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Fulvestrant

Fulvestrant, sold under the trade name Faslodex among others, is used to treat hormone receptor positive breast cancer (breast cancer that depends on hormones such as estrogen to grow) in women who have experienced menopause (change of life; end of monthly menstrual periods) and whose breast cancer has worsened after they were treated with antiestrogen medications such as tamoxifen (Nolvadex). It works 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 palbociclib in women with disease progression after endocrine therapy. It is given by injection into a muscle.
Fulvestrant Suppliers list
Company Name: Lianyungang happen teng technology co., LTD
Tel: 15950718863
Email: wang666xt@163.com
Products Intro: Product Name:Fulvestrant
CAS:129453-61-8
Purity:98.00% Package:1kg,10kg,50kg,100kg
Company Name: TianYuan Pharmaceutical CO.,LTD
Tel: +86-755-23284190 13684996853
Email: sales@tianpharm.com
Products Intro: Product Name:Fulvestrant
CAS:129453-61-8
Purity:99% Package:10g 100g 200g 500g 1kg 5kg per barrel
Company Name: Capot Chemical Co.,Ltd.
Tel: +86 (0)571-855 867 18
Email: sales@capotchem.com
Products Intro: Product Name:Fulvestrant
CAS:129453-61-8
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Shenzhen Sendi Biotechnology Co.Ltd.
Tel: 0755-23311925 18102838259
Email: Abel@chembj.com
Products Intro: Product Name:Fulvestrant (Steroids)
CAS:129453-61-8
Purity:99% Package:2600/G
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Email: info@dakenchem.com
Products Intro: Product Name:Fulvestrant
CAS:129453-61-8
Purity:99% Package:100g,500g,1KG,10KG,100KG

Lastest Price from Fulvestrant manufacturers

  • Irsogladine maleate
  • US $1.00 / kg
  • 2019-05-13
  • CAS:129453-61-8
  • Min. Order: 1kg
  • Purity: 95%-99%
  • Supply Ability: 100kg
  • Fulvestrant
  • US $1.00 / kg
  • 2019-05-13
  • CAS:129453-61-8
  • Min. Order: 1kg
  • Purity: 95%-99%
  • Supply Ability: 100kg
Fulvestrant Basic information
Indications and Usage Mechanisms of Action Pharmacokinetics Adverse reactions
Product Name:Fulvestrant
Synonyms:(7a,17b)-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol;7A,17B-[9[(4,4,5,5,5-PENTAFLUOROPENTYL)SULFINYL]NONYL]ESTRA-1,3,5(10)-TRIENE-3,17-DIOL;(7alpha,17beta)-nonyl);estra-1,3,5(10)-triene-3,17-diol,7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl);Fulvtrant;7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]- (7α,17β)-estra-1,3,5(10)-triene-3,17-diol;(7a,17b)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol Fulvestrant ICI 182,780;Fulvestrant for system suitability
CAS:129453-61-8
MF:C32H47F5O3S
MW:606.77
EINECS:642-998-6
Product Categories:FASLODEX;Anti-cancer&immunity;-;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Nuclear Receptors;Chiral Reagents;Steroids;Sulfur & Selenium Compounds
Mol File:129453-61-8.mol
Fulvestrant Structure
Fulvestrant Chemical Properties
Melting point 104-106°C
storage temp. 2-8°C
solubility DMSO: >5mg/mL
form powder
InChIKeyVWUXBMIQPBEWFH-WCCTWKNTSA-N
CAS DataBase Reference129453-61-8(CAS DataBase Reference)
Safety Information
WGK Germany 3
RTECS KG7623000
Hazardous Substances Data129453-61-8(Hazardous Substances Data)
MSDS Information
Fulvestrant Usage And Synthesis
Indications and UsageFulvestrant is a muscle injection drug developed by the company AstraZeneca and is suitable for treating postmenopausal women with estrogen receptor-positive metastasized breast cancer whose condition continued to worsen despite antiestrogen treatment. Fulvestrant is the only antiestrogen drug that can be widely clinically used following unsuccessful tamoxifen treatment. This drug is a type of endocrine therapy, so it will not cause any adverse effects commonly seen in chemotherapy, giving it relatively good patient compliance. Multiple clinical trials have found that 250mg Fulvestrant is effective and consistently safe as a second line of treatment for advanced breast cancer.
Mechanisms of ActionMany breast cancer cells contain estrogen receptors (ER), so estrogen stimulates breast cancer growth. Fulvestrant is a steroid estrogen receptor antagonist, and its chemical structure is similar to estradiol, except that its 7α position contains a linking group. Fulvestrant is a 17β-estradiol alkylamine analogue, and it binds with, prevents, and decreases ER to inhibit the estrogen signal transduction pathway. It binds competitively with ER, has a similar affinity with ER as estrogen, and inhibits gene activation stimulated by estrogen, thus affecting necessary estrogen-related processes in cell circulation. Its fulvastans have a similar affinity with ER as estrogen and is 100 times that of tamoxifen.
PharmacokineticsFulvestrant has a relatively poor oral bioavailability, so it is commonly injected into the muscle with lipids as excipients. In an open, random and multicenter study on postmenopausal women with advanced breast cancer, one 5ml or 2 2.5ml dosages containing 250mg were injected, and their pharmacokinetics and poisonous side effects did not differ greatly, while its blood concentration was dose-dependent and had individual differences. In the 7-day treatment period, serum LH, FSH or SBHG levels did not change significantly. This drug does not pass through the blood-brain barrier and will not cause side effects such as vasomotor symptoms.
Adverse reactionsFulvestrant causes relatively fewer side effects, including brief vaginal bleeding, body odor change, and sleepwalking. There have not been any reports of effects such as vaginal dryness, weight gain, blood clotting abnormalities, thrombus formation and libido change, and characteristics such as facial flushing and sweating are not affected. A small-scale stage III clinical trial on 19 women with metastasized breast cancer who used this drug showed that its clinical efficacy was 67% and there were no serious safety issues. It showed that continuous monthly injections were crucial and that it was well-tolerated, with only slight swelling and paint at injection site, while facial flushing, uterine lining thickness, sex hormone binding globulin levels, follicle stimulating hormones levels, and luteinizing hormone levels all showed no change.
DescriptionFulvestrant was launched in the US as a novel once monthly injectable steroidal estrogen antagonist for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following estrogen therapy. This 7a-alkylsulphinyl derivative of estradiol can be prepared in 10 steps from 6,7- didehydro-19-nor-testosterone by successive conjugate addition of the organocuprate derived from O-protected 9-bromononan-l-o1 followed by aromatization of the resulting enone, then activation of the protected primary alcohol, substitution with 4,4,5,5,5- pentafluoropentanthiol and oxidation to the sulfoxide. Fulvestrant is the first “pure” estrogen antagonist from a novel class known as selective estrogen receptor down regulators (SERDs). It binds to the estrogen receptor (ER), with affinity close to that of estradiol and 100 fold greater than that of tamoxifen (a partial estrogen antagonist), preventing estrogen-stimulated gene activation, thereby interfering with the estrogenrelated processes essential for cell-cycle completion. Fulvestrant also appears to downregulate the ER by 80-90% often to non detectable level both in vitro and in vivo. In comparison to tamoxifen, fulvestrant is devoid of systemic estrogenic activity, it displays no uterotrophic activity and is able to block the uterine stimulation of estradiol or tamoxifen. Furthermore, fulvestrant completely blocks the cell growth in tamoxifen-resistant breast cancer cell-lines and prevents growth of tamoxifen resistant tumor in mice. In clinical trials, it was also shown that fulvestrant is comparable to anastrozole (a third generation aromatase inhibitor) both in efficacy and tolerability in postmenopausal women with tamoxifen-resistant advanced breast cancers.
Chemical PropertiesWhite or almost white powder.
OriginatorAstra Zeneca (UK)
UsesA novel steroidal estrogen antagonist reported to lack any partial agonist activity. Antineoplastic (hormonal).
Usesantiestrogen
DefinitionChEBI: A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.
Brand nameFaslodex (AstraZeneca).
General DescriptionFulvestrant, 7α-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17β-diol (Faslodex), is an antagonist structurally based onthe estradiol structure, with a long, substituted alkyl chainattached at the 7α-position of the steroid skeleton. Whenbound to the ERs, this alkyl chain induces a conformationof the receptor distinctive from that formed upon estradiolor tamoxifen binding, preventing agonist action.Fulvestrant is a pure antagonist at both ERαand ERβandan ER downregulator (stimulates degradation of the ER),completely lacking the agonist activity that is seen with tamoxifenor raloxifene. The different pharmacological profileof fulvestrant allows the use of this agent in womenwho have had disease progression after prior antiestrogentherapy (typically tamoxifen), providing an alternative toaromatase inhibitors.
Biological ActivityA high affinity estrogen receptor antagonist (IC 50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo . Also high affinity agonist at the membrane estrogen receptor GPR30.
Fulvestrant Preparation Products And Raw materials
Tag:Fulvestrant(129453-61-8) Related Product Information
FULVESTRANT(USAN) DIAMYL SULFOXIDE OCTADECYLMETHYLSULFIDE 4-tetradecylphenol 4-n-Octadecylphenol DODECYL METHYL SULFOXIDE 1-PHENYLOCTADECANE OCTADECYL METHYL SULFOXIDE ETHYL OCTADECYL SULFIDE ECT 4,4,5,5,5-Pentafluoro-1-pentanethiol DI-N-BUTYL SULFOXIDE p-hexadecylphenol 4-DODECYLPHENOL N-NONADECYLBENZENE DECYL METHYL SULFOXIDE 16-MERCAPTO-1-HEXADECANOL Fulvestrant