ArticleACS medicinal chemistry letters2020
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 110 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.
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Who cites it
110 citing papers in PubMed, 180 citations in OpenAlex.
- Vorasidenib in IDH1- or IDH2-Mutant Low-Grade Glioma.The New England journal of medicine · 2023Trial
- Unique fluoroalkyl substituents: is there life after CFChemical science · 2026Review
- Exploring the landscape of targetable alterations in patients with glioblastoma.Nature reviews. Clinical oncology · 2026Review
- Ivosidenib and Vorasidenib Decrease Intratumoral 2-Hydroxyglutarate and Total Choline Levels in Patients with Lower-Grade Glioma: An In Vivo MR Spectroscopy Study.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Article
- Dedifferentiated Chondrosarcoma: Current Advances and Future Perspectives.Current treatment options in oncology · 2026Review
- Current Treatment Options for Adult Grade 2 IDH-mutant Diffuse Gliomas in the Vorasidenib Era: Patient Selection, Sequencing, and Practical Management.Current treatment options in oncology · 2026Review
- Reprogramming the immune suppressive tumor microenvironment in glioma enhances the efficacy of immune-mediated gene therapy.Molecular therapy. Oncology · 2026Article
- Halogenated anthraquinones in breast cancer therapy: Structural modifications targeting VEGF-related angiogenesis pathways.Journal of pharmaceutical analysis · 2026Review
- Review
- Fluorinated Derivatives of AG-881 for Positron Emission Tomography Detection of Mutated Isocitrate Dehydrogenase 1.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Molecularly Targeted Therapies in Oncology: Mechanisms, Resistance, and Combination Strategies.Molecules (Basel, Switzerland) · 2026Review
- A Case of IDH-Mutant Astrocytoma Harboring an IDH2 R172_H173delinsSN Variant.Neuropathology : official journal of the Japanese Society of Neuropathology · 2026Article
- Bayesian active learning-aided structure-based virtual screening reveals novel inhibitors of mutant IDH1.Molecular diversity · 2026Article
- Recent Advances in Targeted Therapies for Adult Gliomas.Current neurology and neuroscience reports · 2026Review
- Advancements in Drug Delivery Systems in Glioblastoma Therapy.International journal of molecular sciences · 2026Review
- Therapeutic targeting of chromatin alterations in leukemia and solid tumors.International journal of cancer · 2026Review
- State of the Art of IDH Inhibitors: Emerging Questions and Perspectives.Anti-cancer agents in medicinal chemistry · 2026Review
- A bibliometric review of triazine hybrids: synthesis, reactions, and applications spanning the last quarter-century (2000-2025).RSC advances · 2025Review
- Review
- From Inhibitors to PET: SAR-Based Development of [Journal of medicinal chemistry · 2025Article
50 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
28 authors at 3 institutions in 2 countries.
Funding
Abstract
Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes prevent the accumulation of the oncometabolite d-2-hydroxyglutarate (2-HG) and are under clinical investigation for the treatment of several cancers harboring an IDH mutation. Herein, we describe the discovery of vorasidenib (AG-881), a potent, oral, brain-penetrant dual inhibitor of both mIDH1 and mIDH2. X-ray cocrystal structures allowed us to characterize the compound binding site, leading to an understanding of the dual mutant inhibition. Furthermore, vorasidenib penetrates the brain of several preclinical species and inhibits 2-HG production in glioma tissue by >97% in an orthotopic glioma mouse model. Vorasidenib represents a novel dual mIDH1/2 inhibitor and is currently in clinical development for the treatment of low-grade mIDH glioma.
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.