Faslodex (fulvestrant)

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There is no enhanced messaging for this drug.

Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.

Estrogen Receptor Blockers (Erbs)/Fluoroestradiol F-18

SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.

MECHANISM OF ACTION: Drugs that bind to the estrogen receptor (ER) may compete with the binding of radioactive diagnostic agent fluoroestradiol F-18.(1)

CLINICAL EFFECTS: Concurrent use of estrogen receptor blockers such as selective estrogen receptor modulators (SERMs) and selective estrogen receptor down-regulators (SERDs) may reduce the detection of ER-positive lesions with fluoroestradiol F-18.(1)

PREDISPOSING FACTORS: None determined.

PATIENT MANAGEMENT: Before administering fluoroestradiol F-18, discontinue drugs that bind to the ER, such as SERMs and SERDs, for at least 5 biological half-lives.(1) The following washout periods apply when discontinuing ERBs, prior to fluoroestradiol F-18 administration: - Bazedoxifene = 7 days - Clomiphene = 25 days - Elacestrant = 11 days - Enclomiphene = 25 days - Fulvestrant = 28 weeks - Imlunestrant = 7 days - Ospemifene = 5 days - Raloxifene = 7 days - Tamoxifen = 8 weeks - Toremifene = 5 weeks

DISCUSSION: The following ERBs are linked to this monograph: SERDs: elacestrant, imlunestrant, and fulvestrant. SERMs: bazedoxifene, clomiphene, enclomiphene, ospemifene, raloxifene, tamoxifen and toremifene.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

Known hypersensitivity to fulvestrant, benzyl alcohol, or any ingredient in the formulation.

• Lactation

• Child-pugh class B hepatic impairment
• Disease of liver
• Increased risk of bleeding due to coagulation disorder
• Pregnancy
• Thrombocytopenic disorder

There are no moderate contraindications for this drug.

The most common adverse effects of fulvestrant are adverse GI effects (e.g., nausea, vomiting, constipation, diarrhea, abdominal pain ), headache, back pain, vasodilation (hot flushes), and pharyngitis, which occurred in approximately 52, 15, 14, 18, and 16% of patients, respectively, who received the drug in clinical studies. Other adverse effects occurring in 5-23% of patients receiving fulvestrant (in order of descending frequency) include asthenia, pain, nutritional disorders, bone pain, dyspnea, injection site pain, increased cough, pelvic pain, anorexia, peripheral edema, rash, chest pain, flu syndrome, dizziness, insomnia, fever, paresthesia, urinary tract infection, depression, anxiety, and sweating. Injection site reactions with mild transient pain and inflammation were reported in 7% of patients receiving a single 5-mL injection of fulvestrant in one study and in 27% of those who received two 2.5-mL injections of the drug in another study.

Vaginal bleeding has been reported infrequently (less than 1%), usually during the first 6 weeks of changing from existing hormonal therapy to fulvestrant; however, if bleeding persists, the manufacturer states that further clinical evaluations may be necessary.

More Frequent

• Abnormal hepatic function tests
• Increased alanine transaminase
• Increased alkaline phosphatase
• Increased aspartate transaminase
• Infection

Less Frequent

• Deep venous thrombosis
• Neutropenic disorder
• Pulmonary thromboembolism

Rare or Very Rare

• Angioedema
• Cerebral thrombosis
• Hepatic failure
• Hepatitis
• Hyperbilirubinemia
• Hypersensitivity drug reaction
• Leukopenia
• Thromboembolic disorder

More Frequent

• Acute abdominal pain
• Anorexia
• Arthralgia
• Back pain
• Bone pain
• Chest pain
• Constipation
• Cough
• Depression
• Diarrhea
• Dizziness
• Drug-induced hot flash
• Dyspnea
• Fatigue
• Fever
• Flu-like symptoms
• General weakness
• Headache disorder
• Injection site sequelae
• Insomnia
• Musculoskeletal pain
• Nausea
• Pain
• Paresthesia
• Pelvic pain
• Peripheral edema
• Pharyngitis
• Pruritus of skin
• Skin rash
• Vasodilation of blood vessels
• Vomiting

Less Frequent

• Accidental injury
• Anemia
• Arthritis
• Hyperhidrosis
• Symptoms of anxiety
• Urinary tract infection

Rare or Very Rare

• Abnormal vaginal bleeding
• Myalgia
• Neuralgia
• Neuropathic pain
• Pain in extremities
• Peripheral neuropathy
• Sciatica
• Urticaria
• Vertigo

No enhanced messaging available.

Safety and efficacy of fulvestrant have not been established in pediatric patients.

Category D. (See Users Guide for a definition and see Warnings: Fetal/Neonatal Morbidity and Mortality, in Cautions for additional information.)

Fulvestrant is distributed into milk in rats; not known whether the drug is distributed into human milk. Discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Objective response rates reported in patients 65 years of age and older (11-16%) appear to be slightly lower than those reported in younger adults (22-24%).

The pharmacokinetics of fulvestrant are not altered substantially by age; therefore, the manufacturer states that dosage adjustment is not necessary in geriatric patients.