Fulvestrant, sold under the brand name Faslodex among others, is an antiestrogenic medication used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with abemaciclib or palbociclib in women with disease progression after endocrine therapy.[2] It is given by injection into a muscle.[5]
Fulvestrant is a selective estrogen receptor degrader (SERD) and was first-in-class to be approved.[6] It works by binding to the estrogen receptor and destabilizing it, causing the cell's normal protein degradation processes to destroy it.[6]
Fulvestrant was approved for medical use in the United States in 2002.[7]
^Cite error: The named reference UKlabel2016 was invoked but never defined (see the help page).
^ ab"Faslodex- fulvestrant injection". DailyMed. 25 September 2020. Archived from the original on 11 December 2023. Retrieved 24 May 2024.
^"Faslodex". European Medicines Agency (EMA). 10 March 2004. Archived from the original on 19 October 2021. Retrieved 24 May 2024.
^ abcdDörwald FZ (4 February 2013). Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. pp. 486–. ISBN 978-3-527-64565-7. Archived from the original on 12 January 2023. Retrieved 20 May 2018.
^Lee CI, Goodwin A, Wilcken N (January 2017). "Fulvestrant for hormone-sensitive metastatic breast cancer". The Cochrane Database of Systematic Reviews. 1 (1): CD011093. doi:10.1002/14651858.CD011093.pub2. PMC 6464820. PMID 28043088.
^ abLai AC, Crews CM (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.
^"Fulvestrant". The American Society of Health-System Pharmacists. Archived from the original on 2 February 2017. Retrieved 8 January 2017.
Fulvestrant, sold under the brand name Faslodex among others, is an antiestrogenic medication used to treat hormone receptor (HR)-positive metastatic...
factor receptor 2-negative breast cancer when used in combination with fulvestrant. The US Food and Drug Administration (FDA) considers it to be a first-in-class...
ZB716, also known as fulvestrant-3-boronic acid, is a synthetic, steroidal, orally active antiestrogen which is under development for the treatment of...
success of fulvestrant led to efforts to discover and develop a parallel drug class of selective androgen receptor degraders (SARDs). Fulvestrant requires...
palbociclib is prescribed as a combination therapy with either letrozole or fulvestrant. Patients should also not consume CYP3A inhibitors or inducers while...
clinical trials: The phase III trial BELLE-2 compared buparlisib + fulvestrant with fulvestrant alone in patients with advanced or metastatic HER2-negative,...
alters a patient's hormones". In studies that compared fulvestrant plus abemaciclib to fulvestrant plus placebo in breast cancer patients, progression-free...
used to treat certain types of breast cancer. It is used together with fulvestrant. It is taken by mouth. It is marketed by Novartis. Common side effects...
efficacy and safety of inavolisib in combination with palbociclib and fulvestrant in patients that have PIK3CA-mutated, locally advanced or metastatic...
ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including...
loading dose include digoxin, teicoplanin, voriconazole, procainamide and fulvestrant. One or series of doses that may be given at the onset of therapy with...
tamoxifen is no longer effective. Fulvestrant is a SERD drug that acts by damaging and blocking estrogen receptors. Fulvestrant is currently only approved by...
or investigator’s choice of endocrine therapy (n=239), which included fulvestrant (n=166) or an aromatase inhibitor (n=73). Randomization was stratified...
cancer. In China, dalpiciclib is approved for use in combination with fulvestrant for treatment of HR-positive, HER2-negative recurrent, or metastatic...
combination with an aromatase inhibitor as initial endocrine-based therapy; or fulvestrant as initial endocrine-based therapy or following disease progression on...
failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce...
toremifen Other Anti-estrogens, including clomiphene, cyclofenil, and fulvestrant Myostatin modifying agents, including myostatin inhibitors (e.g., follistatin)...
conjugate E2-BSA in the absence or presence of the ERα/ERβ antagonist fulvestrant (ICI-182,780) and the GPER antagonist G-15. ER-X GPER (GPR30) Gq-mER...
options include those used in localized cancer, plus toremifene and fulvestrant, often used in combination with CDK4/6 inhibitors (palbociclib, ribociclib...
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