Novartis Pharmaceuticals

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2,5MG/TAB * 30TAB

Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system which 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 (estrone, estradiol and estrone sulfate) levels. Does not affect synthesis of adrenal or thyroid hormones, aldosterone, or androgens.

Rapid and well absorbed; not affected by food.

Hepatic via CYP3A4 and 2A6 to an inactive carbinol metabolite.

Time to Peak
Steady state, plasma: 2 to 6 weeks; steady state serum concentrations are 1.5 to 2 times higher than single-dose values.

Half-Life Elimination
Terminal: ~2 days.

Detection Time
~14 days.

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