Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
藥理
Exemestane is an irreversible, steroidal aromatase inactivator. It prevents conversion of androgens to estrogens by tying up the enzyme aromatase. In breast cancers where growth is estrogen-dependent, this medicine will lower circulating estrogens.
藥動學
Bioavailability is 42%; following a high-fat breakfast, exemestane plasma levels increased by about 40%, extensively metabolized by CYP3A4 , protein binding: 90%, elimination half-life: 24 hours, excretion:urine (42% as metabolites), feces (42%).
禁忌症
Hypersensitivity to exemestane or any component of the formulation, premenopausal women, pregnancy, lactation.