Elacestrant

Elacestrant
Clinical data
Pronunciation	/ˌɛləˈsɛstrənt/; EL-ə-SES-trənt
Trade names	Orserdu
Other names	RAD-1901; ER-306323
License data	US DailyMed: Elacestrant;
Routes of; administration	By mouth
ATC code	L02BA04 (WHO) ;
Legal status
Legal status	US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	~10%
Protein binding	>99%
Metabolism	Liver (major: CYP3A4, minor: CYP2A6, CYP2C9)
Elimination half-life	30–50 hours
Excretion	Feces (82%), urine (7.5%)
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 ;
ECHA InfoCard	100.312.890
Chemical and physical data
Formula	C30H38N2O2
Molar mass	458.646 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 a selective estrogen receptor degrader (SERD) used in the treatment of breast cancer.^[1]^[4] It is taken by mouth.^[1]^[4]

Elacestrant is an antiestrogen that acts as an antagonist of estrogen receptors, which are the biological targets of endogenous estrogens like estradiol.^[1] The most common side effects of elacestrant include body pain, nausea and vomiting, increased serum lipids, elevated liver enzymes, fatigue, decreased hemoglobin, raised creatinine, decreased appetite, diarrhea, headache, constipation, abdominal pain, and hot flashes.^[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.
^ fda.gov 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.

[Orserdu_FDA_label-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.

[FDA_20230127-2] "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.

[Orserdu-3] "Orserdu Product information". Union Register of medicinal products. 18 September 2023. Retrieved 1 October 2023.

[Orserdu_EPAR-4] "Orserdu EPAR". European Medicines Agency (EMA). 9 October 2023. Retrieved 9 October 2023.

[Orserdu_FDA_approval_letter-5] .gov Archived 2023-02-02 at the Wayback Machine 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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