Fulvestrant

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 Y
ATC code L02BA03
PubChem CID 104741
IUPHAR ligand 1015
DrugBank APRD00654
ChemSpider 94553 N
UNII 22X328QOC4 Y
KEGG D01161 N
ChEMBL CHEMBL1358 N
Synonyms 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
Chemical data
Formula C32H47F5O3S 
Mol. mass 606.772 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Fulvestrant, also known as ICI 182,780, 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 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.

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.[2]

External links

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 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). http://www.onclive.com/publications/contemporary-oncology/2011/spring-2011/the-longstanding-quest-for-a-better-endocrine-therapy-continues-high-dose-fulvestrant/.