Elacestrant
Chemical compound / From Wikipedia, the free encyclopedia
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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]
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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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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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ECHA InfoCard | 100.312.890 |
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Formula | C30H38N2O2 |
Molar mass | 458.646 g·mol−1 |
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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]