Advanced breast cancer in women with natural or artificially induced postmenopausal status, who have previously been treated with antiestrogens.
藥理
Letrozole binds to the heme group of aromatase, a cytochrome P450 enzyme which catalyzes conversion of androgens to estrogens (specifically, androstenedione to estrone and testosterone to estradiol). This leads to inhibition of the enzyme and a significant reduction in plasma estrogen levels; approximately 30% of human breast cancers are sensitive to this estrogen deprivation.
藥動學
Letrozole is well absorbed, weakly protein binding, metabolized by CYP3A4 to a glucuronide metabolite, which is excreted in urine(90%), elimination half-life:2 days.
禁忌症
Hypersensitivity to letrozole or any component of the formulation, pre-menopausal women, pregnancy, lactation.