Mr. Ibrahem/Elacestrant
Clinical data
Pronunciation/ˌɛləˈsɛstrənt/
EL-ə-SES-trənt
Trade namesOrserdu
Other namesRAD-1901; ER-306323
License data
Routes of
administration
By mouth
Legal status
Legal status
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
  • (6R)-6-{2-[Ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol
Chemical and physical data
FormulaC30H38N2O2
Molar mass458.646 g·mol−1
3D model (JSmol)
  • CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)C3CCC4=C(C3)C=CC(=C4)O
  • 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 a medication used to treat breast cancer.[1] Specifically it is used for ER-positive, HER2-negative, ESR1-mutated advanced disease that has failed other treatment.[1] It is used in women after menopause or in men.[1] It is taken by mouth.[1]

Common side effects include musculoskeletal pain, nausea, increased cholesterol, elevated liver enzymes, increased triglycerides, tiredness, decreased hemoglobin, decreased sodium, kidney problems, diarrhea, headache, constipation, abdominal pain, hot flashes, and upset stomach.[1] Use in pregnancy may harm the baby.[1] It may interact with medications that affect CYP3A4.[1] It works by blocking the action of estrogens.[1]

Elacestrant was approved for medical use in the United States in 2023.[1] In the United States it costs about 22,500 USD per month.[3]

References

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  1. ^ a b c d e f g h i j k l m n o p q r s "Orserdu- elacestrant tablet, film coated". DailyMed. 8 February 2023. Archived from the original on 11 February 2023. Retrieved 11 February 2023.
  2. ^ "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.   This article incorporates text from this source, which is in the public domain.
  3. ^ "Orserdu Prices, Coupons, Copay & Patient Assistance". Drugs.com. Archived from the original on 1 July 2023. Retrieved 14 May 2023.