Elacestrant

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

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
Hormonal Receptor (HR)-Positive HER2 Negative Breast Cancer Patients Treated With Preoperative ELacestrant and PULSAR Radiotherapy	2025/06/05	NCT07005882	Phase 2	Not yet recruiting	Azienda Ospedaliero-Universitaria Careggi
A Rollover Protocol of Elacestrant, in Combination With Onapristone, for Patients With ER+, PR+, HER2- Advanced or Metastatic Breast Cancer	2025/04/22	NCT06938711	Phase 1	Withdrawn	Context Therapeutics Inc.
ctDNA Guided Adjuvant Treatment With Elacestrant: TBCRC-068	2025/04/11	NCT06923527	Phase 2	Not yet recruiting	Yale University
Immunologic Targeting of ESR1 Receptor for Hormone Receptor Expressing Metastatic Breast Cancer	2024/11/15	NCT06691035	Phase 1	Recruiting	H. Lee Moffitt Cancer Center and Research Institute
A First-in-Human Study of MEN2312 in Adults With Advanced Breast Cancer	2024/10/15	NCT06638307	Phase 1	Recruiting	Stemline Therapeutics, Inc.
Safety of Elacestrant in ER+/HER2- and ESR1 Mutations MBC	2024/08/09	NCT06544577	N/A	Recruiting	SciClone Pharmaceuticals
Elacestrant versus Standard Endocrine Therapy in Women and Men with Node-positive, Estrogen Receptor-positive, HER2-negative, Early Breast Cancer with High Risk of Recurrence - A Global, Multicenter, Randomized, Open-label Phase 3 Study (ELEGANT)	2025/03/11	2024-515445-42-00	Phase 3	Recruiting	Stemline Therapeutics Inc.
A randomized phase 3, double-blind, placebo-controlled study of elacestrant plus everolimus versus elacestrant in patients with estrogen receptor-positive/human epidermal growth factor receptor 2-negative, ESR1-mutated, advanced breast cancer progressing to endocrine therapy and CDK4/6 inhibitors - The ADELA study-	2024/11/26	2024-512926-27-00	Phase 3	Recruiting	Medica Scientia Innovation Research S.L., Medica Scientia Innovation Research S.L., Stemline Therapeutics Inc.
A PK Study Testing Single Oral Dose of Elacestrant in Subjects With Normal or Severely Impaired Hepatic Function	2023/11/13	NCT06126575	Phase 1	Completed	Stemline Therapeutics, Inc.
BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors	2023/11/07	NCT06120283	Phase 1	Recruiting	BeiGene

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
ORSERDU	Stemline Therapeutics, Inc.	72187-0101	ORAL	86 mg in 1 1	2/8/2023
ORSERDU	Stemline Therapeutics, Inc.	72187-0102	ORAL	345 mg in 1 1	2/8/2023

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
Orserdu	Stemline Therapeutics B.V.,Basisweg 10,1043 AP Amsterdam,Netherlands	Authorised	9/15/2023
Orserdu	Stemline Therapeutics B.V.,Basisweg 10,1043 AP Amsterdam,Netherlands	Authorised	9/15/2023

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
ORSERDU FILM-COATED TABLET 345 MG	CATALENT GREENVILLE, INC.	SIN17096P	TABLET, FILM COATED	345 MG	9/25/2024
ORSERDU FILM-COATED TABLET 86 MG	CATALENT GREENVILLE, INC.	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.

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