Drug intelligence / Profile preview

n-desmethylatomoxetine

Development stage
Unknown
Modality
Small Molecules
01

Overview

N-desmethylatomoxetine is a minor metabolite of atomoxetine, a selective norepinephrine reuptake inhibitor (NRI) primarily used for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD). It is formed from atomoxetine mainly by the cytochrome P450 2C19 (CYP2C19) enzyme and other cytochrome P450 enzymes. While it shares the same mechanism of action as atomoxetine, inhibiting the presynaptic norepinephrine transporter, its pharmacological activity is substantially lower, approximately 20-fold less potent than atomoxetine. N-desmethylatomoxetine circulates in plasma at lower concentrations than atomoxetine, particularly in individuals who are extensive metabolizers of CYP2D6. Its half-life varies depending on CYP2D6 metabolizer status, being longer in poor metabolizers. It is highly bound to plasma proteins. N-desmethylatomoxetine is not developed as a standalone therapeutic agent but is studied in the context of atomoxetine's pharmacokinetics and pharmacodynamics.

Other names
Desmethyl Atomoxetine
02

Targets

NET (Norepinephrine Transporter)

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