Overview
Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist. In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer. Elacestrant binds to estrogen receptor-alpha (ERα) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation. Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers. Unlike fulvestrant, another FDA-approved SERD, elacestrant is orally bioavailable.
Background
Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist. In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer. Elacestrant binds to estrogen receptor-alpha (ERα) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation. Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers. Unlike fulvestrant, another FDA-approved SERD, elacestrant is orally bioavailable.
Indication
Elacestrant is 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.
Associated Conditions
- Advanced Breast Cancer
- Metastatic Breast Cancer
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/05 | Phase 2 | Not yet recruiting | |||
2025/04/22 | Phase 1 | Withdrawn | |||
2025/04/11 | Phase 2 | Not yet recruiting | |||
2024/11/15 | Phase 1 | Recruiting | |||
2024/10/15 | Phase 1 | Recruiting | |||
2024/08/09 | N/A | Recruiting | SciClone Pharmaceuticals | ||
2025/03/11 | Phase 3 | Recruiting | |||
2024/11/26 | Phase 3 | Recruiting | Medica Scientia Innovation Research S.L., Medica Scientia Innovation Research S.L., Stemline Therapeutics Inc. | ||
2023/11/13 | Phase 1 | Completed | |||
2023/11/07 | Phase 1 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Stemline Therapeutics, Inc. | 72187-0101 | ORAL | 86 mg in 1 1 | 2/8/2023 | |
| Stemline Therapeutics, Inc. | 72187-0102 | ORAL | 345 mg in 1 1 | 2/8/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 9/15/2023 | ||
Authorised | 9/15/2023 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| ORSERDU FILM-COATED TABLET 345 MG | SIN17096P | TABLET, FILM COATED | 345 MG | 9/25/2024 | |
| ORSERDU FILM-COATED TABLET 86 MG | SIN17097P | TABLET, FILM COATED | 86 MG | 9/25/2024 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||