Letrozole (Femara) CAS 112809-51-5

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Letrozole (Femara) Description

Letrozole (trade name: Femara) is an orally active nonsteroidal aromatase inhibitor. As a competitive inhibitor of the aromatase, Letrozole (Femara) inhibits the conversion of androgens to estrogen (estrogen stimulates breast tissues and breast cancer reoccurrence) and gonadal steroidogenesis. Letrozole (Femara) can be used for the treatment of breast cancer that is hormonally-responsive or has an unknown receptor status in postmenopausal women. Besides this, Letrozole (Femara) also has some off-label use such as ovarian stimulation, pretreatment of termination of pregnancy, treatment of gynecomastia, treatment of endometriosis, and promoting spermatogenesis for male patients of nonobstructive azoospermia.

Letrozole (Femara) Usage

Letrozole (Femara) is part of a new generation of highly selective aromatase inhibitors and is an artificially synthesized benzotriazole derivative. Letrozole (Femara) inhibits aromatase to lower estrogen levels, thus preventing estrogen from stimulating tumor growth. Its in vivo activity is 150-250 times stronger than that of first generation aromatase inhibitor Amarante. As Letrozole (Femara) is highly selective, it will not impact glucocorticoid, mineralocorticoid and thyroid functions; even at high dosages, Letrozole (Femara) will not have any inhibiting effects on adrenal corticosteroid secretion, giving it a high treatment index. Letrozole (Femara) has no latent toxicity towards any bodily systems and target organs, has no mutagenicity and carcinogenic effects, has minimal toxic side effects, is well-tolerated, and has stronger anticancer effects than other aromatase inhibitors and antiestrogen drugs. Letrozole (Femara) is suitable for advanced breast cancer postmenopausal patients who have not responded to estrogen-suppressing treatment and for early breast cancer treatment. Letrozole (Femara) is used to treat postmenopausal patients with advanced breast cancer and serves as a second-line treatment to follow unsuccessful antiestrogen treatment. Compared to the current standard Tamoxifen treatment, Letrozole (Femara) can better prevent the risk of breast cancer recurrence.