フォルメスタンは最初の選択的でした, タイプI, 閉経後の女性のエストロゲン受容体陽性乳がんの治療に使用されるステロイド性アロマターゼ阻害剤. フォルメスタンはアナボリックステロイドまたはプロホルモンからのエストロゲン生成を抑制します. フォルメスタンは 4-ヒドロキシテストステロンのプロホルモンでもあります, 弱いアンドロゲン活性と穏やかなアロマターゼ阻害活性を持つ活性ステロイド. 世界反ドーピング機関によりアスリートへの使用が禁止されている物質としてリストされています。.
フォルメスタンは経口バイオアベイラビリティが低い, したがって、隔週で投与する必要があります (隔週) by intramuscular injection. Some clinical data has suggested that the clinically recommended dose of 250mg was too low. With the discovery of newer, non-steroidal and steroidal, aromatase inhibitors which were orally active and less expensive than formestane, formestane lost popularity.
Lentaron is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Breast cancer may be estrogen sensitive or insensitive. A majority of breast cancers are estrogen sensitive. Estrogen sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone sensitive breast cancers. Lentaron has been targeted specifically for the treatment of postmenopausal women. Unlike premenopausal women who produce most estrogen in the ovaries, postmenopausal women produce most estrogen in peripheral tissues with the help of the aromatase enzyme. Lentaron s, an aromatase inhibitor, can thus help to decrease the local production of estrogen by blocking the aromatase enzyme in peripheral tissues (ie. Adispose tissue of the breast) to treat hormone sensitive breast cancer.
