In vitro metabolism of 14C-moxidectin by hepatic microsomes from various species.

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Dupuy J, Escudero E, Eeckhoutte C, Sutra JF, Galtier P, Alvinerie M

In vitro metabolism of 14C-moxidectin by hepatic microsomes from various species.

Vet Res Commun. 2001 Jul;25(5):345-54. doi: 10.1023/a:1010686508307.

PubMed ID

11469506 [ View in PubMed

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Abstract

Moxidectin is an antiparasitic drug widely used in cattle, sheep and companion animals. No data were available on its metabolism in wild species or in monogastrics. The in vitro metabolism of 14C-moxidectin was studied using hepatic microsomes from several different species: cow (Bos taurus). sheep (Ovis ovis), goat (Capra hircus), deer (Cervus dama), rat (Rattus norvegicus), pig (Sus scrofa and rabbit (Oryctolagus cuniculus). After separation and quantification by HPLC, the extent of metabolism of 14C-moxidectin was greatest with microsomes from sheep (32.7%) as compared to those from cows (20.6%), deer (15.4%), goats (12.7%). rabbits (7.0%) or rats (3.0%). The least metabolism occurred with microsomes from pigs. with 0.8% of total detected metabolites. A C29 monohydroxymethyl metabolite was detected in the greatest amounts. providing 0.4% out of the total detected radioactivity in pigs and 19.3% in sheep. In addition, the importance of P450 3A in the metabolism of 14C-moxidectin was confirmed by using in vivo induced P450 in combination with various P450 inhibitors.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Moxidectin	CYP2B protein	Protein	Humans	No	Substrate	Details