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Biochem Pharmacol. 1994 Mar 29;47(7):1253-7.

Characterization of the enzyme responsible for the metabolism of sumatriptan in human liver.

Author information

1
Department of Drug Metabolism III, Glaxo Group Research Ltd, Ware, Herts, U.K.

Abstract

Studies have been undertaken to investigate the enzymes responsible for the metabolism of [14C]sumatriptan in man. Oxidative deamination of sumatriptan to form the indole acetic acid derivative is the only phase 1 pathway evident in man and both cytochrome P450 (P450) and monoamine oxidase (MAO) are capable of catalysing this type of reaction. The metabolism of [14C]sumatriptan was therefore investigated in vitro in a preparation derived from human liver, which was shown, by the use of the probe substrates [14C]testosterone (P450), [3H]5HT (MAO-A) and [14C]benzylamine (MAO-B) to be a rich source of both enzyme systems. Incubation with clorgyline and deprenyl, probe inhibitors of MAO-A and MAO-B, respectively, showed that [14C]sumatriptan was metabolized by MAO-A; there was no evidence of P450 involvement in its metabolism. The data in this study therefore indicate that the enzyme MAO-A is the major enzyme responsible for the metabolism of sumatriptan in human liver.

PMID:
8161354
DOI:
10.1016/0006-2952(94)90397-2
[Indexed for MEDLINE]

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