Fulvestrant

What is Fulvestrant?

• Fulvestrant (Faslodex) is an estrogen receptor antagonist used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with palbociclib in women with disease progression after endocrine therapy.

Fulvestrant

Fulvestrant2DACS

What are the uses of this medicine?

• Faslodex is a prescription medicine used to treat advanced breast cancer or breast cancer that has spread to other parts of the body (metastatic).

Faslodex may be used alone, if you have gone through menopause, and your advanced breast cancer is:

• hormone receptor (HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative and has not been previously treated with endocrine therapy.

or

• HR-positive and has progressed after endocrine therapy.
• Faslodex may be used in combination with ribociclib, if you have gone through menopause, and your advanced or metastatic breast cancer is HR-positive and HER2-negative, and has not been previously treated with endocrine therapy or has progressed after endocrine therapy.
• Faslodex may be used in combination with palbociclib or abemaciclib if your advanced or metastatic breast cancer is HR-positive and HER2-negative, and has progressed after endocrine therapy.

• It is not known if Faslodex is safe and effective in children.
• It is not known if Faslodex is safe and effective in people with severe liver problems.

How does this medicine work?

• Fulvestrant (ful ves' trant) is a steroidal antiestrogen that is potent and direct antagonist or "down regulator" of the estrogen receptor.
• Fulvestrant is a synthetic derivative of estradiol and binds to the estrogen receptor with 100 times more potency than tamoxifen.
• It not only blocks the effects of estrogen, but also alters the structure of the estrogen receptor and further decreases the intracellular effects of estrogen.
• Unlike tamoxifen, fulvestrant is a pure antiestrogen and has no estrogen receptor agonist activity.
• Fulvestrant has been found to be as effective as tamoxifen as a first line agent to treat metastatic breast cancer, and is similar in efficacy to the aromatase inhibitors in women with progressive disease despite tamoxifen therapy.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• have had an allergic reaction to fulvestrant or any of the ingredients in Faslodex.

What drug interactions can this medicine cause?

• There are no known drug-drug interactions.

Is this medicine FDA approved?

• Fulvestrant was approved for use in the United States in 2002.

How should this medicine be used?

Recommended dosage:

• Faslodex 500 mg should be administered intramuscularly into the buttocks (gluteal area) slowly (1 - 2 minutes per injection) as two 5 mL injections, one in each buttock, on Days 1, 15, 29, and once monthly thereafter.

Hepatic Impairment:

• A dose of 250 mg is recommended in patients with moderate hepatic impairment to be administered intramuscularly into the buttock (gluteal area) slowly (1 - 2 minutes) as one 5 mL injection on Days 1, 15, 29, and once monthly thereafter.

Administration:

• Your healthcare provider will give you Faslodex by injection into the muscle of each buttock.
• Your healthcare provider may change your dose of Faslodex if needed.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As an injection for intramuscular administration, is supplied as 250 mg/5 mL fulvestrant

This medicine is available in fallowing brand namesː

• Faslodex

What side effects can this medication cause?

The most common side effects of this medicine include:

• injection site pain
• nausea
• muscle, joint, and bone pain
• headache
• back pain
• tiredness
• pain in arms, hands, legs, or feet
• hot flashes
• vomiting
• loss of appetite
• weakness
• cough
• shortness of breath
• constipation
• increased liver enzymes
• diarrhea

Faslodex may cause fertility problems in males and females.

Faslodex may cause serious side effects, including:

• Injection site related nerve damage

What special precautions should I follow?

• Because Faslodex is administered intramuscularly, it should be used with caution in patients with bleeding diatheses, thrombocytopenia, or anticoagulant use.
• Faslodex has not been studied in patients with severe hepatic impairment (Child-Pugh class C).
• Injection site related events including sciatica, neuralgia, neuropathic pain, and peripheral neuropathy have been reported with Faslodex injection. Caution should be taken while administering Faslodex at the dorsogluteal injection site due to the proximity of the underlying sciatic nerve.
• Based on findings from animal studies and its mechanism of action, Faslodex can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with Faslodex and for one year after the last dose.
• Due to structural similarity of fulvestrant and estradiol, Faslodex can interfere with estradiol measurement by immunoassay, resulting in falsely elevated estradiol levels.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Human experience of overdose with Faslodex is limited.
• No adverse reactions were seen in healthy male and female volunteers who received intravenous fulvestrant.

Management of overdosage:

• There is no specific treatment in the event of fulvestrant overdose, and symptoms of overdose are not established.
• In the event of an overdose, healthcare practitioners should follow general supportive measures and should treat symptomatically.

Can this medicine be used in pregnancy?

• Based on findings from animal studies and its mechanism of action, Faslodex can cause fetal harm when administered to a pregnant woman
• There are no available data in pregnant women to inform the drug-associated risk.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: fulvestrant.
• Inactive ingredients: alcohol, benzyl alcohol, benzyl benzoate, and castor oil.

Who manufactures and distributes this medicine?

Distributed by: AstraZeneca Pharmaceuticals LP Wilmington, DE

Manufactured for: AstraZeneca UK Limited Macclesfield, Cheshire, England

By: Vetter Pharma-Fertigung GMBH & Co. KG Ravensburg, Germany

What should I know about storage and disposal of this medication?

• Refrigrate, 2°-8°C (36°-46°F).

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• Dailymed label info on Fulvestrant
• FDA Fulvestrant

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