ArticleJournal for immunotherapy of cancer2020
First-in-human phase I study of immunomodulatory E7046, an antagonist of PGE
Article in Journal for immunotherapy of cancer, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02540291 (An Open-Label Multicenter Phase 1 Study of E7046 in Subjects With Selected Advanced Malignancies), which is not on this map. Cited by 39 papers.
What it found
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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.
An Open-Label Multicenter Phase 1 Study of E7046 in Subjects With Selected Advanced Malignancies
Who cites it
39 citing papers in PubMed, 70 citations in OpenAlex.
- First-in-human phase I study of DT-9081, a selective EP4 receptor antagonist, in advanced solid tumors.Investigational new drugs · 2026Article
- Selective EP4 Receptor Antagonism for Osteoarthritis Pain: Emerging Evidence and Future Directions for KF-0210.Pain and therapy · 2026Review
- Review
- How CAR T cells can be shielded from prostaglandin E2 signaling to enhance their therapeutic activity.Molecular therapy. Oncology · 2026Article
- Harnessing myeloid cell plasticity for cancer therapy.Nature cancer · 2026Review
- Engineering with EP2/EP4 knockout and IL-15 transpresentation renders stem cell-derived NK cells self-persistent and resistant to PGE2 inhibition.Frontiers in immunology · 2026Article
- The Phenotypical and Functional Effect of PGE2 on Human Macrophages.European journal of immunology · 2025Article
- The Role of Tumor Microenvironment in Triple-Negative Breast Cancer and Its Therapeutic Targeting.Cells · 2025Review
- Blockade of the PGE2 Pathway Inhibits the Growth of PTEN-Deficient HNSCC Tumors.Molecular cancer therapeutics · 2025Article
- A phase I dose-escalation and expansion study of RMX1002, a selective E-type prostanoid receptor 4 antagonist, as monotherapy and in combination with anti-PD-1 antibody in advanced solid tumors.Investigational new drugs · 2025Article
- Immunoregulatory mechanisms of the arachidonic acid pathway in cancer.FEBS letters · 2025Review
- Marine Phytoplankton Bioactive Lipids and Their Perspectives in Clinical Inflammation.Marine drugs · 2025Review
- Myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment and their targeting in cancer therapy.Molecular cancer · 2025Review
- Polymer Nanoparticles Advancements for Gynecological Cancers.International journal of nanomedicine · 2025Review
- The impact of the tumor microenvironment on macrophages.Frontiers in immunology · 2025Review
- Prostaglandin ENature communications · 2024Article
- Remodeling the immune microenvironment for gastric cancer therapy through antagonism of prostaglandin E2 receptor 4.Genes & diseases · 2024Article
- EP2 and EP4 blockade prevents tumor-induced suppressive features in human monocytic myeloid-derived suppressor cells.Frontiers in immunology · 2024Article
- Docking for EP4R antagonists active against inflammatory pain.Nature communications · 2023Article
- Relevance of Phytochemical Taste for Anti-Cancer Activity: A Statistical Inquiry.International journal of molecular sciences · 2023Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
20 authors at 7 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundE7046 is a highly selective, small-molecule antagonist of the E-type prostanoid receptor 4 (EP4) for prostaglandin E2, an immunosuppressive mediator of the tumor immune microenvironment. This first-in-human phase 1 study assessed the safety, tolerability, pharmacokinetics, pharmacodynamics, maximum tolerated dose (MTD) and recommended phase 2 dose of E7046.
methodsThis first-in-human study enrolled 30 patients with advanced tumors of cancer types associated with high levels of myeloid infiltrates. E7046 was administered orally once-daily in sequential escalating dose cohorts (125, 250, 500, and 750 mg) with ≥6 patients per cohort. Tumor assessments were performed every 6 weeks. Paired tumor biopsies and blood samples, before and on treatment, were collected for pharmacokinetic and pharmacodynamic characterization of the treatment.
resultsNo dose-limiting toxicities were observed, and the MTD was not reached. E7046 had an elimination half-life (t
conclusionsIn this first-in-human study, E7046 administered orally once daily demonstrated manageable tolerability, immunomodulatory effects, and a best response of stable disease (≥18 weeks) in several heavily pretreated patients with advanced malignancies. The 250 and 500 mg doses are proposed for further development in the combination setting. TRIAL REGISTRATION NUMBER: NCT02540291.
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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.