ELACESTRANT

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C30H38N2O2
Molecular Weight	458.6349
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCNCCC1=CC=C(CN(CC)C2=C(C=CC(OC)=C2)[C@@H]3CCC4=C(C3)C=CC(O)=C4)C=C1

InChI

InChIKey=SIFNOOUKXBRGGB-AREMUKBSSA-N

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

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf|https://www.ncbi.nlm.nih.gov/pubmed/28473534 | https://radiuspharm.com/pipeline/ | https://adisinsight.springer.com/drugs/800027755

Elacestrant (ER-306323 or RAD 1901 [6R)-6-(2-(N-(4-(2-(ethylamino)ethyl)benzyl)-N-ethylamino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride]) is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα). In ERpositive (ER ) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17β-estradiol mediated cell proliferation at concentrations inducing degradation of ERα protein mediated through proteasomal pathway. Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations. On January 27, 2023, the Food and Drug Administration (FDA) approved elacestrant (Orserdu, Stemline Therapeutics, Inc.) for postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Estrogen receptor alpha 134 Target ID: CHEMBL206 Gene ID: 2099.0 Gene Symbol: ESR1 Target Organism: Homo sapiens (Human) Sources: https://pubmed.ncbi.nlm.nih.gov/26164151\|https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	Antagonist 2849		48.0 nM [Unknown]

Conditions

Condition	Modality	Targets	Highest Phase	Product
ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	Primary		Approved 8583	ORSERDU Approved Use ORSERDU is an estrogen receptor antagonist indicated for: • treatment of postmenopausal women or adult men, with ERpositive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy Launch Date 2023

C_max

Value	Dose	Analyte	Population
119 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	345 mg single, oral dose: 345 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN
31.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
43.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
543 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

AUC

Value	Dose	Analyte	Population
2440 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	345 mg single, oral dose: 345 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN
774 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
627 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
8327 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

T_1/2

Value	Dose	Analyte	Population
40 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	345 mg single, oral dose: 345 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN
27.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
47.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
41.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

F_unbound

Value	Dose	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639s000lbl.pdf	345 mg single, oral dose: 345 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32661909/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELACESTRANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

Doses

Dose	Population	Adverse events
863 mg 1 times / day multiple, oral Highest studied dose Dose: 863 mg, 1 times / day Route: oral Route: multiple Dose: 863 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf#page=103 https://pubmed.ncbi.nlm.nih.gov/32661909/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: FED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf#page=103 https://pubmed.ncbi.nlm.nih.gov/32661909/	Disc. AE: Gastrointestinal disorder... AEs leading to discontinuation/dose reduction: Gastrointestinal disorder (grade 1-3) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf#page=103 https://pubmed.ncbi.nlm.nih.gov/32661909/
400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	Disc. AE: Musculoskeletal pain, Nausea... Other AEs: Musculoskeletal pain, Nausea... AEs leading to discontinuation/dose reduction: Musculoskeletal pain (1.7%) Nausea (1.3%) Nausea (3.4%) Musculoskeletal pain (1.7%) Increased ALT (1.3%) Other AEs: Musculoskeletal pain (grade 3-4, 7.2%) Nausea (grade 3-4, 1.7%) Vomiting (grade 3-4, 0.4%) Fatigue (grade 3-4, 0.8%) Decreased appetite (grade 3-4, 0.4%) Nausea (1.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/

AEs

AE	Significance	Dose	Population
Gastrointestinal disorder	grade 1-3 Disc. AE	863 mg 1 times / day multiple, oral Highest studied dose Dose: 863 mg, 1 times / day Route: oral Route: multiple Dose: 863 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf#page=103 https://pubmed.ncbi.nlm.nih.gov/32661909/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: FED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf#page=103 https://pubmed.ncbi.nlm.nih.gov/32661909/
Increased ALT	1.3% Disc. AE	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Nausea	1.3% Disc. AE	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Nausea	1.7%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Musculoskeletal pain	1.7% Disc. AE	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Musculoskeletal pain	1.7% Disc. AE	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Nausea	3.4% Disc. AE	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Decreased appetite	grade 3-4, 0.4%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Vomiting	grade 3-4, 0.4%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Fatigue	grade 3-4, 0.8%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Nausea	grade 3-4, 1.7%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/
Musculoskeletal pain	grade 3-4, 7.2%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/217639Orig1s000correctedlbl.pdf#page=4 https://pubmed.ncbi.nlm.nih.gov/35584336/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193 inhibitor 2438 inducer 440	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2E1 1060 CYP2A6 879 OAT3 747 CYP1A2 2153 OAT1 725 CYP2C19 2057 CYP2C8 1057 CYP3A 227 MATE1 415 CYP2B6 926 OATP1B1 1079 OCT2 779 MATE2-K 77 OCT1 620 OATP1B3 961 P-gp 1741 BCRP 910	CYP2A6 626	CYP2B6 669 CYP1A2 832 CYP2C19 329 CYP2A6 86 CYP3A 142

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2A6 911	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP3A 317	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	yes
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94 \| 100	yes	weak (co-administration study) Comment: Elacestrant increased rosuvastatin Cmax by 45% and AUC by 23% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94 \| 100

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	major
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94.0	minor
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94 \| 89	minor	yes (co-administration study) Comment: Itraconazole increased Cmax by 4.4-fold and AUC by 5.3-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 94 \| 89

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217639Orig1s000MultidisciplineR.pdf Page: 47.0

PubMed

Title	Date	PubMed
Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer.	2022-06	34694932
Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER+ Breast Cancer Patient-derived Xenograft Models.	2017-08-15	28473534

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage of ORSERDU is one 345 mg tablet taken orally, once daily, with food

Route of Administration: Oral

In Vitro Use Guide

In competitive receptor binding assays, the IC50 for RAD1901 on ERα was 48 versus 870 nmol/l for ERβ. For the E2 control, the IC50 values for ERα and ERβ were 0.4 and 0.3 nmol/l, respectively.

Name

Type

Language

ELACESTRANT

Official Name

English

elacestrant [INN]

Preferred Name

English

RAD1901

Code

English

ER-306323

Code

English

RAD-1901

Code

English

(2R)-2-(2-(ETHYL-((4-(2-(ETHYLAMINO)ETHYL)PHENYL)METHYL)AMINO)-4-METHOXY-PHENYL)TETRALIN-6-OL

Systematic Name

English

2-NAPHTHALENOL, 6-(2-(ETHYL((4-(2-(ETHYLAMINO)ETHYL)PHENYL)METHYL)AMINO)-4-METHOXYPHENYL)-5,6,7,8-TETRAHYDRO-, (6R)-

Systematic Name

English

ELACESTRANT [USAN]

Common Name

English

Elacestrant [WHO-DD]

Common Name

English

(6R)-6-(2-(ETHYL((4-(2- (ETHYLAMINO)ETHYL)PHENYL)METHYL)AMINO)-4-METHOXYPHENYL)- 5,6,7,8-TETRAHYDRONAPHTHALEN-2-OL

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1821