Breast cancer drug
Fluvestrant is an intramural drug developed by Astrazeneca and approved by the U.S. Food and Drug Administration in April 2002 for the treatment of estrogen receptor-positive metastatic breast cancer in postmenopausal women whose disease has worsened after anti-estrogen therapy. Many breast cancer cells have the estrogen receptor (ER), which stimulates the growth of such tumors. Fluvestrant is a "pure" estrogen receptor antagonist without partial estrogen-like stimulatory effect. It inhibits estrogen signaling pathway by binding, blocking and down-regulating ER. It can competitively bind with ER, and its affinity with ER is close to estrogen. Because it is an endocrine therapy, it will not cause the common adverse reactions of chemotherapy, so it has a good patient compliance. A number of clinical studies have found that 250mg dose of fluvestrine has good therapeutic effect and stable safety in second-line treatment of advanced breast cancer.
Action mechanism
Fluvestrant is a steroid anti-estrogen drug, its chemical structure is similar to estradiol, the difference is that it has a linking group at the 7α position; It is an alkylamine analogue of 17β-estradiol, which can antagonize the effect of estrogen by occupying ER and inhibit the activation of genes stimulated by this estrogen, thus affecting estrogen-related processes necessary for cell circulation; Its affinity with ER is close to estrogen. Apoptosis is essential for homeostasis and may be another major mechanism of the therapeutic effects of fluvestrant.
Pharmacological action
Fluvestrant has relatively poor oral bioavailability, so it is usually injected intramuscular with lipids as excipients. An open, randomized, multicenter study in postmenopausal women with advanced breast cancer showed no significant difference in pharmacokinetics and side effects of one 5ml or two 2.5ml injections of 250mg, with dose-dependent and individual differences in blood concentrations. There was no significant change in serum LH, FSH or SBHG levels during 7 days of treatment. The drug does not cross the blood-brain barrier and does not cause side effects such as vasomotor. In theory, estrogen inactivation can lead to increased bone turnover and promote osteoporosis, however, no such effect was found in animal models, nor did fluvestrant cause an increase in the replacement marker of bone turnover.
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Product Name
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Fulve-strant
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CAS No.
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129453-61-8
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