Trial reportEuropean journal of drug metabolism and pharmacokinetics2020
Pharmacokinetic and Pharmacodynamic Studies of Elacestrant, A Novel Oral Selective Estrogen Receptor Degrader, in Healthy Post-Menopausal Women.
Trial report in European journal of drug metabolism and pharmacokinetics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 22 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 40 citations in OpenAlex.
- Elacestrant in hormone receptor-positive metastatic breast cancer: a post-hoc analysis.Exploration of targeted anti-tumor therapy · 2025Pooled it
- Selective estrogen receptor degraders and their effect on the breast cancer immune microenvironment.The Journal of clinical investigation · 2026Review
- Article
- Breast Cancer Brain Metastases: Current Understanding and Future Directions.Current oncology reports · 2026Review
- Disposition and Absolute Bioavailability of Oral Imlunestrant in Healthy Women: A Phase 1, Open-Label Study.Clinical pharmacology in drug development · 2025Article
- Post-marketing safety of elacestrant in breast cancer: a pharmacovigilance investigation using the FDA adverse event reporting system.BMC pharmacology & toxicology · 2025Article
- Imlunestrant Is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wild-Type and Mutant Breast Cancer.Cancer research · 2025Article
- Oral selective estrogen receptor degraders for breast cancer treatment: focus on pharmacological differences.Breast cancer research and treatment · 2025Review
- Breast cancer brain metastases genomic profiling identifies alterations targetable by immune-checkpoint and PARP inhibitors.NPJ precision oncology · 2024Article
- Breast Cancer Brain Metastasis: A Comprehensive Review.JCO oncology practice · 2024Review
- Novel Treatment Strategies for Hormone Receptor (HR)-Positive, HER2-Negative Metastatic Breast Cancer.Journal of clinical medicine · 2024Review
- Pharmacokinetic Analysis of [Molecular imaging and biology · 2024Article
- Pharmacological Profile of Novel Anti-cancer Drugs Approved by USFDA in 2022: A Review.Current molecular medicine · 2024Review
- Peering into the Brain's Estrogen Receptors: PET Tracers for Visualization of Nuclear and Extranuclear Estrogen Receptors in Brain Disorders.Biomolecules · 2023Article
- Pharmacology and pharmacokinetics of elacestrant.Cancer chemotherapy and pharmacology · 2023Article
- Available Systemic Treatments and Emerging Therapies for Breast Cancer Brain Metastases.Current treatment options in oncology · 2023Review
- Elacestrant: a new FDA-approved SERD for the treatment of breast cancer.Medical oncology (Northwood, London, England) · 2023Review
- Breast Cancer Brain Metastases: Achilles' Heel in Breast Cancer Patients' Care.Cancer treatment and research · 2023Article
- Accelerating drug development in breast cancer: New frontiers for ER inhibition.Cancer treatment reviews · 2022Review
- Advances in the management of breast cancer brain metastases.Neuro-oncology advances · 2021Review
Corrections and comments
- Erratum issued
Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesAdvanced estrogen receptor-positive (ER+) breast cancer is currently treated with endocrine therapy. Elacestrant is a novel, nonsteroidal, selective estrogen receptor degrader with complex dose-related ER agonist/antagonist activity that is being developed as a treatment option for ER+ breast cancer.
methodsTwo first-in-human phase 1 studies of elacestrant in healthy postmenopausal women (Study 001/Study 004) were conducted to determine its pharmacokinetic and pharmacodynamic profile as well as its safety and maximum tolerated dose.
resultsIn total, 140 postmenopausal subjects received at least one dose of study drug (114 received elacestrant and 26 received placebo). Single-ascending dose and multiple-ascending dose assessments showed that doses up to 1000 mg daily were safe and well tolerated, and the maximum tolerated dose was not reached. Oral administration of elacestrant had an absolute bioavailability of 10% and a mean half-life ranging from 27 to 47 h, reaching steady state after 5-6 days. Mean occupancy of the ER in the uterus after seven daily doses was 83% for 200 mg and 92% for 500 mg daily. The median ratio of elacestrant concentrations in the cerebral spinal fluid vs. plasma was 0.126% (500 mg dose) and 0.205% (200 mg dose). Most adverse events were related to the upper gastrointestinal tract.
conclusionsThese data demonstrate that elacestrant has good bioavailability when administered orally with a half-life that supports once-daily administration. Engagement of the ER and some ability to cross the blood-brain barrier was demonstrated in addition to an acceptable safety profile.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.