Fulvestrant Brand Name– FASLODEX
What is Fulvestrant
Fulvestrant is an intramuscular estrogen-receptor antagonist without any known estrogen agonist effects. It was the first in a class of antiestrogens that works by downregulating the estrogen receptor as opposed to blocking it as with tamoxifen.
Fulvestrant has demonstrated potent inhibition of breast cancer cells in vitro and in vivo.
In clinical trials, fulvestrant was as effective as anastrozole, an aromatase inhibitor, in postmenopausal women who had received previous hormonal therapy.
Fulvestrant is FDA approved in postmenopausal women as monotherapy or in combination with ribociclib for the first-line treatment of hormone receptor (HR)-positive, HER2-negative advanced breast cancer and as monotherapy or in combination with ribociclib for the treatment of HR-positive advanced breast cancer after disease progression following endocrine therapy.
It is FDA approved in combination with palbociclib or abemaciclib for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer in women after disease progression on endocrine-based therapy.
Pregnancy should be avoided during treatment and for 1 year after the last dose of fulvestrant. Fulvestrant can also interfere with estradiol measurement by immunoassay, resulting in falsely elevated estradiol levels.
Indications
- breast cancer
For the treatment of breast cancer
for the treatment of hormone receptor (HR)-positive, HER2-negative advanced breast cancer in postmenopausal women who have not previously been treated with endocrine therapy, as monotherapy
Side Effects
- abdominal pain
- acneiform rash
- alopecia
- anemia
- angioedema
- anorexia
- anxiety
- arthralgia
- asthenia
- back pain
- bone pain
- cheilitis
- chest pain (unspecified)
- conjunctivitis
- constipation
- cough
- cystitis
- depression
- diaphoresis
- diarrhea
- dizziness
- dysgeusia
- dyspnea
- elevated hepatic enzymes
- fatigue
- fever
- glossitis
- headache
- hepatic failure
- hepatitis
- hot flashes
- hyperbilirubinemia
- hypoalbuminemia
- hypoglycemia
- hypophosphatemia
- infection
- influenza
- injection site reaction
- insomnia
- leukopenia
- maculopapular rash
- musculoskeletal pain
- myalgia
- nausea
- neuropathic pain
- neutropenia
- ocular infection
- oral ulceration
- paresthesias
- pelvic pain
- peripheral edema
- peripheral neuropathy
- pharyngitis
- pruritus
- pulmonary embolism
- rash
- rhinitis
- stomatitis
- thrombocytopenia
- thromboembolism
- thrombosis
- urticaria
- vaginal bleeding
- vertigo
- vomiting
- weight loss
Monitoring Parameters
- pregnancy testing
Contraindications
- anticoagulant therapy
- breast-feeding
- children
- coagulopathy
- contraception requirements
- hepatic disease
- infants
- infertility
- laboratory test interference
- neonates
- neurologic events
- peripheral neuropathy
- pregnancy
- pregnancy testing
- reproductive risk
- thrombocytopenia
Interactions
- Fluoroestradiol F 18
Fluoroestradiol F 18: (Major) Administer fluoroestradiol F 18 before starting fulvestrant; however, do not delay indicated therapy to administer fluoroestradiol F 18. Fulvestrant may block estrogen receptors (ER) for up to 28 weeks and reduce the uptake of fluoroestradiol F 18 and detection of ER-positive lesions.