Fulvestrant

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Fulvestrant chemical structure
Fulvestrant
Systematic (IUPAC) name
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
Identifiers
CAS number 129453-61-8
ATC code L02BA03
PubChem 104741
DrugBank APRD00654
Chemical data
Formula C32H47F5O3S 
Mol. weight 606.772 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 99%
Metabolism  ?
Half life 40 days
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?
Legal status
Routes Intramuscular injection

Fulvestrant, also known as ICI 182,780, and "Faslodex" is a drug treatment of hormone receptor positive metastatic breast cancer in post-menopausal 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.

Fulvestrant is marketed by AstraZeneca with the brand name Faslodex.

[edit] External links

[edit] References

  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. 2005 Jul 15;239(1-2):27-36.
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Sex hormones and related medications (primarily G03, also L02, H01C) edit
Progestogens:
(receptor)

Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone
Antiprogestogen: Mifepristone
Androgens:
(receptor)

Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, Testosterone, (see also anabolic steroids)
Antiandrogens: Bicalutamide, Cyproterone, Flutamide, Nilutamide, Spironolactone
Estrogens:
(receptor)

Chlorotrianisene, Dienestrol, Diethylstilbestrol, Estradiol, Estriol, Estrone, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate
Selective estrogen receptor modulator: Bazedoxifene, Clomifene, Fulvestrant, Raloxifene, Tamoxifen, Toremifene
Aromatase inhibitor: Aminogluthetimide, Anastrozole, Exemestane, Formestane, Letrozole, Vorozole
Gonadotropins:
(FSHR/LHCGR)

ovulation stim.: Clomifene, Urofollitropin
Antigonadotropins: Danazol, Gestrinone
GnRH:
(receptor)

Gonadotropin-releasing hormone agonist: Buserelin, Goserelin, Leuprorelin, Nafarelin, Triptorelin
Gonadotropin-releasing hormone antagonist: Histrelin, Abarelix
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