Fulvestrant
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| Systematic (IUPAC) name | |
| (7α,17β)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1,3,5(10)-triene-3,17-diol | |
| Clinical data | |
| Trade names | Faslodex |
| AHFS/Drugs.com | monograph |
| Pregnancy cat. | D |
| Legal status | Rx only |
| Routes | Intramuscular injection |
| Pharmacokinetic data | |
| Protein binding | 99% |
| Half-life | 40 days |
| Identifiers | |
| CAS number | 129453-61-8  |
| ATC code | L02BA03 |
| PubChem | CID 104741 |
| IUPHAR ligand | 1015 |
| DrugBank | APRD00654 |
| ChemSpider | 94553  |
| UNII | 22X328QOC4 |
| KEGG | D01161 |
| ChEMBL | CHEMBL1358 |
| Synonyms | 13-methyl-7-[9-( 4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]- 7,8,9,11,12,13,14,15,16,17-decahydro- 6H-cyclopenta[a]phenanthrene-3,17-diol |
| Chemical data | |
| Formula | C32H47F5O3S |
| Mol. mass | 606.772 g/mol |
| SMILES | eMolecules & PubChem |
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Fulvestrant (Faslodex, AstraZeneca) is a drug treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.[1] It is administered as a once-monthly injection.
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[edit] Clinical uses
Fulvestrant is a selective estrogen receptor down-regulator (SERD). Fulvestrant is indicated for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. The dosing schedule for fulvestrant remains under investigation in an attempt to optimize its effectiveness.[2]
[edit] Clinical trials
[edit] Metastatic or locally advanced breast cancer
Fulvestrant provided effective second-line therapy in this setting for postmenopausal women who had relapsed or progressed after previous endocrine therapy.[3]
In particular 4 clinical trials in this setting did show similar efficacy to the other hormonal agents (aromatase inhibitors and tamoxifen) with good tolerability profile. Fulvestrant had a lower incidence of joint disorders.[4][5]
[edit] NICE evaluation
The U.K. National Institute for Health and Clinical Excellence (NICE) said in 2011 that it found no evidence Faslodex was significantly better than existing treatments, so its widespread use would not be a good use of resources.
The first month's treatment of Faslodex, which starts with a loading dose, costs £1,044.82 ($1,666), and subsequent treatments cost £522.41 a month.
A month's supply of anastrozole (Arimidex), which is off patent, costs £5.99, and letrozole (Femara) costs £84.86.[6][7][8]
[edit] Patent extension
The original patent for Faslodex expired in October 2004. Drugs subject to pre-marketing regulatory review are eligible for patent extension, and for this reason AstraZeneca got an extension of the patent to December 2011.[9][10]
AstraZeneca has filed later patents. There is no generic Faslodex available.[11] A later patent for Faslodex expires in January 2021.[12]
[edit] References
- ^ S. Kansra, S. Yamagata, L. Sneade, L. Foster & N. Ben-Jonathan (2005). "Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release". Mol Cell Endocrinol 239 (1-2): 27–36. doi:10.1016/j.mce.2005.04.008. PMID 15950373.
- ^ Angela Mae Obermiller, PharmD; and Mehmet Sitki Copur, MD (2011). "The Longstanding Quest for a Better Endocrine Therapy Continues High-Dose Fulvestrant: Have We Found Its Effective Dose, Combination, Setting, or Sequence?". Contemporary Oncology 3 (1). http://www.onclive.com/publications/contemporary-oncology/2011/spring-2011/the-longstanding-quest-for-a-better-endocrine-therapy-continues-high-dose-fulvestrant/.
- ^ Croxtall, J. D.; McKeage, K. (2011). "Fulvestrant". Drugs 71 (3): 363–380. doi:10.2165/11204810-000000000-00000. PMID 21319872.
- ^ Fulvestrant in the treatment of advanced breast cancer: a systematic review and meta-analysis of randomized controlled trials. Valachis A, Mauri D, Polyzos NP, Mavroudis D, Georgoulias V, Casazza G. Crit Rev Oncol Hematol. 2010 Mar;73(3):220-7. Epub 2009 Apr 14. Review. PMID:19369092
- ^ Fulvestrant for systemic therapy of locally advanced or metastatic breast cancer in postmenopausal women: a systematic review. Flemming J, Madarnas Y, Franek JA. Breast Cancer Res Treat. 2009 May;115(2):255-68. Epub 2008 Aug 6. Review. PMID:18683044
- ^ UK cost body rules against AstraZeneca cancer drug, Reuters, Nov 9, 2011
- ^ UK’s NICE says no to AstraZeneca breast cancer drug Faslodex, The Pharma Letter, 10 November 2011
- ^ National Institute for Health and Clinical Excellence Guidance Breast cancer (metastatic) - fulvestrant
- ^ Patent Term Extensions The United States Patent and Trademark Office.
- ^ Determination of Regulatory Review Period for Purposes of Patent Extension; FASLODEX A Notice by the Food and Drug Administration on 04/17/2003
- ^ Generic Faslodex Availability, Drugs.COM
- ^ Pink Ribbon Blues: How Breast Cancer Culture Undermines Women's Health By Gayle A. Sulik, Oxford University Press (Oct. 2010)
[edit] External links
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