Fulvestrant

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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. mass	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

• Faslodex package insert and prescribing information

[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.

v • d • e Sex hormones and related agents (primarily G03, also L02, H01C) - human endogenous in CAPS
Progestogens: (receptor)	PROGESTERONE, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone Antiprogestogen: Mifepristone
Androgens: (receptor)	TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, (see also anabolic steroids) Antiandrogens: Bicalutamide, Cyproterone, Flutamide, Nilutamide, Spironolactone
Estrogens: (receptor)	ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, 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)	agonist: Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin antagonist: Abarelix, Cetrorelix, Ganirelix