Abstract
Almotriptan is a selective serotonin receptor agonist used for the treatment of migraine headache. Its in vitro metabolic pathway in human liver subcellular fractions and in vivo metabolic pathway in rats, dogs, monkeys, and humans are shown. In humans, almotriptan was converted to the carbinolamine metabolite 2 via hydroxylation of the pyrrolidine group. This reaction was mainly catalyzed by CYP3A4 and 2D6. Metabolite 2 was further oxidized by aldehyde dehydrogenase to the open ring γ‐aminobutyric acid derivative 3 . N‐Demethylation at the dimethylamino group to form 4 was carried out by five different CYPs. FMO‐3 mediated N‐oxidation to form metabolite 5 , and MAO‐A catalyzed oxidative deamination to form indole acetic acid 6 and indole ethyl alcohol 7 . Metabolite 6 further formed a glucuronide conjugate.
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