Orserdu (elacestrant)

To treat estrogen receptor-positive, human epidermal growth factor receptor 2-negative, ESR1-mutated, advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy Drug Trials Snapshot

FDA Approval: 1/27/2023

Research Synopsis

  • Orserdu (elacestrant) is a novel oral selective estrogen receptor degrader (SERD) designed for treatment of estrogen receptor-positive (ER+) breast cancer, particularly in cases where standard therapies have failed.
  • Clinical studies have shown elacestrant to be effective in improving progression-free survival (PFS) among patients with ER+/HER2-negative breast cancer who have previously undergone endocrine therapy.
  • The EMERALD trial, a Phase III study, demonstrated that elacestrant significantly extended PFS compared to standard endocrine treatments, with notable efficacy observed in patients with specific genetic mutations associated with treatment resistance.
  • Elacestrant exhibited strong antitumor activity in various laboratory models and showed effectiveness against breast cancer cells resistant to CDK4/6 inhibitors.
  • Pharmacokinetic studies indicated that elacestrant has a favorable safety profile and is well tolerated, with good oral bioavailability for daily administration.
  • Research highlighted the drug's potential to downregulate estrogen receptor activity effectively, making it a promising option for patients facing resistance to conventional therapies.
  • Ongoing research continues to explore the optimal use of elacestrant, alongside combination therapies, to improve treatment outcomes for patients with advanced breast cancer.
  • The development of elacestrant reflects a broader trend towards investigating next-generation SERDs, aiming to tackle challenges posed by hormone therapy resistance in ER+ breast cancer effectively.

Related articles

Research articles about Orserdu (elacestrant)

Orserdu (elacestrant)

Novel endocrine therapies: What is next in estrogen receptor positive, HER2 negative breast cancer?

London, UK

2 hours ago

1 Received

  • Endocrine therapy (ET) is a key treatment for hormone receptor positive breast cancer, focusing on blocking estrogen's effects since it helps cancer grow.
  • Challenges arise when the cancer stops responding to this therapy, often due to changes in how the cancer cells behave, requiring new treatment methods.
  • New oral treatments called selective estrogen receptor degraders (SERDs), like Elacestrant, are being tested and show promise for helping patients who don't benefit from standard therapies anymore.

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Investigational chemotherapy and novel pharmacokinetic mechanisms for the treatment of breast cancer brain metastases.

London, UK

2 hours ago

1 Received

  • * Current treatments for breast cancer brain metastases (BCBM) include surgery, radiation, and chemotherapy, but they often don't significantly improve survival and are mainly palliative.
  • * Recent advancements in chemotherapy have introduced new targeting agents and formulations, like PARP inhibitors and nanoparticles, which show promise and are being tested in ongoing clinical trials to improve treatment outcomes for BCBM.

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EMERALD: Phase III trial of elacestrant (RAD1901) vs endocrine therapy for previously treated ER+ advanced breast cancer.

London, UK

2 hours ago

1 Received

  • Elacestrant is a new oral medication that works as a selective estrogen receptor degrader (SERD) and shows promise for treating ER-positive/HER2-negative breast cancer in patients who have previously undergone hormone therapy.
  • The text discusses the EMERALD study, which is a large, international Phase III clinical trial that compares the effectiveness and safety of elacestrant against standard endocrine therapies like fulvestrant and aromatase inhibitors in patients with advanced breast cancer.
  • The main goals of the study are to assess progression-free survival in patients with specific mutations known to cause resistance to hormone therapy and in the overall patient population.

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Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors.

London, UK

2 hours ago

1 Received

  • * Elacestrant showed effective growth inhibition in various in vitro models and patient-derived xenografts exhibiting both acquired and de novo resistance to CDK4/6 inhibitors, regardless of ER mutation status.
  • * The findings suggest that even in resistant breast cancer cells, ER signaling remains crucial for tumor growth, indicating potential for elacestrant as a viable treatment option post-CDK4/6 inhibitor therapy.

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Investigation of binding mechanism and downregulation of elacestrant for wild and L536S mutant estrogen receptor-α through molecular dynamics simulation and binding free energy analysis.

London, UK

2 hours ago

1 Received

  • Selective estrogen receptor downregulators (SERDs) like Elacestrant (ELA) are emerging drugs for treating endocrine-resistant breast cancer, currently in phase II clinical trials.
  • Molecular docking studies show ELA binds to several helices of the estrogen receptor alpha (ERα), establishing crucial intermolecular interactions, including π···π interactions with specific amino acid residues.
  • Molecular dynamics simulations reveal that ELA forms a significant interaction with Asn532 in the wild-type ERα, essential for downregulating ERα, while this interaction is absent in the mutated L536S variant, indicating differences in drug efficacy due to genetic variations.

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The Future of ER+/HER2- Metastatic Breast Cancer Therapy: Beyond PI3K Inhibitors.

London, UK

2 hours ago

1 Received

  • - Most breast cancers are classified as estrogen receptor positive (ER+) and human epidermal growth factor receptor 2 negative (HER2-), and they are typically treated with hormone-based therapies that improve survival, especially in advanced cases.
  • - Unfortunately, many patients develop resistance to these hormone therapies, prompting research into new treatments such as CDK4/6 and PI3K inhibitors, along with novel drugs targeting other cancer-related pathways.
  • - New therapeutic strategies also focus on enhancing the immune response and targeting low levels of HER2 in ER+/HER2- cancers, leading to the development of innovative drugs currently in clinical trials.

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A phase 1b study evaluating the effect of elacestrant treatment on estrogen receptor availability and estradiol binding to the estrogen receptor in metastatic breast cancer lesions using F-FES PET/CT imaging.

London, UK

2 hours ago

1 Received

  • Elacestrant is an investigational oral drug designed to degrade estrogen receptors, tested in a phase 1b study to assess its impact on estrogen receptor availability in postmenopausal women with advanced breast cancer.* -
  • The study involved two groups of patients receiving different doses of elacestrant, and aimed to measure changes in tumor response through 16α-F-fluoro-17β-estradiol positron emission tomography (FES-PET) after 14 days of treatment.* -
  • Results showed a significant reduction in FES uptake in tumors (around 89%), but only a small overall response rate (11.1%) and varying levels of residual estrogen receptor presence, with some common

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Pharmacokinetic and Pharmacodynamic Studies of Elacestrant, A Novel Oral Selective Estrogen Receptor Degrader, in Healthy Post-Menopausal Women.

London, UK

2 hours ago

1 Received

  • Elacestrant is a new treatment being tested for advanced estrogen receptor-positive breast cancer, functioning as a selective estrogen receptor degrader with complex effects on estrogen signaling.
  • Two phase 1 studies involving 140 postmenopausal women were conducted to evaluate elacestrant’s pharmacokinetics (how the drug acts in the body), safety, and maximum tolerated dose, showing that doses up to 1000 mg were safe and well tolerated.
  • The findings indicate that elacestrant has good oral bioavailability, a suitable half-life for daily use, and effectively engages estrogen receptors while demonstrating an adequate safety profile.

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Correction to: Pharmacokinetic and Pharmacodynamic Studies of Elacestrant, A Novel Oral Selective Estrogen Receptor Degrader, in Healthy Post-Menopausal Women.

London, UK

2 hours ago

1 Received

  • The authors have identified inaccuracies in Table 2 of their previous work.
  • They have proposed corrections to address these errors.
  • The corrections aim to enhance the accuracy and reliability of the data presented in the table.

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Association of PET-based estradiol-challenge test for breast cancer progesterone receptors with response to endocrine therapy.

London, UK

2 hours ago

1 Received

  • Estrogen receptor (ER) testing for breast cancer is not always accurate in predicting how well patients will respond to endocrine therapy (ET), leading researchers to explore alternative methods.
  • In a clinical trial with 43 postmenopausal women suffering from advanced ER+ breast cancer, a one-day estradiol challenge was used to measure changes in tumor uptake of a specific progestin analog (FFNP).
  • The results showed that an increase in FFNP uptake post-challenge was present only in patients who benefited from ET, indicating that this method is a strong predictor of clinical response and linked to longer survival rates.

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Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer.

London, UK

2 hours ago

1 Received

  • The study focused on evaluating elacestrant, a new oral drug, for women with advanced breast cancer that is positive for estrogen receptors and negative for HER2, particularly those who have undergone extensive previous treatments.
  • It used a specific study design to determine the maximum safe dose and observed safety and effectiveness at a recommended dose of 400 mg taken daily.
  • Results showed an acceptable safety profile with mild side effects, and about 19.4% of patients had positive responses to treatment, especially among those with certain mutations, suggesting potential effectiveness for this patient group.

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Early Signs of Response to Elacestrant Seen in ER HER2 Breast Cancer.

London, UK

2 hours ago

1 Received

  • - A phase I trial was conducted to assess elacestrant, a selective estrogen receptor degrader, in patients with breast cancer.
  • - The study aimed to determine the safety, tolerability, and preliminary effectiveness of elacestrant for treating this type of cancer.
  • - Results from the trial could provide insights into a new treatment option for patients with breast cancer who have hormone receptor-positive tumors.

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Elacestrant in metastatic breast cancer: Is the "standard of care" meeting standard requirements?

London, UK

2 hours ago

1 Received

  • The EMERALD trial tested elacestrant, a new oral drug, against standard treatments in patients with advanced breast cancer that is hormone receptor positive and not HER2 overexpressed.
  • The trial's control group had limited options which may not provide an accurate comparison to elacestrant's effectiveness.
  • To better understand the results, it's important to analyze different patient subgroups based on previous treatments, but further research through another trial is necessary to get clear answers on elacestrant's advantages.

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Novel SERD Has PFS Edge against Breast Cancer.

London, UK

2 hours ago

1 Received

  • - The phase III EMERALD trial tested a new drug called elacestrant for patients with ER-positive/HER2-negative breast cancer.
  • - Elacestrant, an oral selective estrogen receptor degrader, showed a modest yet statistically significant improvement in progression-free survival.
  • - This trial focused on patients who had already received treatment with endocrine therapy and a CDK4/6 inhibitor.

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Elacestrant Improves Progression-Free Survival After Endocrine Therapy for Estrogen Receptor-Positive Metastatic Breast Cancer.

London, UK

2 hours ago

1 Received

  • * The trial showed that elacestrant significantly improved progression-free survival compared to the treatment chosen by the investigator.
  • * These patients had already experienced progression after earlier endocrine therapies, indicating a need for more effective treatment options.

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Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer.

London, UK

2 hours ago

1 Received

  • * The review explores the development and clinical pharmacokinetics of novel oral SERDs, including giredestrant and elacestrant, since 2015 using resources like PubMed and clinicaltrials.gov.
  • * The expert opinion suggests that these oral SERDs could enhance treatment for HR-positive breast cancer by offering better dosing, efficacy, and safety if confirmed in later-phase trials.

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Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role.

London, UK

2 hours ago

1 Received

  • Endocrine therapy (ET) is crucial for treating estrogen receptor-positive breast cancer, but resistance often develops in patients with metastatic breast cancer due to various signaling mechanisms.
  • Mutations in the estrogen receptor can lead to treatment resistance, posing challenges for therapies like aromatase inhibitors and selective estrogen receptor degraders (SERDs), as their role in combination treatments is not fully understood.
  • New oral SERDs, such as elacestrant, show promising results in clinical trials, highlighting the need for ongoing research to optimize treatment sequences and understand the genomic factors related to resistance in ER+ breast cancer.

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Elacestrant Prolongs Progression-Free Survival in Advanced Breast Cancer.

London, UK

2 hours ago

1 Received

  • Elacestrant showed a significant improvement in progression-free survival compared to standard endocrine therapy.
  • This means patients treated with elacestrant experienced longer periods without their cancer advancing.
  • The findings suggest that elacestrant may be a more effective treatment option for certain patients.

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Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial.

London, UK

2 hours ago

1 Received

  • Elacestrant is a new oral medication designed to treat ER-positive/HER2-negative advanced breast cancer, showing promising results in early studies.* -
  • In a phase III trial, patients were given either elacestrant or standard endocrine therapy, and results showed that elacestrant significantly prolonged progression-free survival (PFS) in the overall patient group and those with detectable mutations.* -
  • While elacestrant was associated with some side effects, such as nausea and a higher rate of treatment discontinuation compared to standard care, it was considered safe and effective for this patient population.*

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