INVESTIGATIONS ON IN VITRO METABOLITES OF LINEZOLIDIN VARIOUS SPECIES

摘要

Linezolid is a potent synthetic oxazolidinone used for the treatment of bacterial infections with a new mechanism of action that involves early inhibition of bacterial protein synthesis. In humans, linezolid circulates mainly as parent drug and is excreted primarily as parent drug and a major inactive, morpholine ring-opened carboxylic acid metabolite. In vitro studies were conducted to identify the hepatic enzymes responsible for the oxidative metabolism of linezolid using human liver microsomes. However the specific enzyme responsible for the oxidation of linezolid was not identified. The present study is to check with and identify the probable metabolic pathways in various species like monkey, mouse, rat, dog and human liver microsomes and put up the best model for the contingency studies using modern analytical techniques. The current investigation on the metabolites obtained after 60 minutes incubation revealed three additional metabolites, namely, M10, M11 and M12, adding on to the list of already reported metabolites.