Fulvestrant

Fulvestrant

CAS:129453-61-8
Synonyms: FASLODEX
Chemical Name:(7a,17b)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Molecular Fomular:C32H47F5O3S
Molecular Weight:606.77
Molecular Structure:
 
Density:1.201 g/cm3
Melting Point:104-106°C
Boiling Point:674.8 °C at 760 mmHg
Appearance:white powder
Usage:Antineoplastic (hormonal)

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.

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.

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.
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.

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-

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.
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