Linked Life Data

15865849

Source:http://linkedlifedata.com/resource/pubmed/id/15865849

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2005-5-3
pubmed:abstractText
Fulvestrant is a pure antiestrogen that emerged from a systematic medicinal chemistry strategy of modification of long-chain alkyl substitutes in the 7a-position of estradiol. Fulvestrant has no uterotrophic effects on the immature or ovariectomized rat and blocks the agonistic effects of estradiol and tamoxifen in a dose-dependent manner. In in vivo and in vitro breast cancer models, fulvestrant has anticancer activity at least as good as tamoxifen and is superior to tamoxifen in some models. Fulvestrant requires intramuscular administration in a proprietary formulation of castor oil and alcohols. When fulvestrant binds to estrogen receptor monomers it inhibits receptor dimerization, activating function 1 (AF1) and AF2 are rendered inactive, translocation of receptor to the nucleus is reduced, and degradation of the estrogen receptor is accelerated. This results in pure antiestrogenic effects. There is substantial preclinical evidence that the nonsteroidal hormone-dependent mechanisms of estrogen receptor activation and regulation via growth factor receptors and their signal transduction pathways are important in the development of breast cancer hormonal resistance. Methods of exploiting the interactions between these nonsteroidal hormone-dependent mechanisms of resistance and hormonal agents such as fulvestrant are an active area for drug development and clinical investigation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1526-8209
pubmed:author
pubmed:issnType
Print
pubmed:volume
6 Suppl 1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S5-8
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
The history and mechanism of action of fulvestrant.
pubmed:affiliation
Department of Medicine, Stanford University, 875 Blake Wilbur Drive, Stanford, CA 94305-5826, USA. rcarlson@stanford.edu
pubmed:publicationType
Journal Article, Historical Article