Fulvestrant

Product introduction:

Fluticasone is an intramuscular injection developed by AstraZeneca. It was approved by the food and Drug Administration in April 2002 to treat estrogen receptor positive metastatic breast cancer in postmenopausal women whose disease is still deteriorating after anti estrogen therapy. Many breast cancer cells have estrogen receptor (ER), estrogen can stimulate the growth of such tumors. Fluvestrant is a "pure" estrogen receptor antagonist without partial estrogen like agonistic effect. It inhibits estrogen signal pathway by binding, blocking and down regulating er. It can competitively bind with ER. Its affinity with Er is close to estrogen, 100 times that of tamoxifen. It is the only anti estrogen drug that can be widely used in clinic after tamoxifen fails, Because the drug is endocrine therapy and will not cause common adverse reactions of chemotherapy, it has good patient compliance. A number of clinical studies have found that the dose of flustin 250mg is effective and safe in the second-line treatment of advanced breast cancer.

Mechanism of action:

Fluvestrant is a sterol anti estrogen drug. Its chemical structure is similar to that of estradiol. The difference is that it is in 7 α There is a connecting group at the position; It is 17 β- The alkyl amine analogues of estradiol can antagonize the estrogen effect by occupying ER and inhibit the gene activation stimulated by estrogen, so they affect the estrogen related processes necessary for cell cycle; Its affinity with Er is close to estrogen, but 100 times that of tamoxifen. Apoptosis is very important in maintaining homeostasis, and it may also be another main mechanism of the therapeutic effect of fluvestrant.

Adverse reactions:

Fulvestrant has fewer side effects, such as transient vaginal bleeding, body odor changes and sleepwalking. However, there are no reports such as vaginal dryness, weight gain, abnormal blood coagulation, thrombosis and sexual desire changes, and there are no changes in facial flushing, sweating and other characteristics.