User:Mr. Ibrahem/Fulvestrant

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Mr. Ibrahem/Fulvestrant
Clinical data
Pronunciation/fʊlˈvɛstrənt/
fuul-VES-trənt
Trade namesFaslodex, others
Other namesICI-182780; ZD-182780; ZD-9238; 7α-[9-[(4,4,5,5,5-Pentafluoropentyl)-sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17β-diol
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: D
  • D
Routes of
administration		Intramuscular injection
Drug classAntiestrogen
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityLow[1]
Protein binding99%[1]
MetabolismHydroxylation, conjugation (glucuronidation, sulfation)[1]
Elimination half-lifeIMTooltip Intramuscular injection: 40–50 days[1]
Identifiers
  • (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
Chemical and physical data
FormulaC32H47F5O3S
Molar mass606.78 g·mol−1
3D model (JSmol)
  • FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCCC3Cc1c(ccc(O)c1)[C@H]2CC[C@]4([C@H]([C@@H]23)CC[C@@H]4O)C
  • InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1
  • Key:VWUXBMIQPBEWFH-WCCTWKNTSA-N
 ☒NcheckY (what is this?)  (verify)

Fulvestrant, sold under the brand name Faslodex among others, is a medication used to treat breast cancer.[2] Specifically it is used for hormone receptor (HR) positive cases.[4][5] It is given by injection into a muscle.[2]

Common side effects include nausea, diarrhea, headache, pain, hot flushes, cough, swelling, rash, and trouble sleeping.[2] Other side effects may include low white blood cells, low red blood cells, low platelets, infection, and liver problems.[5] It should not be used in pregnancy or breastfeeding.[5] It is a selective estrogen receptor degrader (SERD) which binds to estrogen receptor resulting in their destruction.[6]

Fulvestrant was approved for medical use in the United States in 2002 and Europe in 2004.[2][5] It is available as a generic medication.[3] In the United Kingdom it costs the NHS about £520 per dose of 2021.[3] This amount in the United States costs about 100 USD.[7]

References[edit]

  1. ^ a b c d Dörwald FZ (4 February 2013). Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. pp. 486–. ISBN 978-3-527-64565-7. Archived from the original on 10 October 2021. Retrieved 19 September 2021.
  2. ^ a b c d e f "Fulvestrant". The American Society of Health-System Pharmacists. Archived from the original on 2 February 2017. Retrieved 8 January 2021.
  3. ^ a b c BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 996. ISBN 978-0857114105.
  4. ^ "DailyMed - FULVESTRANT injection, solution". dailymed.nlm.nih.gov. Archived from the original on 12 December 2021. Retrieved 12 December 2021.
  5. ^ a b c d "Faslodex". Archived from the original on 19 October 2021. Retrieved 12 December 2021.
  6. ^ Lai AC, Crews CM (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.
  7. ^ "Faslodex Prices and Faslodex Coupons - GoodRx". GoodRx. Retrieved 12 December 2021.
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