Elacestrant
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Pronunciation | /ˌɛləˈsɛstrənt/ EL-ə-SES-trənt |
Trade names | Orserdu |
Other names | RAD-1901; ER-306323 |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | ~10%[1] |
Protein binding | >99%[1] |
Metabolism | Liver (major: CYP3A4, minor: CYP2A6, CYP2C9)[1] |
Elimination half-life | 30–50 hours[1] |
Excretion | Feces (82%), urine (7.5%)[1] |
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Elacestrant, sold under the brand name Orserdu, is an
Elacestrant is an
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]
Medical uses
Elacestrant is
Pharmacology
Pharmacodynamics
Elacestrant is an
Pharmacokinetics
The
History
Efficacy was evaluated in EMERALD (NCT03778931), a randomized, open-label, active-controlled, multicenter trial that enrolled 478 postmenopausal women and men with ER-positive, HER2-negative advanced or metastatic breast cancer of which 228 participants had ESR1 mutations.[2] Participants were required to have disease progression on one or two prior lines of endocrine therapy, including one line containing a CDK4/6 inhibitor.[2] Eligible participants could have received up to one prior line of chemotherapy in the advanced or metastatic setting.[2] Participants were randomized (1:1) to receive elacestrant 345 mg orally once daily (n=239) or investigator’s choice of endocrine therapy (n=239), which included fulvestrant (n=166) or an aromatase inhibitor (n=73).[2] Randomization was stratified by ESR1 mutation status (detected vs. not detected), prior treatment with fulvestrant (yes vs. no), and visceral metastasis (yes vs. no).[2] ESR1 mutational status was determined by blood circulating tumor deoxyribonucleic acid (ctDNA) using the Guardant360 CDx assay and was limited to ESR1 missense mutations in the ligand binding domain.[2]
The FDA granted the application for elacestrant priority review and fast track designations.[2]
Research
It is a
References
- ^ a b c d e f g h i j k l m n o p q r "Orserdu- elacestrant tablet, film coated". DailyMed. 8 February 2023. Archived from the original on 11 February 2023. Retrieved 11 February 2023.
- ^ a b c d e f g h i j k "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.
- ^ a b "Orserdu Product information". Union Register of medicinal products. 18 September 2023. Retrieved 1 October 2023.
- ^ a b c d "Orserdu EPAR". European Medicines Agency (EMA). 9 October 2023. Retrieved 9 October 2023.
- ^ https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2023/217639Orig1s000ltr.pdf Archived 2023-02-02 at the Wayback Machine This article incorporates text from this source, which is in the public domain.
- ^ "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.
- ^ "EC approves Menarini Group's Orserdu for advanced or metastatic breast cancer". PMLive. 21 September 2023. Retrieved 22 September 2023.
- PMID 35923930.
- ^ Clinical trial number NCT03778931 for "Phase 3 Trial of Elacestrant vs. Standard of Care for the Treatment of Patients With ER+/HER2- Advanced Breast Cancer" at ClinicalTrials.gov
- ^ PMID 26162914.
- ^ PMID 26164151.