Exemestane

$69.90 – $4,200.00

Exemestane is a steroidal aromatase inactivator. Its structure is similar to androstenedione, the natural substrate of aromatase. It is a pseudo-substrate of aromatase.

Sku:

N/A

Tag:

Anti-Estrogen

Description

Product Information:

Name: Exemestane
CAS No.: 107868-30-4
Molecular Formula: C20H24O2
Molecular Weight: 296.4
Appearance:White Powder

What is Exemestane?
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women.
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body’s estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally via the actions of the aromatase enzyme in these peripheral tissues where it acts locally. Any circulating estrogen in post-menopausal women, as well as men, is the result of estrogen escaping local metabolism and entering the circulatory system.

Medical use
Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as “suicide inhibition.” By being structurally similar to enzyme targets, Exemestane permanently binds to the enzymes, preventing them from converting androgen into estrogen.

Exemestane is taken in tablet form once a day. Patients can experience side effects like nausea, anxiety, shortness of breath, abdominal pain, bone pain, and chest pain. Side effects vary widely between patients and patients should report the side effects they experience to their doctors, as some may be indicators of dangerous complications. Shortness of breath and chest pain in particular are causes for concern in patients taking exemestane.

Side effects
The most common side effects (more than 10% of patients) are hot flashes and sweating, which are typical estrogen deficiency caused by exemestane, as well as insomnia, headaches, and joint pain. Nausea and fatigue are mainly seen in patients with advanced breast cancer.

In approximately 20% of patients receiving Aromasin, an occasional decrease in lymphocytes has been observed, especially in patients with pre-existing lymphopenia.

Exemestane has androgenic properties similar to formestane and can produce androgenic side effects such as acne and weight gain, although these are usually related to the over-therapeutic dose of the drug.

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