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| Clinical data | |
|---|---|
| Pronunciation | /ˌɛləˈsɛstrənt/ EL-ə-SES-trənt |
| Trade names | Orserdu |
| Other names | RAD-1901; ER-306323 |
| License data |
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| Routes of administration | By mouth |
| ATC code | |
| Legal status | |
| Legal status | |
| 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] |
| Identifiers | |
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| CAS Number | |
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| DrugBank | |
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| UNII | |
| KEGG | |
| ChEMBL | |
| PDB ligand | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.312.890 |
| Chemical and physical data | |
| Formula | C30H38N2O2 |
| Molar mass | 458.646 g·mol−1 |
| 3D model (JSmol) | |
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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]
- ^ 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.
- ^ 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.
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 "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.
