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Elacestrant information


Elacestrant
Clinical data
Pronunciation/ˌɛləˈsɛstrənt/
EL-ə-SES-trənt
Trade namesOrserdu
Other namesRAD-1901; ER-306323
License data
  • US DailyMed: Elacestrant
Routes of
administration
By mouth
ATC code
  • L02BA04 (WHO)
Legal status
Legal status
  • US: ℞-only[1][2]
  • EU: Rx-only[3][4]
Pharmacokinetic data
Bioavailability~10%[1]
Protein binding>99%[1]
MetabolismLiver (major: CYP3A4, minor: CYP2A6, CYP2C9)[1]
Elimination half-life30–50 hours[1]
ExcretionFeces (82%), urine (7.5%)[1]
Identifiers
IUPAC name
  • (6R)-6-{2-[Ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol
CAS Number
  • 722533-56-4
PubChem CID
  • 23642301
DrugBank
  • DB06374
ChemSpider
  • 57583807
UNII
  • FM6A2627A8
KEGG
  • D11671
ChEMBL
  • ChEMBL4297509
PDB ligand
  • I0V (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID901045846 Edit this at Wikidata
ECHA InfoCard100.312.890 Edit this at Wikidata
Chemical and physical data
FormulaC30H38N2O2
Molar mass458.646 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)C3CCC4=C(C3)C=CC(=C4)O
InChI
  • InChI=1S/C30H38N2O2/c1-4-31-17-16-22-6-8-23(9-7-22)21-32(5-2)30-20-28(34-3)14-15-29(30)26-11-10-25-19-27(33)13-12-24(25)18-26/h6-9,12-15,19-20,26,31,33H,4-5,10-11,16-18,21H2,1-3H3/t26-/m1/s1
  • Key:SIFNOOUKXBRGGB-AREMUKBSSA-N

Elacestrant, sold under the brand name Orserdu, is an anticancer medication which is used in the treatment of breast cancer.[1][4] It is taken by mouth.[1][4]

Elacestrant is an antiestrogen, or an antagonist of the estrogen receptors, the biological targets of endogenous estrogens such as estradiol.[1] The most common side effects of elacestrant include musculoskeletal pain, nausea, increased cholesterol, elevated liver enzymes, increased triglycerides, fatigue, decreased hemoglobin, vomiting, increased ALT, increased AST, decreased sodium, increased creatinine, decreased appetite, diarrhea, headache, constipation, abdominal pain, hot flashes, and upset stomach.[2]

Elacestrant was approved for medical use in the United States in January 2023,[1][2][5][6] and in the European Union in September 2023.[3][7]

  1. ^ a b c d e f g h i j "Orserdu- elacestrant tablet, film coated". DailyMed. 8 February 2023. Archived from the original on 11 February 2023. Retrieved 11 February 2023.
  2. ^ a b c "FDA approves elacestrant for ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer". U.S. Food and Drug Administration (FDA). 27 January 2023. Archived from the original on 2 February 2023. Retrieved 1 February 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ a b "Orserdu Product information". Union Register of medicinal products. 18 September 2023. Retrieved 1 October 2023.
  4. ^ a b c "Orserdu EPAR". European Medicines Agency (EMA). 9 October 2023. Retrieved 9 October 2023.
  5. ^ https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2023/217639Orig1s000ltr.pdf Archived 2023-02-02 at the Wayback Machine Public Domain This article incorporates text from this source, which is in the public domain.
  6. ^ "Stemline Therapeutics Inc., a wholly owned subsidiary of Menarini Group, Receives Approval from U.S. FDA for Orserdu (elacestrant) as the First and Only Treatment Specifically Indicated for Patients with ESR1 Mutations in ER+, HER2- Advanced or Metastatic Breast Cancer". Radius (Press release). 31 January 2023. Archived from the original on 2 February 2023. Retrieved 1 February 2023.
  7. ^ "EC approves Menarini Group's Orserdu for advanced or metastatic breast cancer". PMLive. 21 September 2023. Retrieved 22 September 2023.

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