Anastrozole is a nonsteroidal aromatase inhibitor that blocks estrogen synthesis in postmenopausal animal models.
According to rat studies, anastrozole treated breast cancer cells shrink them, making it an antineoplastic agent. It is used in cancer research, especially in hormone receptor positive breast cancer studies. Researchers are also investigating anastrozole for prevention or slowing down of hormone-sensitive breast cancer in postmenopausal models at risk of breast cancer. It may also inhibit androstenedione-induced uterine hypertrophy in sexually immature rats.
Sold in 1 mg per ml vials for research and analytical use.
What is Anastrozole Aromatase Inhibitor?
Anastrozole is an anti-aromatase hormone that blocks estrogen synthesis and inhibits human placental aromatase. This is important in hormone receptor positive breast cancer research as estrogen plays a significant role in the growth of cancer cells in postmenopausal women. By blocking estrogen production, anastrozole may help reduce the growth and spread of these cancer cells, making it a valuable tool in cancer research.
It specifically inhibits human placental aromatase with high selectivity and low IC50 value, demonstrating its potency and efficacy in research. As a member of the nitrile and triazole family, anastrozole’s chemical structure allows it to target and inhibit the aromatase enzyme efficiently. Its role in research is crucial, especially in advanced breast cancer treatment and prevention of metastatic breast cancer.
Anastrozole is a research liquid used for hormone therapy in rats. It has great potential in managing breast cancer and provides new therapeutic approaches and understanding of cancer’s intrinsic endocrine effects. Research on anastrozole goes beyond cancer treatment as it is also being studied for its application in other estrogen-dependent conditions in animal models. Researchers are still investigating its efficacy and safety to gain a broader understanding of its benefits and side effects in different medical settings.
Structure of Anastrozole
- Molecular Formula: C17H19N5
- Molecular Weight: 293.4 g/mol
- CAS Number: 120511-73-1
- IUPAC Name: 2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
Uses, Benefits, and Research Applications in Breast Cancer
Anastrozole is a nonsteroidal third-generation aromatase inhibitor. It binds selectively and reversibly to aromatase, a cytochrome P-450 enzyme complex that interferes with estradiol production in peripheral tissues including premenopausal ovary, liver, breast, and other fatty tissues.
Since estrogen is a growth factor for hormone-dependent breast cancer cells, anastrozole can be used to treat animal models of breast cancer caused by estrogen.
Anastrozole has a long duration of action and can be given once a day. Its half-life is around 50 hours. It is also used in the treatment of advanced breast cancer that has progressed after tamoxifen therapy.
Mechanism of Action and Uses
Anastrozole is a potent and highly selective aromatase inhibitor that works by inhibiting the enzyme aromatase, which is involved in estrogen production in the body. By blocking estrogen production, anastrozole reduces the growth of hormone-sensitive breast cancer cells. This makes it effective in breast cancer in postmenopausal women with hormone receptor positive early breast cancer. Anastrozole is also used in the treatment of advanced breast cancer that has progressed after tamoxifen therapy. By targeting the estrogen production pathway, anastrozole slows down or shrinks the growth of breast cancer cells, making it a valuable tool in the fight against this disease.
Comparison to Other Aromatase Inhibitors
Anastrozole is a third-generation aromatase inhibitor known for its high selectivity and potency compared to previous generations. This selectivity allows anastrozole to reduce estrogen levels more effectively and slow down breast cancer cell growth. Clinical trials have shown anastrozole to be as effective, if not more effective, than tamoxifen, another hormone therapy for breast cancer. These trials have demonstrated that anastrozole reduces breast cancer recurrence and has a better side effect profile compared to other aromatase inhibitors. This makes anastrozole a preferred choice in many treatment protocols for hormone receptor positive breast cancer.
Handling and Storage
Proper handling and storage of anastrozole is important to ensure its effectiveness and integrity in research applications. This compound should be stored in a sealed container at room temperature, protected from moisture and light. Research protocols suggest keeping the container closed in its original packaging and storing it in a location inaccessible to unauthorized personnel. By following these guidelines, researchers can maintain the integrity of the substance and obtain reliable results in their experimental studies.
Research Dose and Administration
The recommended research dose of anastrozole is 1 mg per day, orally in test subjects. Research protocols suggest administering the compound at consistent times daily with or without food to maintain uniform blood levels. For test subjects with feeding difficulties, anastrozole is available in 1 mg/ml gastric tube liquid form, which can be administered via gastric tube. Follow the administration protocol strictly in laboratory settings. Researchers should adhere to these guidelines meticulously to obtain accurate and reliable results in their experimental work.
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References
- Lønning P (2003). “Clinical pharmacokinetics of aromatase inhibitors and inactivators”. Clinical Pharmacokinetics. 42 (7): 619–31. doi:10.2165/00003088-200342070-00002. PMID 12844324. S2CID 9585901.
- Lønning P, Pfister C, Martoni A, Zamagni C (2003). “Pharmacokinetics of third-generation aromatase inhibitors”. Seminars in Oncology. 30 (4 Suppl 14): 23–32. doi:10.1016/S0093-7754(03)00305-1. PMID 14513434.
- Sanford M, Plosker GL (2008). “Anastrozole: a review of its use in postmenopausal women with early-stage breast cancer”. Drugs. 68 (9): 1319–40. doi:10.2165/00003495-200868090-00007. PMID 18547136.
- ChEBI. European Molecular Biology Laboratory. Retrieved 14 August 2011.
- “Anastrozole Highlights of Prescribing Information” (PDF). FDA. 31 July 2019.
- ASHP. 21 December 2016. Retrieved 8 December 2016.
- Chen S (1998) Aromatase and breast cancer. Front Biosci 3: d922–d933
