ArticleJournal of medicinal chemistry2016
Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 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.
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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.
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Who cites it
35 citing papers in PubMed, 81 citations in OpenAlex.
- Allosteric Induction of Estrogen Receptor Ligand Binding Domain Tetramerization by a Distinct Complete Estrogen Receptor Antagonist.ACS medicinal chemistry letters · 2026Article
- Hydrophobic tagging: A promising paradigm for targeted protein degradation.Cell insight · 2026Review
- Targeting estrogen receptor alpha in breast cancer for novel therapies resistance mechanisms and future directions.Discover oncology · 2025Review
- Biological and computer-aided evaluation of 3-methoxy-13α-estrone-16α-diphenylphosphine oxide as a new antiestrogenic agent.Scientific reports · 2025Article
- Boron-containing anticancer agents: a target-centric review of structure-activity relationships and clinical pipeline.Archives of pharmacal research · 2025Review
- Recent Development of Boron-Containing Small-Molecule Anticancer Agents.ACS pharmacology & translational science · 2025Review
- α-Triazolylboronic Acids: A Novel Scaffold to Target FLT3 in AML.ChemMedChem · 2025Article
- Analysis of the Main Directions in the Development of Mono and Combination Pharmacotherapy Acting on Hormonal Signaling Pathways of Breast Cancer According to the FDA Databases and Clinicaltrials.gov.Current medicinal chemistry · 2025Review
- Boronate-Based Bioactive Compounds Activated by Peroxynitrite and Hydrogen Peroxide.Redox biochemistry and chemistry · 2024Article
- New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives.Acta materia medica · 2024Article
- Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies.Acta pharmaceutica Sinica. B · 2024Review
- Review
- Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope.Journal of enzyme inhibition and medicinal chemistry · 2023Review
- Optimization of small molecule degraders and antagonists for targeting estrogen receptor based on breast cancer: current status and future.Frontiers in pharmacology · 2023Review
- Article
- Advances in the Development of Prodrugs as Selective Modulators of Estrogen Receptors.Journal of the Endocrine Society · 2022Review
- Design and synthesis of a novel ZB716-d6 as a stable isotopically labeled internal standard.Synthetic communications · 2022Article
- Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status.Drug design, development and therapy · 2022Review
- Recent developments in the medicinal chemistry of single boron atom-containing compounds.Acta pharmaceutica Sinica. B · 2021Review
- Fulvestrant-3-Boronic Acid (ZB716) Demonstrates Oral Bioavailability and Favorable Pharmacokinetic Profile in Preclinical ADME Studies.Pharmaceuticals (Basel, Switzerland) · 2021Article
Corrections and comments
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Authors and funding
16 authors at 2 institutions in 1 country.
Funding
Abstract
Orally bioavailable SERDs may offer greater systemic drug exposure, improved clinical efficacy, and more durable treatment outcome for patients with ER-positive endocrine-resistant breast cancer. We report the design and synthesis of a boronic acid modified fulvestrant (5, ZB716), which binds to ERα competitively (IC50 = 4.1 nM) and effectively downregulates ERα in both tamoxifen-sensitive and tamoxifen-resistant breast cancer cells. Furthermore, It has superior oral bioavailability (AUC = 2547.1 ng·h/mL) in mice, indicating its promising clinical utility as an oral SERD.
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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.