Title : Effects of drug interactions on biotransformation and antiplatelet effect of clopidogrel in vitro.

Pub. Date : 2010 Sep

PMID : 20735423






7 Functional Relationships(s)
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1 KEY RESULTS: Experiments using HLM or specific CYPs (3A4, 2C19) revealed that at clopidogrel concentrations >10 microM, CYP3A4 was primarily responsible for clopidogrel biotransformation. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 KEY RESULTS: Experiments using HLM or specific CYPs (3A4, 2C19) revealed that at clopidogrel concentrations >10 microM, CYP3A4 was primarily responsible for clopidogrel biotransformation. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Clarithromycin, another CYP3A4 inhibitor, impaired clopidogrel biotransformation and antiplatelet activity almost as effectively as ketoconazole. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 The CYP3A4 substrates atorvastatin and simvastatin both inhibited clopidogrel biotransformation and antiplatelet activity, less potently than ketoconazole. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 CONCLUSIONS AND IMPLICATIONS: At clopidogrel concentrations >10 microM, CYP3A4 is mainly responsible for clopidogrel biotransformation, whereas CYP2C19 contributes only at clopidogrel concentrations < or =10 microM. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
6 CONCLUSIONS AND IMPLICATIONS: At clopidogrel concentrations >10 microM, CYP3A4 is mainly responsible for clopidogrel biotransformation, whereas CYP2C19 contributes only at clopidogrel concentrations < or =10 microM. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens
7 CONCLUSIONS AND IMPLICATIONS: At clopidogrel concentrations >10 microM, CYP3A4 is mainly responsible for clopidogrel biotransformation, whereas CYP2C19 contributes only at clopidogrel concentrations < or =10 microM. Clopidogrel cytochrome P450 family 3 subfamily A member 4 Homo sapiens