Fulvestrant
Fulvestrant is an anti-endocrine compound that exhibits anticancer chemotherapeutic benefit in the treatment of estrogen receptor (ER)-positive breast cancer. Fulvestrant causes degradation of ERs and downregulates ER expression, inhibiting cell growth. Fulvestrant also upregulates expression of UDP glucoronosyltransferase 1A4 (UGT1A4) in cancer cells. Additionally, fulvestrant exhibits some anti-hyperlipidemic benefit in clinical settings, as patients receiving it as a chemotherapeutic also exhibited lower serum levels of total cholesterol and LDL.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18925875
| Cas No. |
129453-61-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C32H47F5O3S |
| Formula Wt. |
606.77 |
| IUPAC Name |
(7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol |
| Solubility |
Soluble in ethanol (>200 mg/mL), DMSO (>20 mg/mL). Insoluble in water. DMF 20 mg/mL, chloroform. |
| Appearance |
White to off white powder |
Edavana VK, Penney RB, Yao-Borengasser A, et al. Fulvestrant up regulates UGT1A4 and MRPs through ERα and c-Myb pathways: a possible primary drug disposition mechanism. Springerplus. 2013 Nov 20;2:620. PMID: 24298433.
Krell J, Januszewski A, Yan K, et al. Role of fulvestrant in the management of postmenopausal breast cancer. Expert Rev Anticancer Ther. 2011 Nov;11(11):1641-52. PMID: 22050013.
Scott SM, Brown M, Come SE. Emerging data on the efficacy and safety of fulvestrant, a unique antiestrogen therapy for advanced breast cancer. Expert Opin Drug Saf. 2011 Sep;10(5):819-26. PMID: 21699443
Camerini A, Rondini M, Garrone O, et al. Fulvestrant treatment is associated with cholesterol plasma level reduction in hormone-receptor-positive metastatic breast cancer patients. Cancer Biol Ther. 2009 Aug;8(15):1450-5. PMID: 19556864.
