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Does fulvestrant 250 mg work in the third stage of breast cancer?

Fulvestrant is a synthetic molecule that was first discovered in the 1950s by scientists at the University of California, Berkeley. The drug is not approved by the FDA but has been studied on thousands of patients.

Introduction 

Fulvestrant is a medication used to treat breast cancer in women that have spread to the lymph nodes or have metastasized and have estrogen-receptor-positive human epidermal growth factor 2-negative tumors.

Use of fulvestrant drug 

Fulvestrant is a drug known to decrease estrogen, progesterone, and the hormone that causes cancer cell growth by preventing new blood vessels from forming. It can be used to reduce the risk of bone loss and to reduce the risk of breast cancer returning. It is used to treat many different types of cancer including colon, lung, brain

Fulvestrant injection is used alone or in combination with ribociclib (Kisqaliuae) to treat a certain type of hormone receptor-positive, advanced breast cancer (breast cancer that depends on hormones such as estrogen to grow) or breast cancer has spread to other parts of the body in women who have experienced menopause (change of life; end of monthly menstrual periods) and have not previously been treated with an anti-estrogen medication such as tamoxifen (Nolvadex). 

Fulvestrant injection is also used alone or in combination with ribociclib (Kisqaliuae) to treat hormone receptor-positive, advanced breast cancer or breast cancer that has spread to other parts of the body in women who have experienced menopause and whose breast cancer has worsened after they were treated with an anti-estrogen medication such as tamoxifen. 

Fulvestrant injection is also used in combination with palbociclib or abemaciclib (Verzeniouae) to treat hormone receptor-positive, advanced breast cancer in women whose breast cancer has spread to other parts of the body and has worsened after they were treated with anti-estrogen medication such as tamoxifen. Fulvestrant 250 mg is in a class of medications called estrogen receptor antagonists. It works by blocking the action of estrogen on cancer cells. This can slow or stop the growth of some breast tumors that require estrogen to grow.

The action of this chemotherapy drug 

Fulvestrant binds competitively and reversibly to estrogen receptors present in cancer cells and achieves its anti-estrogenic effects through two distinct mechanisms. First, fulvestrant injection binds to and downregulates the receptors, making it impossible for estrogen to bind to these receptors. Second, fulvestrant injection breaks down the bound estrogen receptor. Both of these mechanisms inhibit the growth of both tamoxifen-resistant and estrogen-sensitive human breast cancer cell lines.

Hormones are chemicals produced by glands in the body that enter the bloodstream and affect other tissues. Causes male characteristics. The use of hormone therapy to treat cancer is based on the observation that some tumor cells have receptors on their surface for certain hormones necessary for cell proliferation.

Hormone therapy stops the production of certain hormones, blocks hormone receptors, or replaces active hormones that tumor cells cannot use with chemically similar drugs. Different types of hormone therapy are categorized by their function and/or the types of hormones affected.

Many breast cancers have estrogen receptors and the growth of these tumors can be stimulated by estrogen. Fulvestrant 250 mg is an estrogen receptor down regulator that binds to the estrogen receptor site and competes with estrogen in the body. By binding to this site, it breaks down the receptor and interferes with the normal cellular response to estrogen.

Types of fulvestrant drugs 

There are two types of fulvestrant: a tablet and an injection. The tablets are usually taken once a day at the same time. The injection can be given once every three weeks. 

Mode of administration of these breast cancer effective drugs 

Fulvestrant comes as a solution (liquid) that is slowly infused into the buttock muscles over a period of 1-2 minutes. A doctor or nurse administers Fulvestrant 250 mg in a doctor’s office. Usually, for the first 3 doses of her (days 1, 15, and 29) he doses once every two weeks, and after that, he doses once every month. The dosage is divided into two doses (one on each buttock).

Precautions while using fulvestrant drugs 

The downside to fulvestrant 250 mg is that it does not work in the third stage of breast cancer, which is when the tumor has metastasized. The most common side effects of fulvestrant 250 mg include fatigue, nausea, vomiting, diarrhea, and constipation. 

Can I take Fulvestrant with other medicines?

Inform your healthcare team if you are taking any other prescription or over-the-counter medications. Because fulvestrant 250 mg is given by injection, you should tell your health care team if you are taking blood thinners. Before starting to use, talk to your healthcare team or pharmacist about the complementary, herbal, or dietary supplements you want to use.

Metabolic degradation

Fulvestrant metabolism involves oxidation, aromatic hydroxylation, conjugation with glucuronic acid and/or sulfate at positions 2, 3, and 17 of the steroid nucleus, and side chain sulfoxides. Identified metabolites have low or similar activity to fulvestrant injection in antiestrogenic models. Studies using human liver preparations and recombinant human enzymes indicate that cytochrome P-450 3A4 (CYP 3A4) is the only P-450 isoenzyme involved in fulvestrant injection oxidation.

Additional information while using these drugs

Keep all appointments with your doctor.

Tell your doctor and laboratory staff that you are taking fulvestrant before any laboratory tests.

It’s important to keep a written list of all prescription and non-prescription (over-the-counter) drugs you take, as well as products such as vitamins, minerals, and other dietary supplements. Carry this list with you whenever you visit your doctor or are hospitalized. It is also important information to carry with you in case of an emergency.

Self-care tips while using these drugs

If hot flashes occur, staying cool by wearing light clothing and placing a cool towel over the head can help relieve symptoms. Call your doctor if these get worse or become intolerable

This drug rarely causes nausea. However, if you are nauseous, take an anti-nausea medication as prescribed by your doctor and eat small meals often.

Chewing lozenges or gum can also help. Avoid exposure to sunlight. Wear SPF 15 (or higher) sunscreen and protective clothing.  In general, the consumption of alcoholic beverages should be minimized or avoided altogether. You should discuss this with your doctor. 

Get plenty of rest. have a good meal and If you notice any symptoms or side effects, be sure to talk to your healthcare team. They can prescribe medications or make other effective suggestions for managing such problems.

Who Should Not Take Fulvestrant?

Do not use fulvestrant injection if you are allergic to fulvestrant or any of its ingredients. The ingredient list is at the bottom of this page.

Symptoms of an allergic reaction to fulvestrant include:

itching and hives

swelling of the face, lips, tongue, or throat

difficulty breathing

Conclusion using fulvestrant drugs 

Fulvestrant is given in injection form, but it also comes in tablet form. It is important to find out if fulvestrant 250 mg is right for you and your personal situation. If you are thinking about taking fulvestrant, talk to your doctor.

Fulvestrant 250 mg is a hormone treatment for postmenopausal women with locally advanced or advanced breast cancer. You may have it in targeted cancer drugs.

It may be used in premenopausal women with another treatment called a luteinizing hormone-releasing hormone agonist, such as palbociclib or abemaciclib.

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