Effect of CYP2D6 and CYP2C19 genotypes on atomoxetine serum levels -- a
study based on therapeutic drug monitoring data
Abstract
Atomoxetine is mainly metabolized by CYP2D6 while CYP2C19 plays a
secondary role. It is known that patients carrying genotypes encoding
decreased/absent CYP2D6 metabolism obtain higher atomoxetine
concentrations and are at increased risk of adverse effects. Here, we
aimed to investigate the added effects of reduced-function CYP2C19
genotype on atomoxetine concentrations in real-world settings. Serum
atomoxetine concentrations and CYP2D6/2C19 genotypes were included from
a therapeutic drug monitoring service. Patients were first subgrouped
according to CYP2D6 encoding normal, reduced or absent CYP2D6
metabolism, referred to as normal (NM), intermediate (IM) or poor
metabolizers (PM). Then, the effect of reduced-function CYP2C19
genotypes was investigated. Genotyping of the CYP2D6 nonfuctional or
reduced variant alleles comprised CYP2D6*3-*5, *9-*10 and *41. For
CYP2C19, the CYP2C19*2 was analysed to define metabolizer phenotype.
Dose-adjusted serum atomoxetine concentration was the exposure measure.
Using a patient cohort (n=315), it was found that CYP2D6 IM and PM
patients had 1.9-fold (95%CI: 1.4-2.7) and 9.6-fold (5.9-16) higher
exposure of atomoxetine compared with CYP2D6 NMs. CYP2C19*2 carriers had
1.5-fold (1.1-2.2) higher atomoxetine exposure than non-carriers
regardless of CYP2D6 genotype. CYP2D6 genotype has a great impact on
atomoxetine exposure, where our real-world data suggest atomoxetine dose
requirements to be around half and one-tenth in CYP2D6 IM and PM vs. NM
patients, respectively. When adding CYP2C19 genotype as a factor of
relevance for personalized atomoxetine dosing, CYP2C19*2 carriers should
further reduce the dose by a third. These findings suggest that
pre-emptive CYP2D6/CYP2C19 genotyping should be performed to
individualize atomoxetine dosing and prevent adverse effects.