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A - Regimen Name

FLVS Regimen
Fulvestrant


Disease Site
Breast

Intent
Palliative

Regimen Category
Evidence-Informed :

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.


Rationale and Uses
  • 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 or recurrence following prior anti-estrogen therapy.
  • 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
 
B - Drug Regimen

fulvestrant
500 mg IM Days 1, 15 and 29 (loading dose), then every 28 days
(This drug is not currently publicly funded for this regimen and intent)
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C - Cycle Frequency

REPEAT EVERY 28 DAYS
Until evidence of disease progression or unacceptable toxicity

 
D - Premedication and Supportive Measures

Antiemetic Regimen:

Not applicable

 
E - Dose Modifications

Doses should be modified according to the protocol by which the patient is being treated. 

Dosage with toxicity

Toxicity
Action
Hypersensitivity

Consider discontinuing if severe

Mild hepatotoxicity

Hold until recovery and then restart

Moderate to severe hepatotoxicity

Discontinue



Hepatic Impairment

Fulvestrant is metabolized primarily in the liver.  There are no efficacy and safety data in patients with breast cancer and hepatic impairment.

Impairment Action
Mild to moderate (Child Pugh Class A or B) Use with caution. No dose adjustment needed.
Severe (Child Pugh Class C) Not studied. Use not recommended

Renal Impairment

CrCl (ml/min) Action (fulvestrant dose)
≥ 30 no dosage adjustment
< 30 use with caution; no data

Dosage in the Elderly

No adjustment required.


 
F - Adverse Effects

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

  • Injection site reaction (may be severe)
  • Fatigue
  • Nausea, vomiting
  • Increased LFTs (may be severe)

 

  • Arterial / venous thromboembolism
  • Hypersensitivity
  • Thrombocytopenia
  • Estrogen deprivation symptoms
 
G - Interactions

Refer to fulvestrant drug monograph(s) for additional details


Fulvestrant does not significantly inhibit any of the major cytochrome P450 (CYP) isoenzymes and has no inhibitory effects on CYP3A4. Although CYP3A4 is involved in the metabolism of fulvestrant, clinical trials have shown that dosage adjustment is not necessary in patients co-prescribed CYP3A4 inhibitors or inducers.

Fulvestrant may interfere with estradiol immunoassay measurements (falsely elevated estradiol levels) due to its structural similarity with estradiol. 

 
H - Drug Administration and Special Precautions

Refer to fulvestrant drug monograph(s) for additional details


Administration:

  • Drug supplied by outpatient prescription
  • Intramuscular injection, slowly administered into the buttock (1-2 minutes per injection); caution due to proximity of sciatic nerve and large vessels
  • According to local guidelines at the Cancer Centre or physician's office
  • Store refrigerated at 2 to 8°C in original package

Contraindications:

  • Patients with known hypersensitivity to the drug or to any of the excipients
  • Pregnant and breastfeeding women

Warnings/precautions:

  • Use with caution in patients with bleeding disorders or on anticoagulants
  • There is a potential osteoporosis risk due to fulvestrant's mechanism of action

Pregnancy & lactation:

  • Fulvestrant is contraindicated in pregnancy.  Adequate contraception should be used by both sexes during treatment, and for at least 6 months after the last dose.
  • Fulvestrant is secreted into animal milk and is contraindicated in breastfeeding. 
 
I - Recommended Clinical Monitoring

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

Suggested Clinical Monitoring

  • Renal function tests; baseline and as clinically indicated

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J - Administrative Information
Outpatient prescription; drug administration at Cancer Centre or physician's office

 
K - References

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, 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.

June 2019 Updated emetic risk category


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M - Disclaimer

Regimen Abstracts
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.
Information in regimen abstracts is accurate to the extent of the ST-QBP regimen master listings, and has not undergone the full review process of a regimen monograph.  Full regimen monographs will be published for each ST-QBP regimen as they are developed.
Regimen Monographs
Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.
The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.
The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.
Some Formulary documents, such as the medication information sheets, regimen information sheets and symptom management information (for patients), are intended for patients. Patients should always consult with their healthcare provider if they have questions regarding any information set out in the Formulary documents.
While care has been taken in the preparation of the information contained in the Formulary, 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.
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