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Anti-Estrogen Powders

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Formestane (Lentaron) Powder (566-48-3)


Product Name: Formestanes
Synonyms: 4-hydroxy-androst-4-ene-17-dione;4-hydroxy-delta(sub4)-androstenedione;4-HYDROXYANDROST-4-ENE-3,17-DIONE;4-HYDROXYANDROSTENEDIONE;4-HYDROXY-4-ANDROSTENE-3,17-DIONE;4-ANDROSTEN-4-OL-3,17-DIONE;4-OHA;CGP-32349
CAS: 566-48-3
MF: C19H26O3
MW: 302.41
Chemical Properties Needles
Usage An antitumor drug. An aromatase inhibitor
Usage antineoplastic, aromatase inhibitor


Formestane Description:


Formestane Is the second generation of irreversible steroid aromatase inhibitors. It inhibits the aromatase responsible for converting androgen into estrogen, thereby preventing estrogen production. Breast cancer may be estrogen-sensitive or insensitive. Most breast cancers are estrogen-sensitive. Estrogen-sensitive breast cancer cells are dependent on estrogenic activity. Therefore, removal of estrogen from the body can become an effective treatment for hormone-sensitive breast cancer.

Formestane is dedicated to the treatment of postmenopausal women. Unlike premenopausal women who produce the most estrogen in the ovaries, postmenopausal women produce most estrogens in peripheral tissues with the help of aromatases. Methanesulfonamide aromatase inhibitors can help reduce the production of estrogen by blocking aromatase (ie, attached to mammary gland tissue) in peripheral tissues to treat hormone-sensitive breast cancer.

Formestane is Also known as lentaron, is an anti-cancer drug, mainly used for the treatment of advanced breast cancer in postmenopausal women, also effective for prostate cancer.

Methanesulfonic acid is a androstenedione derivative, an aromatic enzyme inhibitor with amino hydroxyethyl amide, is a hormone antineoplastic agent. Under physiological conditions, it may competitively inhibit the synthesis of enzymes, resulting in reduced estrogen biosynthesis in the tissue, and then it works in cancer. When tumor tissue growth depends on the presence of estrogen, it is necessary to eliminate tumor estrogen-mediated growth stimuli in order to inhibit tumor growth.

The product is more selective than amino isoflavones, and its activity is amino-hydroxyethylamine 100 to 1000 times, does not inhibit the synthesis of adrenal hormones, without the need to add cortisone and so on. The in vitro inhibition of the product’s aromatase is 60 times stronger than that of aminosuccinimide.

When it is used alone, when it is combined with goserelin (gonadotropin-releasing hormone agonist), the drug does not significantly reduce premenopausal estrogen levels in women’s blood, and estrogen inhibition in premenopausal women The effect is greater than that of goserelin alone using methanesulfonic acid with other aromatase inhibitors without cross resistance, which does not have side effects of aminoglucan.

After oral administration, it is rapidly absorbed by the gastrointestinal tract, the plasma concentration of the peak time of 1 ~ 1.5 hours, but the individual peak concentration difference; intramuscular injection, can be accumulated in the injection site and slowly absorbed. It performs a biphasic elimination process, the initial elimination half-life of 2 to 4 days, the terminal elimination half-life of 5 to 10 days. After oral administration mainly in the liver metabolism, uridine excretion of glycoside metabolites in the form of existence.


Formestane Application :


Treatment of Breast Cancer:


Because of its potent estrogen-suppressing action, formestanes has been used clinically to treat breast cancer patients in a number of countries including England, Germany, Switzerland, Spain, Australia, New Zealand, Italy, and Malaysia. It has been shown to be an effective option as a second line of defense after , an estrogen receptor antagonist, has failed to elicit a positive response with patients, and produces an overall response statistically similar to when administered as the first-line therapy. In terms of overall potency, formestanes is not as strong as the selective third generation inhibitors like Arimidex or Femara .


Use for Bodybuilding:


Formestane can lower SHBG up to 34%, which will increase free levels. SHBG (sex hormone binding globulin) is a protein that binds to sex steroids, and renders them inactive, for as long as SHBG is bound to them. There is a difference between ‘free’ , and ‘bound’ . Free testosterone is what matters, so lowering SHBG will increase ‘free’ testosterone. Higher means more strength, muscle mass, less body fat, better sense of well being, and libido.

Formestane Dosages :


The most common version of formestane sold was in a topical gel form and it was dosed at 100-200mgs per application. Users would apply it onto clean, dry skin and rub in thoroughly; usually on the thighs or upper arms. It took 1 to 5 minutes to dry.

The injectable version for both breast cancer purposes and bodybuilders is 125mgs twice per week or 250mgs once per week.


Formestane COA :


Description White or Almost White Crystalline Powder white powder
Identification A.B. Positive
Assay 97.0~103.0% 99.3%
Specific Rotation +101°~+105° +102.6°
Loss On Drying 1.0%max 0.27%
Melting Point 153~157°C 153.0~155.0°C
Organic Volatile Impurities meets the requirement. Conforms
Related Substances meets the requirement. Conforms
Residual Solvents meets the requirement. Conforms
Particle Size 100% ≤ 20 microns Conforms
Conclusion The specification conform with USP35 standard
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