Steroid Hormones Medicine API Factory Price Manufacture Supply Exemestane CAS 107868-30-4 for Anti -tumor

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Exemestane CAS 107868-30-4

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Exemestane is an irreversible steroidal aromatase inhibitor for postmenopausal women with estrogen-progesterone receptor-positive advanced breast cancer. The structure is similar to its substrate natural androstenedione. Estrogen deprivation by inhibition of aromatase is an effective and optional approach for the treatment of hormone-dependent breast cancer in postmenopausal women, natural or artificial postmenopausal women whose disease has not progressed after tamoxifen therapy of advanced breast cancer.
Exemestane is a steroidal aromatase inactivator, its structure is similar to the natural substrate of aromatase androstenedione, and it is a pseudo-substrate of aromatase. Since estrogen in postmenopausal women is mainly produced by the conversion of androgen (produced by the adrenal cortex) under the action of aromatase in peripheral tissues, this product is irreversibly combined with the active site of aromatase to inactivate it, thus significantly Reduces circulating estrogen levels in postmenopausal women. This product has no obvious effect on the biosynthesis of adrenal cortex hormone, even if the concentration is 600 times higher than the concentration of inhibiting aromatase, it has no obvious effect on other enzymes in the corticosteroid production pathway. This product is rapidly absorbed orally, and the absorption is affected by food. The oral bioavailability is 42%. Postmenopausal women have a higher absorption rate of the drug than healthy subjects. Patients reach the peak plasma concentration 2 to 4 hours after oral administration of this product, and the peak time is 1.2 hours on average, which is shorter than healthy subjects (2.9 hours). It is mainly bound to α1-acid glycoprotein and protein, and the total protein binding rate is 90%. Mainly metabolized by the liver, the metabolite is inactive 17-hydroexemestane, and the elimination half-life is 24 hours. It is mainly excreted through urine or feces, each accounting for 42% of the dose.
A second-generation aromatase inhibitor for the treatment of metastatic breast cancer and as an adjuvant therapy for early breast cancer.
It is an irreversible steroidal aromatase inactivator, which can inhibit the synthesis of estrogen and reduce the level of estrogen in blood circulation. It is suitable for postmenopausal patients with advanced breast cancer whose disease has progressed after treatment with tamoxifen.