Regimen is considered appropriate as part of the standard care of patients; meaningfully improves outcomes (survival, quality of life), tolerability or costs compared to alternatives (recommended by the Disease Site Team and national consensus body e.g. pan-Canadian Oncology Drug Review, pCODR). Recommendation is based on an appropriately conducted phase III clinical trial relevant to the Canadian context OR (where phase III trials are not feasible) an appropriately sized phase II trial. Regimens where one or more drugs are not approved by Health Canada for any indication will be identified under Rationale and Use.
For the treatment of metastatic or locally advanced hormone-receptor-positive (ER+ and/or PR+) breast cancer in postmenopausal women, regardless of age, who have disease progression following prior anti-estrogen therapy
For the treatment of estrogen receptor-positive, human epidermal growth receptor 2 (HER2) negative locally advanced or metastatic breast cancer in postmenopausal women not previously treated with endocrine therapy
ODB - General Benefit (fulvestrant)
|fulvestrant||500 mg||IM||Days 1, 15 and 29 (loading dose), then Day 1 every 28 days|
REPEAT EVERY 28 DAYS
Until evidence of disease progression or unacceptable toxicity
Doses should be modified according to the protocol by which the patient is being treated.
Dosage with toxicity
Consider discontinuing if severe.
Hold until recovery and then restart.
Moderate to severe hepatotoxicity
Fulvestrant is metabolized primarily in the liver. There are no efficacy and safety data in patients with breast cancer and hepatic impairment. Decreased clearance (by 2.2 fold) and changes in exposure (↑ 70%) were observed in women with moderate hepatic impairment compared to patients with normal hepatic function.
|Hepatic Impairment||Fulvestrant Dose|
Mild to Moderate
(Child-Pugh Class A or B)
|Use with caution. No dose adjustment required.|
(Child-Pugh Class C)
|Not studied. Use not recommended.|
|Creatinine Clearance (mL/min)||Fulvestrant Dose|
|≥ 30||No dosage adjustment required.|
|< 30||Use with caution; no data.|
Dosage in the Elderly
No dosage adjustment required.
Refer to fulvestrant drug monograph(s) for additional details of adverse effects.
Less common (10-24%)
Uncommon (< 10%),
but may be severe or life-threatening
Refer to fulvestrant drug monograph(s) for additional details.
- Fulvestrant may interfere with estradiol immunoassay measurements (falsely elevated estradiol levels) due to its structural similarity with estradiol.
Refer to fulvestrant drug monograph(s) for additional details.
- Each dose consists of 2 pre-filled syringes (250 mg/5mL). Administer each pre-filled syringe as SLOW intramuscular injection (1-2 minutes per injection) into EACH buttock.
- Caution should be taken due to proximity of the sciatic nerve and large blood vessels.
- Administer according to local guidelines at the Cancer Centre or physician's office.
- Store refrigerated at 2 to 8°C in original package.
- Patients with known hypersensitivity to the drug or to any of the formulation or container
- Pregnant and breastfeeding women
- Due to the route of administration, use with caution in patients with bleeding disorders or on anticoagulants.
- Exercise caution when driving or operating machinery due to fatigue.
- There is a potential osteoporosis risk due to fulvestrant's mechanism of action.
- Fulvestrant is contraindicated in pregnancy. Adequate contraception should be used by both sexes during treatment, and for at least 2 years after the last dose.
- Breastfeeding: Contraindicated
- Fertility effects: Probable
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
Recommended Clinical Monitoring
Liver function tests; Baseline and as clinically indicated
Clinical assessment of injection site reactions, hypersensitivity, estrogen deprivation symptoms, fatigue, thromboembolism and musculoskeletal effects; At each visit
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
Suggested Clinical Monitoring
- Renal function tests; Baseline and repeat as clinically indicated
Outpatient prescription; drug administration at Cancer Centre or physician's office
Chia S, Gradishar W, Mauriac L, et al. Double-blind, randomized placebo controlled trial of fulvestrant compared with exemestane after prior nonsteroidal aromatase inhibitor therapy in postmenopausal women with hormone receptor-positive, advanced breast cancer: results from EFECT. J Clin Oncol 2008; 26:1664-70.
Di Leo A, Jerusalem G, Petruzelka L, et al. Results of the CONFIRM phase III trial comparing fulvestrant 250 mg with fulvestrant 500 mg in postmenopausal women with estrogen receptor-positive advanced breast cancer. J Clin Oncol 2010;28(30):4594-600.
Fulvestrant drug monograph, Ontario Health (Cancer Care Ontario).
Howell A, Pippen J, Elledge RM, et al. Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma: a prospectively planned combined survival analysis of two multicenter trials. Cancer 2005;104(2):236-9.
Howell A, Robertson JF, Abram P, et al. Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: A multinational, double-blind, randomized trial. J Clin Oncol 2004;22:1605-13.
Howell A, Robertson JFR, Quersma Albano J, et al. Fulvestrant, formerly ICI182,870 is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. JCO 2002;20:3396-403.
McCormack P, Sapunar F. Pharmacokinetic profile of the fulvestrant loading dose regimen in postmenopausal women with hormone receptor-positive advanced breast cancer. Clin Breast Cancer 2008;8(4):347-51.
Osborne CK, Pippen J, Jones SE et al. Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial. J Clin Oncol 2002;20:3386-95.
Robertson JFR, Bondarenko IM, Trishkina E, et al. Fulvestrant 500 mg versus anastrozole 1 mg for hormone receptor-positive advanced breast cancer (FALCON): an international, randomised, double-blind, phase 3 trial. Lancet. 2016 Dec 17;388(10063):2997-3005.
Robertson JFR, Osborne CK, Howell A et al. Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma in postmenopausal women: a prospective combined analysis of two multicentre trials. Cancer 2003;98:229-38.
November 2020 Updated monitoring section
A Regimen Abstract is an abbreviated version of a Regimen Monograph and contains only top level information on usage, dosing, schedule, cycle length and special notes (if available). It is intended for healthcare providers and is to be used for informational purposes only. It is not intended to constitute or be a substitute for medical advice, and all uses of the Regimen Abstract are subject to clinical judgment. Such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability, and Cancer Care Ontario disclaims all liability for the use of this information, and for any claims, actions, demands or suits that arise from such use.
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