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Faslodex Quick Detail:
674.8Â° C at 760 mmHg
Antiestrogen;A novel sterodal estrogen antagonist reported to lack any partial agonist activity. Antineoplastic (hormonal).
Faslodex (Faslodex, AstraZeneca) is a drug treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works by down-regulating the estrogen receptor.
Faslodex is a selective estrogen receptor down-regulator (SERD). Faslodex is indicated for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. The dosing schedule for Faslodex remains under investigation in an attempt to optimize its effectiveness.
Faslodex provided effective second-line therapy in this setting for postmenopausal women who had relapsed or progressed after previous endocrine therapy.
Faslodex is used to treat some hormone-related breast cancer and postmenopausal women whose breast cancer has progressed after treatment with other anti-estrogen medication.It is an estrogen receptor antagonist and works by blocking estrogen from tumors that need estrogen to grow. Faslodex is also being studied in the treatment of other types of cancer,it is used to treat hormone receptor positive breast cancer in women who have experienced menopause and whose breast cancer has worsened after they were treated with antiestrogen medications.This can slow or stop the growth of some breast tumors that need estrogen to
Many breast cancers are stimulated to grow by the female sex hormones oestrogen and progesterone.These breast cancers are called hormone sensitive or hormone receptor positive. Drugs that block the effects of these hormones can slow or stop the growth of the breast cancer cells. Faslodex stops oestrogen getting to the cancer cells by blocking oestrogen receptors and reducing the number of receptors the cancer cell has.
In particular 4 clinical trials in this setting did show similar efficacy to the other hormonal agents with good
tolerability profile. Faslodex had a lower incidence of joint disorders.
Medicine for Breast Cancer:
Faslodex (trade name Faslodex) which was developed by AstraZeneca isan intramuscular injection drug, and it was approved for marketing by the US Food and Drug Administration in April 2002. FaslodexÂ is a drug treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. The use of hormone therapy to treat cancer is based on the observation that receptors for specific hormones that are needed for cell growth are on the surface of some tumor cells.Many breast cancer cells have estrogen receptor (ER), and these cancers rely on the hormone oestrogen to grow, This type of breast cancer is called oestrogen-receptor positive (ER positive) breast cancer. Drugs that block the effects of these hormones can slow or stop the growth of the breast cancer cells.
FaslodexÂ stops oestrogen getting to the cancer cells by blocking oestrogen receptors and reducing the number of receptors the cancer cells have.Thus,Faslodex is a " pure" estrogen receptor antagonists, it has no partial estrogen-like effect of excitement, which can inhibit estrogen signaling pathway by binding, blocking and reduced ER. Faslodex has competitively combine with ER, its binding capacity with ER was the same as estrogen, but is about 100 times as tamfen.
Faslodex provided effective second-line therapy in this setting for postmenopausal women whose breast cancer has worsened after they were treated with antiestrogen medications such as tamfen.Faslodex is a hormone therapyand itdoes not cause common adverse reactions as in chemotherapy, so it has a better patient compliance. A number of clinical studies have approved that a dosage of 250mg Faslodex has a outstanding effect and security stability in the second-line treatment of advanced breast cancer.
Mechanism of Action:
Faslodex is an anti-estrogen drugs, its chemical structure is almost like estradiol, the difference is that there is functional group at 7Î± position, thus it is a analogues of 17Î²-estradiol alkylamines. Many breast cancer cells have estrogen receptor (ER) which are stimulated to grow by the female sex hormones oestrogen and progesterone. Faslodex can stop oestrogen getting to the cancer cells by blocking oestrogen receptors and reducing the number of receptors the cancer cells have.It can antagonize the action of estrogen by occupying the ER, and thereby suppress stimulation of gene activation by estrogen, so as toaffect estrogen related processes required by cell cycle.Its affinity with ER is close to estrogen, which is100 times as tamfen.Apoptosis is very essential in maintaining homeostasis, and it could also be another major mechanism of Faslodex therapy.
Faslodex has poor oral bioavailability, it comes as a solution (liquid) in the buttockto be administeredvia intramuscular injection once a month.Open, randomized and multi-center study in postmenopausal women with advanced breast cancer showed that dosage ofonce 5 ml or twice 2.5 ml injection of FaslodexÂ product 250 mg have no significant difference on pharmacokinetic and toxicity,but have individual differences in blood concentration and dose-dependent manner.
The serum LH, FSH or SBHG levels did not change significantly during 7d treatment. Faslodex can`t pass into blood-brain barrier to cause side effects such as vasomotor.Theoretically, estrogen inactivation can lead to increased bone turnover, promote osteoporosis, however this dosen`t happenedin animal models. FaslodexÂ can`t lead to increased surrogate marker of bone turnover.
A white to off-white crystalline powder
A white crystalline powder
The retention time of the major peak in the chromatogram of the assay preparation is same as that of the standard preparation obtained in the assay
Any Individual impurity
Not more than 0.10%
Not more than 1.0%
Faslodex is used to treat hormone receptor positive breast cancer in women who have experienced menopause and whose breast cancer has worsened after they were treated with antiestrogen medications such as tamfen Faslodex is in a class of medications called estrogen receptor antagonists.
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