Elacestrant
drugOn this page
Also known as ER-306323RAD-1901Rad1901
Summary
Elacestrant (CHEMBL4297509) is an approved small-molecule antineoplastic agent (ATC L02BA04); indicated across 6 conditions including breast neoplasm and breast carcinoma; with CIViC clinical evidence for 13 variant-indication associations (e.g. ESR1 D538G in estrogen-receptor positive breast cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L02BA04
- Indications: 6 conditions
- Clinical trials: 35
- Precision-oncology evidence (CIViC): 13 variant–indication associations
- Chemistry: 458.6 Da · C30H38N2O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4297509 |
| Name | Elacestrant |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 23642301 |
| ChEBI | CHEBI:229213 |
| ATC | L02BA04 |
| Molecular formula | C30H38N2O2 |
| Molecular weight | 458.6 |
| InChIKey | SIFNOOUKXBRGGB-AREMUKBSSA-N |
SMILES: CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)[C@@H]3CCC4=C(C3)C=CC(=C4)O
IUPAC name: (6R)-6-[2-[ethyl-[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
ChEBI definition: A member of the class of tetralins that is 1,2,3,4-tetrahydronaphthalene which is substituted by hydroxy group at position 2 and by a 2-(ethyl{4-[2-(ethylamino)ethyl]benzyl}amino)-4-methoxyphenyl group at position 6R. It is a is an estrogen receptor degrader indicated for the treatment of 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.
Pharmacological roles (ChEBI): antineoplastic agent, estrogen receptor antagonist, anti-estrogen.
Also known as: Elacestrant, ER-306323, RAD-1901, Rad1901, RAD1901, ELACESTRANT
Parent form; salt/anhydrous children: CHEMBL4594273
Patent coverage: 454 distinct patent families (1,095 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 943 (86%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Estrogen receptor, Estrogen receptor beta.
Bioactivity
ChEMBL activities: 5 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ESR1 | 8.25 | IC50 | 5.6 | nM | CHEMBL_ACT_29237539 |
| ESR1 | 7.32 | IC50 | 48 | nM | CHEMBL_ACT_25651308 |
| ESR1 | 7.32 | IC50 | 48 | nM | CHEMBL_ACT_25905425 |
| ESR2 | 6.06 | IC50 | 870 | nM | CHEMBL_ACT_25651309 |
| ESR2 | 6.06 | IC50 | 870 | nM | CHEMBL_ACT_25905426 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
6 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| breast neoplasm | 3 | MONDO:0021100 | MONDO:0007254 |
| breast carcinoma | 3 | MONDO:0004989 | EFO:0000305 |
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| ductal breast carcinoma in situ | 2 | MONDO:0005023 | EFO:0000432 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 35.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 14 |
| PHASE1/PHASE2 | 8 |
| PHASE3 | 5 |
| PHASE1 | 5 |
| Not specified | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05512364 | PHASE3 | RECRUITING | Elacestrant for Treating ER+/HER2- Breast Cancer Patients With ctDNA Relapse (TREAT ctDNA) |
| NCT06382948 | PHASE3 | RECRUITING | Elacestrant + Everolimus in Patients ER+/HER2-, ESR1mut, Advanced Breast Cancer Progressing to ET and CDK4/6i. |
| NCT06492616 | PHASE3 | RECRUITING | A Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence |
| NCT07242352 | PHASE3 | RECRUITING | Marker - Adjusted Therapy Comparing Adjuvant Elacestrant With Standard Endocrine Treatment in Genomically and/or Clinically High-risk ER+/HER2- eBC |
| NCT03778931 | PHASE3 | COMPLETED | Phase 3 Trial of Elacestrant Versus Standard of Care for the Treatment of ER+/HER2- Advanced Breast Cancer |
| NCT05386108 | PHASE1/PHASE2 | RECRUITING | Study of Abemaciclib and Elacestrant in Participants With Brain Metastasis Due to ER+/HER-2- Breast Cancer |
| NCT05563220 | PHASE1/PHASE2 | RECRUITING | Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer |
| NCT05573126 | PHASE1/PHASE2 | RECRUITING | Phase 1/2 Study to Evaluate EP0062 as Monotherapy and in Combination in Patients With Advanced or Metastatic AR+/HER-2-/ER+ Breast Cancer |
| NCT05596409 | PHASE2 | ACTIVE_NOT_RECRUITING | ELACESTRANT in Women and Men With CDK4/6 Inhibitor-Naive Estrogen Receptor Positive, HER-2 Negative Metastatic Breast Cancer Study |
| NCT05982093 | PHASE2 | RECRUITING | Elacestrant With/Without Triptorelin in Premenopausal Women With Luminal Breast Cancer |
| NCT06062498 | PHASE2 | RECRUITING | Elacestrant vs Elacestrant Plus a CDK4/6 Inhibitor in Patients With ERpositive/HER2-negative Advanced or Metastatic Breast Cancer |
| NCT06075953 | PHASE2 | RECRUITING | DCIS: RECAST Trial Ductal Carcinoma In Situ: Re-Evaluating Conditions for Active Surveillance Suitability as Treatment |
| NCT06201234 | PHASE2 | RECRUITING | Evaluating the Addition of Elacestrant (Oral SERD) to Olaparib (PARP-inhibitor) in Patients With Advanced/Metastatic HR+/HER2- Breast Cancer |
| NCT06923527 | PHASE2 | RECRUITING | Circulating Tumor DNA |
| NCT07005882 | PHASE2 | NOT_YET_RECRUITING | Hormonal Receptor (HR)-Positive HER2 Negative Breast Cancer Patients Treated With Preoperative ELacestrant and PULSAR Radiotherapy |
| NCT07159451 | PHASE2 | RECRUITING | A Short-term Preoperative, Evaluating Activity and Safety of Elacestrant Monotherapy as Compared to Elacestrant + Ovarian Function Suppression (LHRH Agonist) in Premenopausal Patients With Stage I-II ER+/HER2- Breast Cancer |
| NCT07198724 | PHASE1/PHASE2 | RECRUITING | ERADICATE: A Phase Ib/II Study of Elacestrant Plus Trastuzumab Deruxtecan in Patients With CDK4/6 Inhibitor and Endocrine-resistant HR+/HER2-low or HER2-ultralow Metastatic Breast Cancer |
| NCT07209449 | PHASE2 | RECRUITING | A Study of Elacestrant Alone or in Combination With Abemaciclib in People With Endometrial Cancer |
| NCT07222215 | PHASE2 | RECRUITING | PhII Randomized CAPecitabine + ELAcestrant vs. Capecitabine Alone in ER+ Breast Cancer (CAPELA) |
| NCT07395336 | PHASE2 | RECRUITING | Elacestrant and Exemestane for Patients With Pretreated HR+/HER2- Metastatic Breast Cancer and [18F] FES-avid Lesions (COMBINE) |
| NCT07467772 | PHASE2 | RECRUITING | Ph 2 Elacestrant in ER Positive Uterine Sarcomas |
| NCT07612215 | PHASE1/PHASE2 | RECRUITING | Elacestrant in Advanced Triple Positive Breast Cancer |
| NCT00875420 | PHASE2 | COMPLETED | A Study to Evaluate the Effects of RAD1901 in the Treatment of Vasomotor Symptoms in Postmenopausal Women |
| NCT02653417 | PHASE2 | TERMINATED | Study to Evaluate the Safety and Efficacy of RAD1901 in Postmenopausal Women With Moderate to Severe Vasomotor Symptoms |
| NCT04791384 | PHASE1/PHASE2 | TERMINATED | Phase Ib/II Trial of Abemaciclib and Elacestrant in Patients With Brain Metastasis Due to HR+/Her2- Breast Cancer |
| NCT05618613 | PHASE1/PHASE2 | TERMINATED | Study of Elacestrant in Combination With Onapristone in Patients With Advanced or Metastatic Breast Cancer |
| NCT06938711 | PHASE1/PHASE2 | WITHDRAWN | A Rollover Protocol of Elacestrant, in Combination With Onapristone, for Patients With ER+, PR+, HER2- Advanced or Metastatic Breast Cancer |
| NCT06120283 | PHASE1 | RECRUITING | BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors |
| NCT06638307 | PHASE1 | RECRUITING | A First-in-Human Study of MEN2312 in Adults With Advanced Breast Cancer |
| NCT06691035 | PHASE1 | RECRUITING | Immunologic Targeting of ESR1 Receptor for Hormone Receptor Expressing Metastatic Breast Cancer |
| NCT02338349 | PHASE1 | COMPLETED | A Phase I, Multicenter, Open-Label, Multi-Part, Dose-escalation Study of RAD1901 in Postmenopausal Women With Advanced Estrogen Receptor Positive and HER2-Negative Breast Cancer |
| NCT02650817 | PHASE1 | COMPLETED | Phase IB Study to Evaluate RAD1901 on the Availability of Estrogen Receptor Binding Sites in Metastatic Breast Cancer |
| NCT04797728 | EARLY_PHASE1 | COMPLETED | Elacestrant in Preoperative Setting, a Window of Opportunity Study |
| NCT06544577 | Not specified | RECRUITING | Safety of Elacestrant in ER+/HER2- and ESR1 Mutations MBC |
| NCT07563595 | Not specified | NOT_YET_RECRUITING | Elacestrant in Patients With ER+ HER2- ESR1-mutated Locally Advanced or Metastatic Breast Cancer |
Clinical evidence (CIViC)
Variant × indication × effect (13 predictive associations from 13 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| ESR1 D538G | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12219 |
| ESR1 E380Q | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12224 |
| ESR1 L469V | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12225 |
| ESR1 L536H | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12226 |
| ESR1 L536P | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12227 |
| ESR1 L536Q | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12229 |
| ESR1 L536R | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12228 |
| ESR1 Mutation | Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID11443 |
| ESR1 S463P | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12230 |
| ESR1 Y537C | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12222 |
| ESR1 Y537D | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12223 |
| ESR1 Y537N | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12221 |
| ESR1 Y537S | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Elacestrant | CIViC A | EID12220 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: breast neoplasm, breast carcinoma, neoplasm, estrogen-receptor positive breast cancer
- Biomarker genes: ESR1