Fulvestrant


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Estrogen receptor positive locally advanced breast cancer in postmenopausal women, Estrogen receptor positive metastatic breast cancer in postmenopausal women
Adult: As monotherapy for those who are not previously treated with endocrine therapy, or with disease relapse on or after adjuvant antiestrogen therapy, or disease progression on antiestrogen therapy: 500 mg (250 mg into each buttock) on days 1, 15, and 29, then once monthly thereafter.

Intramuscular
Hormone receptor positive, HER2-negative locally advanced carcinoma of breast, Hormone receptor positive, HER2-negative metastatic carcinoma of breast
Adult: In combination with palbociclib or abemaciclib, in women with disease progression following endocrine therapy: 500 mg (250 mg into each buttock) on days 1, 15, and 29, then once monthly thereafter. Continue until disease progression or unacceptable toxicity.

Intramuscular
Hormone receptor positive, HER2-negative locally advanced breast cancer in postmenopausal women, Hormone receptor positive, HER2-negative metastatic breast cancer in postmenopausal women
Adult: In combination with ribociclib, as initial endocrine-based therapy or following disease progression on endocrine therapy: 500 mg (250 mg into each buttock) on days 1, 15, and 29, then once monthly thereafter. Continue until disease progression or unacceptable toxicity.
Hepatic Impairment
Moderate (Child-Pugh Class B): 250 mg (into 1 buttock) on days 1, 15, and 29, then once monthly thereafter. Severe: Contraindicated.
Chống chỉ định
Severe hepatic impairment. Pregnancy and lactation.
Thận trọng
Patient with bleeding diatheses, thrombocytopenia. Administration at dorsogluteal injection site. Mild to moderate hepatic and severe renal (CrCl <30 mL/min) impairment.
Phản ứng phụ
Significant: Hypersensitivity reactions (e.g. angioedema, urticaria), injection site-related events (e.g. neuropathic pain, peripheral neuropathy, sciatica, neuralgia), thromboembolic events, risk of osteoporosis.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea.
General disorders and administration site conditions: Asthenia.
Investigations: Increased ALT, AST, ALP, bilirubin.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Joint and musculoskeletal pain, back pain.
Nervous system disorders: Headache, vertigo.
Renal and urinary disorders: UTI.
Reproductive system and breast disorders: Vaginal haemorrhage.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Hot flushes.
MonitoringParameters
Monitor LFT, signs and symptoms of bleeding. Perform pregnancy test within 7 days prior to initiation.
Tương tác
Increased risk of bleeding with anticoagulants.
Lab Interference
May interfere with estradiol immunoassay, resulting in falsely elevated estradiol levels.
Tác dụng
Description: Fulvestrant competitively binds to estrogen receptors on tumours, forming a nuclear complex, causing down-regulation of estrogen receptor protein levels and inhibition of tumour growth.
Pharmacokinetics:
Absorption: Slowly absorbed. Time to peak plasma concentration: Approx 7 days.
Distribution: Extensively and rapidly distributed, primarily into the extravascular space. Volume of distribution: Approx 3-5 L/kg. Plasma protein binding: 99%, mainly to LDL, VLDL, and HDL fractions.
Metabolism: Metabolised mainly in the liver via multiple pathways to form several metabolites.
Excretion: Mainly via faeces (approx 90%); urine (<1%). Elimination half-life: Approx 40-50 days.
Đặc tính

Chemical Structure Image
Fulvestrant

Source: National Center for Biotechnology Information. PubChem Database. Fulvestrant, CID=104741, https://pubchem.ncbi.nlm.nih.gov/compound/Fulvestrant (accessed on Jan. 21, 2020)

Bảo quản
Store between 2-8°C. Protect from light.
Phân loại MIMS
Phân loại ATC
L02BA03 - fulvestrant ; Belongs to the class of anti-estrogens. Used in treatment of neoplastic diseases.
References
Anon. Fulvestrant. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/11/2020.

Buckingham R (ed). Fulvestrant. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

Faslodex 250 mg Solution for Injection (AstraZeneca UK Limited). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2020.

Faslodex Injection (AstraZeneca Pharmaceuticals LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/11/2020.

Fulvestrant 250 mg Solution for Injection in Pre-Filled Syringe (Genus Pharmaceuticals [Trading as Stada]). MHRA. https://products.mhra.gov.uk/. Accessed 04/11/2020.

Joint Formulary Committee. Fulvestrant. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

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