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Elacestrant

Generic Name
Elacestrant
Brand Names
Orserdu
Drug Type
Small Molecule
Chemical Formula
C30H38N2O2
CAS Number
722533-56-4
Unique Ingredient Identifier
FM6A2627A8
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
Related News

Samuraciclib Shows Promise in HR+ Breast Cancer Patients Without TP53 Mutations or Liver Metastases

• Carrick Therapeutics' CDK7 inhibitor samuraciclib demonstrated significantly extended progression-free survival in HR+ advanced breast cancer patients without TP53 mutations or liver metastases in two independent Phase 2 trials. • Patients without TP53 mutations showed median progression-free survival of 14.2 and 7.4 months across two trials, compared to just 1.8 months for patients with these mutations. • The biomarker-driven approach could provide a new treatment option for patients who develop resistance to standard CDK4/6 inhibitor therapy, with Phase 3 trials planned for 2026.

Orserdu Shows Promise in Real-World Breast Cancer Treatment, Highlighting Need for Access

Orserdu (elacestrant) demonstrates comparable or slightly better outcomes in real-world settings for HR-positive/HER2-negative advanced breast cancer patients with ESR1 mutations, as presented at the 2024 San Antonio Breast Cancer Symposium. Dr. Maxwell Lloyd emphasizes the critical need for improved access to innovative therapies and companion diagnostics, especially in underserved areas. The push for insurance coverage and equitable access to these treatments is vital for enhancing patient outcomes.

Arvinas Advances Vepdegestrant into Phase 3 Trials for Breast Cancer and Updates Pipeline Milestones

• Arvinas plans to initiate two Phase 3 trials in 2025 for vepdegestrant in ER+/HER2- metastatic breast cancer, one in the first-line setting with atirmociclib and another in the second-line setting with a CDK4/6 inhibitor. • Topline data from the Phase 3 VERITAC-2 monotherapy trial of vepdegestrant in second-line-plus ER+/HER2- metastatic breast cancer is anticipated in the first quarter of 2025. • Arvinas is set to present initial data from the Phase 1 trial of ARV-393 in B-cell lymphomas and file an IND application for a novel PROTAC KRAS G12D degrader in 2025. • Phase 1 trial with PROTAC LRRK2 degrader ARV-102 in patients with Parkinson’s disease has been initiated, with data expected to be presented in the first half of 2025.

Bayer's Elinzanetant Shows Promise in Reducing Hot Flashes for Breast Cancer Patients

• Elinzanetant met primary endpoints in the Phase III OASIS 4 trial, significantly reducing the frequency of moderate to severe vasomotor symptoms (VMS) in women undergoing endocrine therapy for breast cancer. • The study also achieved secondary endpoints, demonstrating a reduction in the severity of VMS, improvements in sleep disturbances, and enhanced menopause-related quality of life compared to placebo. • Elinzanetant is a dual neurokinin-1 and 3 receptor antagonist, representing a potential non-hormonal treatment option for VMS in breast cancer patients and women at high risk. • Bayer is advancing regulatory submissions for elinzanetant in the US, EU, and other global markets, with potential launch expected later this year, pending regulatory approvals.

SABCS 2024: Advances in Breast Cancer Treatment Highlighted

• Orserdu shows comparable real-world effectiveness to EMERALD trial results in HR-positive/HER2-negative advanced breast cancer with ESR1 mutations. • Older patients with early breast cancer may face a higher risk of immune-related side effects from immune checkpoint inhibitors. • Enhertu improves progression-free survival in HR-positive, HER2-low/ultralow metastatic breast cancer, regardless of endocrine resistance type. • Postoperative radiation therapy offers better quality of life and fewer side effects than exclusive endocrine therapy for older patients with stage 1 luminal-like breast cancer.

Imlunestrant Shows Promise in Advanced ER+/HER2- Breast Cancer Treatment

• Imlunestrant monotherapy significantly improved progression-free survival (PFS) in advanced breast cancer patients with ESR1 mutations compared to standard endocrine therapy. • The combination of imlunestrant and abemaciclib demonstrated a statistically significant improvement in PFS compared to imlunestrant alone, regardless of ESR1 mutation status. • The EMBER-3 trial results suggest imlunestrant, particularly in combination with abemaciclib, could offer a new all-oral targeted therapy option for pre-treated advanced breast cancer. • Safety data from the trial indicated that imlunestrant, both as a monotherapy and in combination, was generally well-tolerated, with manageable adverse events.

Real-World Data Suggests Elacestrant Offers Similar or Improved Outcomes in Advanced Breast Cancer

• A real-world analysis shows elacestrant demonstrates similar or slightly higher time to treatment discontinuation compared to the EMERALD trial. • The median real-world time to next treatment with elacestrant was 6.43 months, and time to treatment discontinuation was 4.6 months. • Patients with PIK3CA pathway alterations experienced worse outcomes with elacestrant, underscoring the need for precision medicine. • Most patients received elacestrant beyond the second line of treatment, with outcomes remaining consistent across different lines of therapy.

ADELA Phase III Trial Explores Elacestrant and Everolimus Combination for Advanced Breast Cancer

• The ADELA trial investigates elacestrant combined with everolimus for ER+/HER2- advanced breast cancer with ESR1 mutations, addressing endocrine therapy resistance. • Presented at SABCS 2024, the study aims to improve outcomes for patients who have progressed after standard first-line treatments. • The international, randomized, double-blind trial evaluates progression-free survival, overall survival, toxicity, and quality of life. • MEDSIR's involvement highlights its commitment to personalized oncology and overcoming tumor resistance, potentially leading to regulatory approval.

Novel Anti-Estrogen Therapies Expand Options for Advanced ER+ Breast Cancer

• Novel anti-estrogen therapies are poised to expand treatment options for patients with estrogen receptor (ER)-positive advanced breast cancer after CDK4/6 inhibitor therapy. • The phase 3 INAVO120 trial showed that inavolisib, combined with palbociclib and fulvestrant, significantly improved progression-free survival in patients with PIK3CA-mutated advanced breast cancer. • Updated INAVO120 findings presented at ASCO 2024 demonstrated a longer time to next-line treatment with the inavolisib combination compared to palbociclib and fulvestrant alone. • Researchers are focusing on identifying specific subgroups of patients who may benefit most from certain therapies or combinations, bringing a more personalized approach.
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