Letrozole / Femara inhibitors treat breast cancer

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Product Name:Letrozole/ Femara

Synonyms:4,4'-(1H-1,2,4-triazol-1-ylmethylene) bis-benzonitrile;femara;CGS-20267

CAS:

MF:C17H11N5

MW:285.3

Chemical Properties:white to light yellow crystal

MP:181-183°C

Storage Temp. :-20°C Freezer

Usage:Pyrrole type aromatization enzyme inhibitors. Used in the treatment of breast cancer.

Pharmacological Function:Letrozole is a new generation of selective aromatase inhibitors. It is a synthetic benzyl triazole derivative, can inhibit aromatase and decrease estrogen levels, further eliminates the stimulation of estrogen on tumor growth. The activity of letrozole in the body is 150-250 times more than that of the first generation of aromatase inhibitors - aminoglutethimide. Due to its high selectivity, and shall not affect the sugar cortical hormone, mineralocorticoid and thyroid functions, large dosage is of no inhibition for adrenal corticosteroid secretions, therefore, it has a higher therapeutic index. Preclinical studies have shown that Letrozole is of no potential toxicity to each system and target organ in the body, no mutagenic and carcinogenic effect, little side reaction, well tolerated, and compared with other aromatase inhibitors and anti-estrogen drugs, it has a stronger antitumor effect. Applicable to the treatment of advanced breast cancer in postmenopausal patients who anti-estrogen ineffective, and early breast cancer.

In December 2005, the British drug and health care products regulatory approved letrozole (furlong) produced by Swiss Novartis used to treat breast cancer patients, and allowed it to treat early invasive breast cancer patients after the surgery caused by positive postmenopausal hormone. This is the second aromatase inhibitors approved by UK after Astrazeneca's Arimidex June in 2005. Two drugs in clinical trials have shown that compared with the current standard Tamoxifen treatment, it can better prevent the risk of breast cancer recurrence.

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