Exemestane

Exemestane, commonly known by its brand name Aromasin, is a medication classified as an aromatase inhibitor (AI).

Some breast cancers require estrogen to grow. Those cancers have estrogen receptors (ERs), and are called ER-positive. They may also be called estrogen-responsive, hormonally-responsive, or hormone-receptor-positive. Aromatase is an enzyme that synthesizes estrogen. Aromatase inhibitors block the synthesis of estrogen. This lowers the estrogen level, and slows the growth of cancers.

 

 

 

Exemestane is indicated for the adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received two to three years of tamoxifen and are switched to it for completion of a total of five consecutive years of adjuvant hormonal therapy. US FDA approval was in October 1999.

Exemestane is also indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.

For premenopausal women with hormone-receptor–positive breast cancer, adjuvant treatment with ovarian suppression plus the aromatase inhibitor exemestane, as compared with ovarian suppression plus tamoxifen, provides a new treatment option that reduces the risk of recurrence. The TEXT and SOFT trials demonstrated improved disease free survival in patients treated with exemestane and ovarian suppression compared to the tamoxifen and ovarian suppression group. Premenopausal women who receive ovarian suppression may now benefit from an aromatase inhibitor, a class of drugs that until now has been recommended only for postmenopausal women.

Exemestane belongs to a class of drugs called aromatase inhibitors. It works by inhibiting the enzyme aromatase, which is responsible for converting androgens (such as testosterone) into estrogen. By reducing estrogen levels in the body, exemestane helps slow down or halt the growth of estrogen receptor-positive breast cancer cells.

Exemestane significantly reduces estrogen levels in postmenopausal women by blocking the aromatase enzyme. By doing so, it helps to deprive estrogen-dependent breast cancer cells of the hormone they need to grow and proliferate.

Hormone Replacement Therapy (HRT): Exemestane is not intended for use as a hormone replacement therapy in postmenopausal women. It is specifically used in the context of breast cancer treatment and not as a general approach to managing menopausal symptoms.

 

 

Exemestane is metabolized by the liver enzyme CYP3A4. While the CYP3A4 inhibitor ketoconazole had no significant effect on exemestane levels in a clinical trial, the strong CYP3A4 inductor rifampicin significantly cut exemenstane levels about in half (AUC −54%, Cmax −41% for a single dose), potentially compromising its effectiveness. Other 3A4 inductors such as carbamazepine and St John's Wort are expected to have similar effects. The clinical relevance of this effect has not been investigated.

Estrogens probably reduce exemestane effectiveness: It would usually be counter-productive to reduce the body's estrogen synthesis with exemestane and then substitute estrogen with pharmaceuticals.

 

 

Exemestane is quickly absorbed from the gut, but undergoes a strong first-pass effect in the liver. Highest blood plasma concentrations are reached after 1.2 hours in breast cancer patients and after 2.9 hours in healthy subjects. Maximal aromatase inhibition occurs after two to three days. 90% of the absorbed substance are bound to plasma proteins. The liver enzyme CYP3A4 oxidizes the methylidene group in position 6, and the 17-keto group (on the five-membered ring) is reduced by aldo-keto reductases to an alcohol. Of the resulting metabolites, 40% are excreted via the urine and 40% via the feces within a week. The original substance accounts for only 1% of excretion in the urine. The terminal half-life is 24 hours.

 

 

Product Name	Aromasin
Other Name	FCE-24304
CAS	107868-30-4
Molar mass	296.410
MF	C20H24O2
Purity	Above 98%
Apprarance	White Cyrstalline Powder

 

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Exemestane, also known by its brand name Aromasin, is not a chemotherapy drug. It is classified as an aromatase inhibitor (AI) and is used in the treatment of hormone receptor-positive breast cancer in postmenopausal women.

Chemotherapy refers to a broad category of drugs that are designed to kill rapidly dividing cells, including cancer cells. Chemotherapy drugs work by targeting and destroying cancer cells throughout the body. They are often used in systemic treatment regimens to eliminate cancer cells that may have spread beyond the primary tumor site.

Exemestane, on the other hand, is an endocrine therapy drug specifically designed to target the hormone receptor-positive breast cancer cells. It works by blocking the enzyme aromatase, which is responsible for converting androgens (such as testosterone) into estrogen. By reducing estrogen levels in the body, exemestane helps to slow down or halt the growth of estrogen-dependent breast cancer cells.

Endocrine therapy drugs like exemestane are typically used in combination with other treatments, such as surgery, radiation therapy, or chemotherapy, depending on the individual's specific cancer situation. They are often used as adjuvant therapy to reduce the risk of cancer recurrence or as a treatment for advanced breast cancer.

 

 

Tamoxifen and exemestane are both medications used in the treatment of hormone receptor-positive breast cancer in postmenopausal women, but they have different mechanisms of action and are classified as different types of drugs. Here are the main differences between tamoxifen and exemestane:

1) Mechanism of Action:

Tamoxifen: Tamoxifen is a selective estrogen receptor modulator (SERM). It works by binding to estrogen receptors in breast tissue, blocking the effects of estrogen and inhibiting the growth of estrogen receptor-positive breast cancer cells.

Exemestane: Exemestane is an aromatase inhibitor (AI). It works by inhibiting the enzyme aromatase, which is responsible for converting androgens (such as testosterone) into estrogen. By reducing estrogen levels in the body, exemestane helps to deprive estrogen-dependent breast cancer cells of the hormone they need to grow and proliferate.

2) Menopausal Status:

Tamoxifen: Tamoxifen can be used in both premenopausal and postmenopausal women.

Exemestane: Exemestane is specifically used in postmenopausal women. It is not effective in women who still have functioning ovaries and are producing estrogen.

3) Treatment Stage:

Tamoxifen: Tamoxifen is commonly used as adjuvant therapy after surgery for early-stage hormone receptor-positive breast cancer. It can also be used for the treatment of advanced breast cancer.

Exemestane: Exemestane is often used as adjuvant therapy after initial treatment with tamoxifen or another SERM. It is used specifically in postmenopausal women with hormone receptor-positive early-stage breast cancer or as a treatment for advanced breast cancer after progression on tamoxifen.

4) Side Effects:

Tamoxifen: Common side effects of tamoxifen may include hot flashes, mood swings, vaginal dryness, irregular menstrual periods, and an increased risk of blood clots and endometrial cancer.

Exemestane: Common side effects of exemestane may include hot flashes, fatigue, joint pain, headache, increased sweating, and insomnia. Long-term use may also lead to bone loss or osteoporosis.

It is important to note that the choice between tamoxifen and exemestane, or other treatments, depends on various factors, including the individual's menopausal status, tumor characteristics, and overall treatment plan.

 

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