Wednesday, September 21, 2016

Ivacaftor pathway, pharmacokinetics/pharmacodynamics published in Pharmacogenetics and Genomics

The PharmGKB summary of the pharmacokinetics and pharmacodynamics of ivacaftor has been published in Pharmacogenetics and Genomics. Ivacaftor is approved for use in patients who carry particular variants in the CFTR gene. By repotentiating the CFTR ion channel, ivacaftor targets the underlying cause of some forms of cystic fibrosis. Ivacaftor is metabolized by CYP3A4 and CYP3A5 and inhibits ABCB1. Its metabolites are excreted through the transporter SLCO1B1. 

A stylized illustration of the PK/PD pathways of ivacaftor accompanies the publication, and can also be viewed on the PharmGKB website. The illustration and text also includes lumacaftor, a drug that is sometimes used in conjunction with ivacaftor to treat patients with CFTR variants that result in localization defects. The full text and pathway image can be found on the pharmgkb website at

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