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Fulvestrant

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Title: Fulvestrant  
Author: World Heritage Encyclopedia
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Subject: Selective estrogen-receptor modulator, Estradiol, Conjugated estrogen, Estrone sulfate, Formestane
Collection: Antiestrogens, Hormonal Antineoplastic Drugs, Organofluorides, Steroids
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Fulvestrant

Fulvestrant
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
Pregnancy
category
  • D
Legal status
  • (Prescription only)
Routes of
administration
Intramuscular injection
Pharmacokinetic data
Protein binding 99%
Biological half-life 40 days
Identifiers
CAS Registry Number  Y
ATC code L02
PubChem CID:
IUPHAR/BPS
DrugBank  N
ChemSpider  N
UNII  Y
KEGG  N
ChEBI
ChEMBL  N
Synonyms ICI-182,780
Chemical data
Formula C32H47F5O3S
Molecular mass 606.772 g/mol
 N   

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 a complete estrogen receptor antagonist with no agonist effects, which in addition, accelerates the proteasomal degradation of the estrogen receptor.[1]

Contents

  • Clinical uses 1
  • Clinical trials 2
    • Metastatic or locally advanced breast cancer 2.1
  • NICE evaluation 3
  • Patent extension 4
  • References 5
  • External links 6

Clinical uses

Fulvestrant is a selective estrogen receptor degrader (SERD).[2] 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.[3]

Clinical trials

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.[4]

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.[5][6]

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 for the country's National Health Service

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 92 pence/day, and letrozole (Femara) costs £1.57/day- [7][8][9]

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.[10][11]

AstraZeneca has filed later patents. There is no generic Faslodex available.[12] A later patent for Faslodex expires in January 2021.[13]

References

  1. ^ Scott SM, Brown M, Come SE (2011). "Emerging data on the efficacy and safety of fulvestrant, a unique antiestrogen therapy for advanced breast cancer". Expert Opin Drug Saf 10 (5): 819–26.  
  2. ^ Wardell SE, Marks JR, McDonnell DP. (2011). "The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy.". Biochem Pharmacol. 82 (2). 
  3. ^ 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). 
  4. ^ Croxtall JD, McKeage K (2011). "Fulvestrant: a review of its use in the management of hormone receptor-positive metastatic breast cancer in postmenopausal women". Drugs 71 (3): 363–80.  
  5. ^ Valachis A, Mauri D, Polyzos NP, Mavroudis D, Georgoulias V, Casazza G (2010). "Fulvestrant in the treatment of advanced breast cancer: a systematic review and meta-analysis of randomized controlled trials". Crit. Rev. Oncol. Hematol. 73 (3): 220–7.  
  6. ^ Flemming J, Madarnas Y, Franek JA (2009). "Fulvestrant for systemic therapy of locally advanced or metastatic breast cancer in postmenopausal women: a systematic review". Breast Cancer Res. Treat. 115 (2): 255–68.  
  7. ^ UK Department of Health Commercial Medicines Unit Electronic Medicines Information Tool, London, 2015
  8. ^ UK’s NICE says no to AstraZeneca breast cancer drug Faslodex, The Pharma Letter, 10 November 2011
  9. ^ National Institute for Health and Clinical Excellence Guidance Breast cancer (metastatic) - fulvestrant
  10. ^ Patent Term Extensions The United States Patent and Trademark Office.
  11. ^ Determination of Regulatory Review Period for Purposes of Patent Extension; FASLODEX A Notice by the Food and Drug Administration on 04/17/2003
  12. ^ Generic Faslodex Availability, Drugs.COM
  13. ^ Pink Ribbon Blues: How Breast Cancer Culture Undermines Women's Health By Gayle A. Sulik, Oxford University Press (Oct. 2010)

External links

  • Faslodex product website
  • Faslodex prescribing information
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