PharmGKB efavirenz pharmacokinetic pathway published in Pharmacogenetics and Genomics

The PharmGKB summary describing the efavirenz (EFV) pharmacokinetic pathway, and the pharmacogenetic variants that affect EFV pharmacokinetics has been published by Pharmacogenetics & Genomics. Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor that is used as part of a highly active anti-retroviral therapy (ART) regimen (HAART) against HIV-1 infection. The primary route of EFV metabolism is through CYP2B6 to 8-hydroxyefavirenz (8-hydroxy-EFV).  In vitro studies using human liver microsomes show that there is considerable variability in the formation rate of 8-hydroxy-EFV between samples and genetic variants in CYP2B6 are likely major contributors to this variability. There is also evidence that CYP3A4, CYP3A5, CYP1A2 and CYP2A6 also play minor roles in this xenometabolic step. View the interactive online version of the PharmGKB summary: Efavirenz pathway, pharmacokinetics (PK) here and on Pubmed.View all pathways on PharmGKB.