Pub. Date : 2010 Jul
PMID : 20590614
10 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 2 | Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 3 | BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 4 | BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 5 | Here, we have assessed the individual and combined effects of CYP3A, ABCB1 and ABCC2 on the pharmacokinetics of lopinavir and the relative importance of intestinal and hepatic metabolism. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 6 | Increased lopinavir AUC(oral) (>2000-fold) was observed in cytochrome P450 3A knockout (Cyp3a(-/-)) mice compared with wild-type mice. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 7 | Increased lopinavir AUC(oral) (>2000-fold) was observed in cytochrome P450 3A knockout (Cyp3a(-/-)) mice compared with wild-type mice. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 8 | CONCLUSIONS AND IMPLICATIONS: CYP3A was the major determinant of lopinavir pharmacokinetics, far more than Abcb1a/b. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 9 | Both intestinal and hepatic CYP3A activity contributed importantly to low oral bioavailability of lopinavir. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |
| 10 | Ritonavir increased lopinavir bioavailability primarily by inhibiting CYP3A. | Lopinavir | cytochrome P450, family 3, subfamily a, polypeptide 11 | Mus musculus |