Letrozole

$75 $69
Letrozole is a new generation of highly selective aromatase inhibitor, a synthetic derivative of benzotriazole. It works by inhibiting aromatase, lowering estrogen levels, and is a very potent anti-es

Performance

anti-oestrogen：

★★★★★

Muscle Gain：

★★★★★

Reduce Fat/Water：

★★★★★

Side Effects：

★★★★★

Sustained Effects：

★★★★★

SKU：

2.5mg/tablet × 60 tablets/bottle

Package：

tablet

Appearance：

oral

Dosage：

2.5 mg/every other day

Cycle：

Throughout the cycle

Introduction:

Letrozole is a non-steroidal selective third-generation aromatase inhibitor. Its structure and activity are very similar to those of anastrozole and are used for similar medical purposes. Specifically, in the United States, the prescription guidelines recommend using letrozole for the treatment of postmenopausal women with estrogen receptor-positive or unknown estrogen receptor status breast cancer (where it is unclear if the cancer is responsive to estrogen). It is typically used as a second-line therapy after the failure of estrogen receptor antagonists like tamoxifen, and sometimes as a first-line treatment depending on the situation. Male bodybuilders and athletes have found that letrozole is effective in alleviating estrogenic side effects associated with synthetic metabolic/androgenic steroids, such as gynecomastia, fat accumulation, and increased water retention.

Letrozole is one of a series of new drugs targeting aromatase inhibitors. It is one of the most effective estrogen-reducing drugs developed to date and has a stronger effect than non-selective first-generation aromatase inhibitors such as testolactone and aminoglutethimide. Each letrozole tablet is dosed at 2.5 mg, which, according to product information, is sufficient to reduce estrogen levels by an average of 78% during clinical use. The drug is also generally quite effective at lower dosages. The product's literature states that in clinical studies, low dosages of 0.1 and 0.5 mg produced estrogen suppression of 75 and 78% respectively in many patients. The recommended dosage also causes the desired level of suppression in nearly all patients, thus many respond well to lower dosages.

History:

The U.S. Food and Drug Administration approved letrozole for prescription sales in 1997, marketed by Novartis under the brand name Femara. Novartis also widely markets this drug in other countries, and it is currently approved in over 70 countries. The Femara brand dominates globally, available in Argentina, Australia, Belgium, Brazil, Canada, Chile, Czech Republic, France, Germany, Greece, Hong Kong, India, Netherlands, New Zealand, Italy, South Africa, Switzerland, and Russia. Novartis also markets it under the Femar brand name in other countries including Finland, Denmark, Norway, and Sweden. Additionally, letrozole is also sold under other brand names such as Fempro (India), Oncolet (India), Trozet (India), Insegar (Spain), Aromek (Poland), Lametta (Poland), Cendalon (Argentina), Fecinole (Argentina), and Kebirzol (Argentina). Due to the high efficacy and strong market support of Femara and Femar, they remain the most popular letrozole products.

Available Forms:

Letrozole is most commonly supplied in 2.5mg tablets.

Structural Characteristics:

Letrozole is classified as a non-steroidal selective third-generation aromatase inhibitor. Its chemical name is 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile.

Side Effects:

Common side effects associated with aromatase inhibitors include hot flashes, joint pain, weakness, fatigue, mood changes, depression, high blood pressure, swelling of arms/legs, and headaches. Aromatase inhibitors also reduce bone mineral density, which may increase the risk of osteoporosis and fractures in susceptible individuals. Some individuals may also experience gastrointestinal side effects (including nausea and vomiting). Aromatase inhibitors can harm the development of an unborn fetus and should not be taken during pregnancy. When used long-term in steroid therapy, men can take it (off-label) to reduce estrogenicity, as aromatase inhibitors can increase the risk of cardiovascular diseases (CVD) by delaying the beneficial properties of estrogen on cholesterol values. Studies have shown that when aromatizable steroids like testosterone enanthate are used in conjunction with aromatase inhibitors, the suppression of HDL (good) cholesterol becomes more pronounced. Because the estrogen receptor agonist/antagonist tamoxifen generally does not have the anti-estrogenic (negative) effect on cholesterol values, it is often preferred by male bodybuilders and athletes concerned with cardiovascular health to maintain estrogen levels.

Usage Guidelines:

Letrozole is FDA approved for: 1) adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer; 2) extended adjuvant treatment of postmenopausal women with early breast cancer who have received 5 years of adjuvant tamoxifen therapy; 3) first-line treatment of postmenopausal women with hormone receptor-positive or unknown hormone receptor status locally advanced or metastatic breast cancer; 4) treatment of advanced breast cancer in postmenopausal women after anti-estrogen therapy has progressed. The recommended dose of letrozole is one 2.5 mg tablet once daily, regardless of meals. When used (off-label) to mitigate estrogenic side effects of synthetic metabolic/androgenic steroids or to increase muscle mass, male athletes and bodybuilders typically take 1.25 mg to 2.5 mg daily. In some cases, a dose of half a tablet (1.25 mg) every other day is also sufficient to prevent estrogenic side effects.


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