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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/12/14 18:08:53」(JST)

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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 by down-regulating the estrogen receptor.^[1] It is administered as a once-monthly injection.

Clinical uses[edit]

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]

Clinical trials[edit]

Metastatic or locally advanced breast cancer[edit]

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]

NICE evaluation[edit]

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 £5.99, and letrozole (Femara) costs £84.86.^[6]^[7]^[8]

Patent extension[edit]

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]

References[edit]

^ 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).
^ Croxtall, J. D.; McKeage, K. (2011). "Fulvestrant". Drugs 71 (3): 363–380. doi:10.2165/11204810-000000000-00000. PMID 21319872. edit
^ 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)

External links[edit]

Faslodex product website
Faslodex prescribing information

UpToDate Contents

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1. 転移性ホルモン受容体陽性乳癌に対する治療アプローチ：内分泌療法 treatment approach to metastatic hormone receptor positive breast cancer endocrine therapy
2. 上皮性卵巣癌、卵管癌、または腹膜癌の再発に対する薬物療法：プラチナ製剤抵抗性癌 medical treatment for relapsed epithelial ovarian fallopian tubal or peritoneal cancer platinum resistant disease
3. 腫瘍学の最新情報 whats new in oncology
4. 男性における乳癌 breast cancer in men
5. 思春期早発症の治療 treatment of precocious puberty

English Journal

Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs.

Dolfi SC1, Jäger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.
Cancer letters.Cancer Lett.2014 Aug 1;350(1-2):52-60. doi: 10.1016/j.canlet.2014.04.009. Epub 2014 Apr 18.
The human homologue of mouse double minute 2 (MDM2) is overexpressed in tumors and contributes to tumorigenesis through inhibition of p53 activity. We investigated the effect of the anti-estrogen fulvestrant on MDM2 expression and sensitivity of estrogen receptor positive human breast cancer cell li
PMID 24747123

Effects of the oestrogen receptor antagonist Fulvestrant on expression of genes that affect organization of the epididymal epithelium.

Pereira MF1, Fernandes SA, Nascimento AR, Siu ER, Hess RA, Oliveira CA, Porto CS, Lazari MF.
Andrology.Andrology.2014 Jul;2(4):559-71. doi: 10.1111/j.2047-2927.2014.00219.x. Epub 2014 Apr 30.
The role of oestrogens in epididymal function is still unclear. Knockout of the oestrogen receptor ESR1 (Esr1(-/-) ) or treatment with the anti-oestrogen Fulvestrant affect epididymal milieu and sperm motility. We investigated the effect of in vivo treatment of rats with Fulvestrant on: (i) expressi
PMID 24782439

Randomised, phase II, placebo-controlled, trial of fulvestrant plus vandetanib in postmenopausal women with bone only or bone predominant, hormone-receptor-positive metastatic breast cancer (MBC): the OCOG ZAMBONEY study.

Clemons MJ1, Cochrane B, Pond GR, Califaretti N, Chia SK, Dent RA, Song X, Robidoux A, Parpia S, Warr D, Rayson D, Pritchard KI, Levine MN.
Breast cancer research and treatment.Breast Cancer Res Treat.2014 Jul;146(1):153-62. doi: 10.1007/s10549-014-3015-6. Epub 2014 Jun 13.
Biomarkers of bone turnover, including urine N-telopeptide (uNTx), have been used as surrogate measures of response to bone-targeted therapies. Vascular endothelial growth factor (VEGF) levels correlate with extent of bone metastases. We assessed whether vandetanib, an inhibitor of VEGF, epidermal g
PMID 24924416

Japanese Journal

各AI剤で忍容性が保てずFulvestrant 使用となった１例

大久保文恵,永井成勲,井上賢一,坪井美樹,黒住献,久保和之,戸塚勝理,林祐二,松本広志,武井寛幸,大庭華子,黒住昌史
The Kitakanto medical journal = 北関東医学 64(2), 230-230, 2014-05-01
NAID 120005429899

PS-219-3 閉経後ホルモン受容体陽性再発・転移性乳癌に対するFulvestrantの治療成績の検討(PS-219 乳腺内分泌療法,ポスターセッション,第114回日本外科学会定期学術集会)

由良昌大,嶋田昌彦,阿賀健一郎,原田宏輝,冠城拓示,山近大輔,武市悠,関博章,安井信隆,坂田道生,松本秀年
日本外科学会雑誌 115(臨時増刊号_2), 1012, 2014-03-05
NAID 110009871651

OP-094-2 閉経後女性ホルモン受容体陽性乳癌の再発治療におけるFulvestrantの位置づけ(OP-094 乳腺ホルモン・放射線・分子標的治療,一般演題,第114回日本外科学会定期学術集会)

露木茂,山口絢音,仙田典子,有本明
日本外科学会雑誌 115(臨時増刊号_2), 481, 2014-03-05
NAID 110009869537

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★リンクテーブル★

リンク元	「フルベストラント」「ICI 182」

「フルベストラント」

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	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	DB00947
ChemSpider	94553
UNII	22X328QOC4
KEGG	D01161
ChEMBL	CHEMBL1358
Synonyms	ICI-182,780
Chemical data
Formula	C32H47F5O3S
Mol. mass	606.772 g/mol
	SMILES FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCCC3Cc1c(ccc(O)c1)[C@H]2CC[C@]4([C@H]([C@@H]23)CC[C@@H]4O)C;
(what is this?) (verify);

　　[★]

英: fulvestrant
同: ICI 182
商: フェソロデックス
関: その他の腫瘍用薬

乳癌治療薬;エストロゲン受容体遮断

「ICI 182」

　　[★] フルベストラント, fulvestrant

[1] 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.

[2] 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).

[Croxtall_2011-3] Croxtall, J. D.; McKeage, K. (2011). "Fulvestrant". Drugs 71 (3): 363–380. doi:10.2165/11204810-000000000-00000. PMID 21319872. edit

[4] 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

[5] 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

[6] UK cost body rules against AstraZeneca cancer drug, Reuters, Nov 9, 2011

[7] UK’s NICE says no to AstraZeneca breast cancer drug Faslodex, The Pharma Letter, 10 November 2011

[8] National Institute for Health and Clinical Excellence Guidance Breast cancer (metastatic) - fulvestrant

[9] Patent Term Extensions The United States Patent and Trademark Office.

[10] Determination of Regulatory Review Period for Purposes of Patent Extension; FASLODEX A Notice by the Food and Drug Administration on 04/17/2003

[11] Generic Faslodex Availability, Drugs.COM

[12] Pink Ribbon Blues: How Breast Cancer Culture Undermines Women's Health By Gayle A. Sulik, Oxford University Press (Oct. 2010)

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fulvestrant