Fulvestrant, also known as ICI-182780, is a medication used to treat hormone receptor-positive (HR+) breast cancer in postmenopausal women. It belongs to the class of drugs called selective estrogen receptor degraders (SERDs), which work by binding to and degrading the estrogen receptor (ER) in breast cancer cells. Fulvestrant was developed by AstraZeneca and approved by the US Food and Drug Administration (FDA) in 2002 under the brand name Faslodex.
Chemical Name:
(7α,17β)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Molecular Formula:
C32H47F5O3S
Formula Weight:
606.77 g/mol
CAS No:
129453-61-8
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Synonyms:
ICI-182780
Health Benefits of Fulvestrant:
Fulvestrant has been shown to effectively treat HR+ breast cancer in postmenopausal women who have progressed on prior endocrine therapy. In clinical trials, fulvestrant demonstrated improved progression-free survival (PFS) compared to aromatase inhibitors such as anastrozole and exemestane. Additionally, fulvestrant may have potential applications in other hormone-dependent cancers such as prostate cancer.
Potential Effects:
Aside from its anti-cancer effects, fulvestrant may also have beneficial effects on bone health. Estrogen plays a crucial role in maintaining bone density, and its loss during menopause can lead to osteoporosis. By blocking the effects of estrogen on breast cancer cells, fulvestrant may also indirectly protect against bone loss and fractures. Additionally, fulvestrant may have potential uses in combination with other treatments such as immune checkpoint inhibitors or CDK4/6 inhibitors.
Product Mechanism:
Fulvestrant works by binding to the estrogen receptor and causing its degradation, which reduces the number of receptors available for estrogen to bind to. This leads to decreased signaling through the ER pathway, which is critical for the growth of many HR+ breast cancers. Unlike other anti-estrogen drugs like tamoxifen or aromatase inhibitors, fulvestrant does not block estrogen from binding to the receptor but rather removes the receptor itself.
Safety:
Fulvestrant has a favorable safety profile, with most adverse events being mild to moderate in severity. The most common side effects include injection site pain, nausea, fatigue, and hot flashes. More serious side effects such as liver dysfunction, blood clots, and allergic reactions are rare but can occur. Fulvestrant should not be used in women who are pregnant, as it can cause harm to the developing fetus.
Dosing Information:
The recommended dose of fulvestrant is 500 mg administered by intramuscular injection on days 1, 15, and 29, followed by monthly injections thereafter. It can be given as a single injection or divided into two separate injections of 250 mg each. Fulvestrant should be administered by a healthcare professional and patients should receive appropriate premedication to reduce injection site pain.
Conclusion:
In conclusion, fulvestrant is a valuable treatment option for HR+ breast cancer in postmenopausal women who have progressed on prior endocrine therapy. Its unique mechanism of action and lack of cross-resistance with other anti-estrogen drugs make it an important addition to the armamentarium against this disease. Furthermore, its potential benefits on bone health and combination with other treatments may broaden its utility even further. Ongoing studies are exploring its use in earlier stages of breast cancer and in other hormone-dependent cancers, which could expand its indications in the future.
