Description of Exemestane:
- Molecular formula – C20H24O2
- Suitable temperature for storage – 2-8 Celsius
- Molecular weight – 296.4
Other names:Â
-
- 6-methylideneandrosta-1,4-diene-3,17-dione
- Aromasin
- 107868-30-4
- NY22HMQ4BX
- Aromasine
- PNU-155971
Discovery of Exemestane:
Exemestane / Aromasin belongs to the category of drugs known as an irreversible aromatase inhibitor. Exemestane was initially approved and discovered in the year 1987. At first, Exemestane had indications for the treatment of breast cancer patients and those patients who weren’t responding well to the anti-estrogenic therapies. Recently, Exemestane has sown different potential advantages for other indications due to the feasibility of its oral administration and potency.
Mechanism of action:
Cancer cells and their growth can be dependent on the concentrations of estrogen hormone. Exemestane (Aromasin) is the main enzyme that tends to help convert androgens to estrogens in both pre and post-menopausal women.
In women in their pre-menopausal phase, the main source of energy is estradiol or estrogen. However, in the case of post-menopausal women, circulating estrogen has the main source from the adrenal or ovarian androgen conversion to the estrogen through the help of these enzymes.
Aromatase inhibition can be both effective and selective intervention for estrogen deprivation in postmenopausal women with hormone-dependent cancer of the breast.
Exemestane is irreversible, structurally related to natural androstenedione (substrate), and a steroidal aromatase inhibitor. Exemestane tends to bind (irreversibly) to the active sites in the body to cause inhibition (permanent) to restore the enzymatic function.
Clinical application:
Anti-inflammatory properties:
Exemestane is a strong enzyme against oxidation activity, UV radiations, and hypoxia. All of these properties have similarities with sulforaphane activity or action in the body. After the first single 25mg dosage of Exemestane, it can cause suppression of circulating estrogen levels after 2-3 days of administration.
The property of Exemestane being an antineoplastic drug, makes it a beneficial drug to treat breast cancer in postmenopausal women. Exemestane therapy is mostly for patients who have had cancer progression even after initial treatment with tamoxifen for 2-3 years.
According to the American Society of Clinical Oncology guidelines, Exemestane is the suitable alternative for tamoxifen/raloxifene to prevent invasive breast cancer in postmenopausal women at higher risk.
Lung cancer treatment:
Aromatase enzyme complex or Exemestane catalyzes estrogen synthesis (final step). Exemestane also aids in decreasing cancer cell proliferation and apoptosis enhancement in cell lines. In the case of a lungs tumor, Exemestane can reduce estrogen biosynthesis for inhibiting
Breast cancer treatment:
Estrogen-dependent pathways belong to the 3rd Gen aromatase inhibitor steroidal drug for breast cancer intervention. In different metastatic diseases, AI or Exemestane works as 1st and 2nd line treatment for advanced-stage estrogen-receptor-positive cancer among post-menopausal women.
Disclaimer
The data provided in this article about Exemestane / Aromasin has been written to provide knowledge for research advancement. It mainly aims to provide the best information to the emerging researchers who plan to study the benefits and effects of Exemestane. The article is specifically designed to provide information about Exemestane rather than giving instructions about the use of Exemestane. Furthermore, there has been no mention of the route of administration or dosage of Exemestane. The information provided in the article has been collected from different published researchers by a group of expert researchers keeping the medical protocols in view.
Furthermore, this article does not contain any information that will encourage the readers to consume or advertise Exemestane. We do not condone any advertisement of any supplement or drug that the FDA has not approved. Melanotan Express insists that no product should be ingested under any circumstances.
References:
- Bliss, J. M., Kilburn, L. S., Coleman, R. E., Forbes, J. F., Coates, A. S., Jones, S. E., … & Coombes, R. C. (2012). Disease-related outcomes with long-term follow-up: an updated analysis of the intergroup exemestane study. J Clin Oncol, 30(7), 709-717.
- Sobral, A. F., Amaral, C., Correia-da-Silva, G., & Teixeira, N. (2016). Unravelling exemestane: From biology to clinical prospects. The Journal of steroid biochemistry and molecular biology, 163, 1-11.
- Van Asten, K., Neven, P., Lintermans, A., Wildiers, H., & Paridaens, R. (2014). Aromatase inhibitors in the breast cancer clinic: focus on exemestane. Endocrine-related cancer, 21(1), R31-49.
- Scott, L. J., & Wiseman, L. R. (1999). Exemestane. Drugs, 58(4), 675-680.
- Mauras, Nelly, et al. “Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males.” The Journal of Clinical Endocrinology & Metabolism 88.12 (2003): 5951-5956.
- Dank, Magdolna. “The role of aromasin in the hormonal therapy of breast cancer.” Pathology Oncology Research 8.2 (2002): 87-92.
- Liu, Hua, and Paul Talalay. “Relevance of anti-inflammatory and antioxidant activities of exemestane and synergism with sulforaphane for disease prevention.” Proceedings of the National Academy of Sciences 110.47 (2013): 19065-19070.
Where to Buy Aromasin / Exemestane?
Melanotan Express offers Exemestane / Aromasin for Sale with at least 99% purity. If you are looking to purchase Exemestane 25 mg for research purposes, visit Melanotan Express, one of the leading suppliers of the USA Peptides and SARMs for sale:
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