Title : Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers.

Pub. Date : 2014 Jan

PMID : 24240480






8 Functional Relationships(s)
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1 The peak plasma concentration of quetiapine was 208.39 ng/ml for CYP3A5*1/*1, 243.46 ng/ml for CYP3A5*1/*3, and 332.94 ng/ml for CYP3A5*3/*3 (P=0.0118). Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
2 Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers. Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
3 Quetiapine is metabolized by CYP3A enzymes including CYP3A5 and is a substrate of P-glycoprotein, an efflux drug transporter encoded by the ABCB1 gene. Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
4 However, the CYP3A5*3 polymorphism significantly affected the plasma level of quetiapine and its pharmacokinetics. Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
5 The peak plasma concentration of quetiapine was 208.39 ng/ml for CYP3A5*1/*1, 243.46 ng/ml for CYP3A5*1/*3, and 332.94 ng/ml for CYP3A5*3/*3 (P=0.0118). Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
6 The peak plasma concentration of quetiapine was 208.39 ng/ml for CYP3A5*1/*1, 243.46 ng/ml for CYP3A5*1/*3, and 332.94 ng/ml for CYP3A5*3/*3 (P=0.0118). Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
7 CONCLUSION: The results indicated that the genetic polymorphism of CYP3A5*3 but not ABCB1 significantly influences the plasma level of quetiapine and its pharmacokinetics. Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens
8 These findings suggest that the CYP3A5 genetic polymorphism affects the disposition of quetiapine and provide a plausible explanation for interindividual variation in the disposition of this drug. Quetiapine Fumarate cytochrome P450 family 3 subfamily A member 5 Homo sapiens