What question did this study set out to answer?

The study aims to evaluate how CYP2D6 inhibition affects the pharmacokinetics of venlafaxine and its metabolite O-desmethylvenlafaxine.

Enantioselective Pharmacokinetics of Venlafaxine in the Presence of CYP2D6 Inhibition: A Population Parent–Metabolite Modeling Approach

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Quantifies venlafaxine pharmacokinetics in the presence of CYP2D6 inhibition, suggesting dosing alignment with intermediate metabolizers.

The study aims to evaluate how CYP2D6 inhibition affects the pharmacokinetics of venlafaxine and its metabolite O-desmethylvenlafaxine.
Conducted a two-phase crossover study with 24 subjects receiving 150 mg racemic venlafaxine.
Administered a strong CYP2D6 inhibitor (paroxetine) daily for 10 days and co-administered with venlafaxine on the last day.
Developed enantiomer-specific parent-metabolite models using nonlinear mixed-effect modeling.
CYP2D6 inhibition significantly reduced the conversion from parent venlafaxine to its metabolite O-desmethylvenlafaxine.
The effect was 2.5 times greater on (R)-venlafaxine compared to (S)-venlafaxine.
Potency-adjusted exposure for norepinephrine and serotonin transporters decreased by approximately 8% under CYP2D6 inhibition.

Alves et al. (2026) studied this question.

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