Exemestane Review | Buy Aromasin Liquid
03December 3, 2019
Exemestane is a type of aromatase inhibitor, a class of compounds used in the study of breast cancer in postmenopausal models. It functions by blocking the production of estrogen, which can help slow or stop the growth of hormone receptor-positive breast cancer cells in research settings. By inhibiting the aromatase enzyme, Exemestane effectively reduces estrogen levels, making it a crucial component in the exploration of hormone receptor-positive breast cancer in postmenopausal models and a key part of aromatase inhibitor treatment.
What is Exemestane?
Exemestane is a medication specifically used in the treatment of breast cancer in postmenopausal women. As a member of the aromatase inhibitors class, Exemestane works by blocking the production of estrogen in the body. Estrogen can promote the growth of certain types of breast cancer cells, and by reducing estrogen levels, Exemestane helps to slow or halt the growth of these cells. This makes it a crucial tool in managing breast cancer in postmenopausal women, offering a targeted approach to hormone receptor-positive breast cancer.
Exemestane Review | Buy Aromasin Liquid
Research suggests that estrogen hormones are implicated in the occurrence and development of breast cancer in experimental subjects. With this in mind, endocrine manipulation has been explored in various studies for its potential applications. Initial research was undertaken to observe the regression of local cancers following ovary removal in subjects who were premenopausal.
Ovaries are the main source of estrogen in these subjects. However, post-menopause, the main source of circulating estrogen is the result of the aromatization of androstenedione and testosterone. This reaction is facilitated by aromatase, a member of the cytochrome P-450 (CYP) family. Aromatase is typically found in the liver, adrenal glands, and fat tissue. In the context of breast cancer research, adjuvant therapy plays a crucial role. Exemestane, an aromatase inhibitor, is often considered an alternative to tamoxifen in research settings for postmenopausal models. Exemestane is often used as part of adjuvant hormonal therapy for postmenopausal women with estrogen-receptor positive early breast cancer, particularly for those transitioning from tamoxifen to complete a total of five consecutive years of therapy. Clinical trials have explored the efficacy of exemestane in reducing breast cancer recurrence, comparing different treatment regimens and highlighting its potential benefits and associated toxicities.
Indications and Uses
Exemestane is primarily indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. Additionally, it serves as an adjuvant treatment in postmenopausal women with early breast cancer who have completed 2 to 3 years of tamoxifen therapy. It is important to note that Exemestane is not indicated for the treatment of breast cancer in premenopausal women. This targeted use underscores its role in managing cancer in postmenopausal women, providing an effective option for those transitioning from tamoxifen therapy.
Dosage and Administration
The recommended dose of Exemestane is 25 mg once daily, taken after a meal to minimize gastrointestinal side effects. While it can be taken with or without food, post-meal administration is preferred. Consistency is key, so taking the dose at the same time every day helps maintain stable blood levels of the medication. For patients on a strong CYP 3A4 inducer, the maximum recommended dose is 50 mg once daily. This careful dosing ensures optimal efficacy and safety in patients receiving Exemestane.
Research into treatment of hormone-sensitive breast cancer with aromatase inhibitors
Against this background, various endocrine strategies have been tested in the search for effective cancer treatments. This has resulted in the development of specific antagonists of aromatase. These are third-generation compounds: anastrozole, letrozole, and exemestane. Studies indicate that other aromatase inhibitors also offer potential benefits and alternative options, especially for subjects experiencing intolerable effects with a current treatment. However, it is important to monitor for bone mineral density loss, a common side effect associated with aromatase inhibitors, to ensure the overall health and well-being of the subjects.
What is Exemestane for postmenopausal early breast cancer models?
Exemestane liquid and other forms of Exemestane are available as the brand name Aromasin. Anyone purchasing Exemestane for research needs to understand that it is a steroidal aromatase inhibitor, aiming to restrain the aromatase present in peripheral fat. In doing so, the aim is to restrict the levels of circulating estrogen that are present in post-menopausal test subjects. Aromatase inhibitors, such as exemestane, are known for their potential efficacy and pharmacologic properties in research, but they require careful monitoring.
Exemestane has an androstenedione-like structure, enabling it to compete with androstenedione and testosterone. It proceeds to form covalent bonds with the substrate-binding part of the enzyme, leading to eventual irreversible aromatase inactivation.
Early in vitro studies recognized Exemestane as a strong inhibitor. It has a stronger aromatase affinity compared to related compounds.
Following these early studies, work was conducted to study the antitumor effects of Exemestane, involving the use of rats with induced mammary tumors. The results of these experiments suggested that Exemestane has a high level of efficacy, whether administered orally or subcutaneously. Exemestane is particularly effective in research models of breast cancer in postmenopausal subjects, as it significantly reduces estrogen levels, which is crucial for this demographic in a research context. It is crucial to monitor patients for any adverse effects, including changes in bone mineral density, to ensure the safety and efficacy of the treatment.
Pharmacologic Properties
Exemestane is a potent steroidal aromatase inactivator, meaning it works by irreversibly binding to the aromatase enzyme. This binding prevents the conversion of androgens to estrogens, leading to a significant decrease in estrogen levels in the model. This reduction in estrogen can help slow the growth of hormone receptor-positive breast cancer cells in research settings, making Exemestane a valuable tool in the study of this disease.
One of the key attributes of Exemestane is its high specificity and affinity for the aromatase enzyme, allowing it to effectively inhibit estrogen production. Additionally, Exemestane boasts a high bioavailability, with a mean absolute bioavailability of 42% following oral administration. Once ingested, it is metabolized by the liver and primarily excreted through the kidneys. The half-life of Exemestane is approximately 27 hours, which supports a convenient once-daily administration regimen in research models. For patients receiving Aromasin, it is important to follow the recommended dosing guidelines to achieve optimal results and minimize potential side effects.
Adverse Reactions
Common adverse reactions to Exemestane include hot flashes, fatigue, arthralgia, headache, insomnia, increased sweating, and hypertension. More serious adverse reactions can occur, such as a reduction in bone mineral density (BMD) over time, leading to an increased risk of osteoporosis and fractures. Other serious adverse reactions include allergic reactions, liver damage, and changes in blood cell counts. Monitoring patients for these adverse reactions is crucial to ensure their safety and well-being during treatment.
Drug Interactions
Exemestane can interact with other medications, particularly estrogen-containing agents like hormone replacement therapy and birth control pills. These medications can interfere with Exemestane’s pharmacologic action, reducing its efficacy. Therefore, Exemestane should not be coadministered with systemic estrogen-containing agents. Additionally, strong CYP 3A4 inducers, such as rifampicin and phenytoin, can decrease Exemestane exposure. For patients receiving a strong CYP 3A4 inducer, dose modification is recommended to maintain the effectiveness of Exemestane.
Clinical Effectiveness
Research suggests that Exemestane has demonstrated significant potential in treating postmenopausal models with hormone receptor-positive breast cancer. In various clinical trials, Exemestane has been compared to other hormone therapies, such as tamoxifen, and has shown superior results in terms of disease-free survival and overall survival. Additionally, it is important to consider the potential impact of Exemestane on male and female fertility, and appropriate measures should be taken to address these concerns.
One notable study, the Intergroup Exemestane Study (IES), compared Exemestane to tamoxifen in postmenopausal models with early breast cancer. The findings revealed that Exemestane significantly improved disease-free survival and overall survival compared to tamoxifen. Specifically, the absolute benefit in disease-free survival was 3.3% at 5 years, and the hazard ratio for overall survival was 0.83, indicating a substantial advantage for models treated with Exemestane.
Exemestane has also been evaluated in the research of advanced breast cancer. In a phase III trial, Exemestane was compared to megestrol acetate, a progestin, in postmenopausal models with advanced breast cancer. The results suggested that Exemestane was superior to megestrol acetate in terms of time to tumor progression and overall survival, further establishing its efficacy in managing advanced stages of the disease.
Early Breast Cancer
Exemestane is used to study early breast cancer in postmenopausal models who have already received adjuvant tamoxifen therapy. Typically administered orally once a day, the treatment duration usually spans 2-3 years. Clinical studies have shown that Exemestane significantly improves disease-free survival and reduces the risk of breast cancer recurrence in postmenopausal models with early breast cancer. This makes it a valuable option for those transitioning from tamoxifen therapy to further reduce the likelihood of cancer returning. Exemestane is often used as part of adjuvant hormonal therapy for postmenopausal women with estrogen-receptor positive early breast cancer, particularly for those transitioning from tamoxifen to complete a total of five consecutive years of therapy.
Advanced Breast Cancer
Exemestane is also employed in the study of advanced breast cancer in postmenopausal models who have previously undergone hormone therapy. Often used in combination with other treatments, such as radiation, Exemestane helps to slow or halt the progression of cancer cells. Research has demonstrated its effectiveness in managing advanced breast cancer, providing a viable option for models who have not responded adequately to initial hormone therapies. For patients receiving Aromasin, it is important to follow the recommended dosing guidelines to achieve optimal results and minimize potential side effects.
Neoadjuvant Treatment
Exemestane is sometimes utilized as a neoadjuvant treatment for breast cancer, meaning it is administered before surgery to help shrink the tumor. By reducing the tumor size, Exemestane can make surgical removal more manageable and potentially improve overall treatment outcomes. This pre-surgical approach can be particularly beneficial in cases where the tumor is initially too large or in a challenging location for immediate surgery.
It is crucial to monitor patients for any adverse effects, including changes in bone mineral density, to ensure the safety and efficacy of the treatment.
Where to buy Exemestane
Research suggests that Exemestane is a valuable compound for studying advanced breast cancer. For those interested in purchasing Exemestane for research purposes, it can be obtained from Loti Labs, a leading online research supply company. Acquiring Exemestane from Loti Labs ensures the integrity of your research due to their rigorous quality control standards and third-party testing. When buying research substances online, it is crucial to choose a reputable source that stands behind their products.
Conclusion
In conclusion, Exemestane, marketed as Aromasin, stands out as a potent steroidal aromatase inhibitor with significant implications for breast cancer research. Its ability to effectively reduce estrogen levels makes it a valuable tool in the study of hormone receptor-positive breast cancer, particularly in postmenopausal models. Clinical trials have consistently demonstrated its superiority over other hormone therapies like tamoxifen, highlighting its potential to improve disease-free survival and overall survival rates. Furthermore, Exemestane’s efficacy in managing advanced breast cancer stages reinforces its role in cancer research. For researchers, acquiring Exemestane from reputable suppliers like Loti Labs ensures the integrity and reliability of their studies, paving the way for further advancements in breast cancer treatment.
References
Coombes, R. C., et al. (2004). “A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer.” New England Journal of Medicine, 350(11), 1081-1092.
Goss, P. E., et al. (2003). “Efficacy of adjuvant letrozole extended to five years in postmenopausal women after tamoxifen therapy: the MA.17 trial.” Lancet, 366(9483), 1711-1717.
Lonning, P. E., et al. (2000). “The pharmacokinetics of exemestane and its clinical implications.” European Journal of Cancer, 36(8), 976-982.
Smith, I. E., et al. (2005). “Neoadjuvant treatment of postmenopausal breast cancer with exemestane: results of a phase II trial.” Journal of Clinical Oncology, 23(22), 5108-5116.
Miller, W. R., & Dixon, J. M. (2002). “Aromatase inhibitors: mechanism of action and role in the treatment of breast cancer.” Seminars in Oncology, 29(3 Suppl 11), 3-8.
Howell, A., et al. (2005). “Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years’ adjuvant treatment for breast cancer.” Lancet, 365(9453), 60-62.
Lønning, P. E., et al. (2001). “Pharmacokinetics and pharmacodynamics of exemestane in breast cancer patients: clinical and preclinical studies.” Cancer Research, 61(18), 6719-6723.
Buzdar, A. U., et al. (2001). “Anastrozole versus megestrol acetate in the treatment of postmenopausal women with advanced breast carcinoma: results of a survival update based on a combined analysis of data from two mature phase III trials.” Cancer, 92(8), 2247-2258.
Lønning, P. E., & Geisler, J. (2008). “Breast cancer: recent advances in endocrine therapy.” Clinical Oncology, 20(5), 455-462.
Lønning, P. E., et al. (2005). “Exemestane: a review of its clinical efficacy and safety in the treatment of breast cancer.” Breast Cancer Research and Treatment, 91(2), 171-182.
