Description: Exemestane is an irreversible, selective aromatase inhibitor which acts as a false substrate for the enzyme and forms an intermediate that binds to its active site. This leads to inactivation or suicide inhibition, thus preventing the conversion of androgens to oestrogens in peripheral tissues. It lowers circulating oestrogens in postmenopausal women w/ breast cancers where growth is oestrogen-dependent. Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 1.2 hr. Distribution: Extensively distributed into tissues; crosses the placenta. Plasma protein binding: 90%, primarily to albumin and α1-acid glycoprotein. Metabolism: Metabolised via oxidation by CYP3A4 enzyme and via reduction by aldoketoreductase into inactive metabolites. Excretion: Via urine (>1% as unchanged drug; 39-45% as metabolites); faeces (36-48%). Elimination half-life: Approx 24 hr.
L02BG06 - exemestane ; Belongs to the class of enzyme inhibitors. Used in treatment of neoplastic diseases.
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