of CYP2C8 function. candesartan cytochrome P450 family 2 subfamily C member 8 Homo sapiens
2 Taken together, these data suggest that candesartan acyl-beta-D-glucuronide is actively transported by OATPs into hepatocytes, and drug-drug interactions may occur with coadministration of candesartan and CYP2C8 substrates including paclitaxel as a result of the inhibition of CYP2C8 function. candesartan cytochrome P450 family 2 subfamily C member 8 Homo sapiens
3 Significance Statement This study demonstrates that the acyl glucuronidation of candesartan to form candesartan acyl-beta-D-glucuronide enhances CYP2C8 inhibition while exerting minimal effects on CYP3A4, OATP1B1, and OATP1B3. candesartan cytochrome P450 family 2 subfamily C member 8 Homo sapiens
4 Thus, candesartan acyl-beta-D-glucuronide might represent a potential mediator of drug-drug interactions between candesartan and CYP2C8 substrates, such as paclitaxel, in clinical settings. candesartan cytochrome P450 family 2 subfamily C member 8 Homo sapiens