Evidence map›Paper›PMID 28232670›Full record

ArticleLeukemia2017

Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo.

A Chaturvedi, L Herbst, S Pusch, L Klett, R Goparaju, D Stichel, S Kaulfuss, O Panknin, K Zimmermann, L Toschi and 19 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Leukemia, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 70 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
70citing papers in PubMed, 1 pooled it
10.8field-weighted citation impact, top 1% of its field
1 · What the graph read from 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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

70 citing papers in PubMed, 1 synthesis or guideline pooled it, 118 citations in OpenAlex.

  1. Pooled it
  2. Review
  3. Review
  4. Article
  5. Review
  6. Article
  7. Review
  8. Article
  9. Energy metabolism in health and diseases.Signal transduction and targeted therapy · 2025
    Review
  10. Article
  11. Review
  12. Review
  13. Review
  14. Metabolomics in oncology.Cancer reports (Hoboken, N.J.) · 2023
    Review
  15. Review
  16. Overview of Cancer Metabolism and Signaling Transduction.International journal of molecular sciences · 2022
    Review
  17. Review
  18. Targeting Energy Metabolism in Cancer Treatment.International journal of molecular sciences · 2022
    Review
  19. Article
  20. Review

10 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

29 authors at 6 institutions in 2 countries.

A ChaturvediDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
L HerbstClinical Cooperation Unit Molecular Hematology/Oncology, German Cancer Research Center (DKFZ) and Department of Internal Medicine V, University of Heidelberg, Heidelberg, Germany.
S PuschDepartment of Neuropathology, University of Heidelberg, Heidelberg, Germany.ORCID 0000-0002-3407-4249
L KlettResearch Group Genome Organization &Function, German Cancer Research Center (DKFZ) and Bioquant Center, Heidelberg, Germany.
R GoparajuDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
D StichelDepartment of Neuropathology, University of Heidelberg, Heidelberg, Germany.
S KaulfussDrug Discovery, Bayer Pharma AG, Berlin, Germany.
O PankninDrug Discovery, Bayer Pharma AG, Berlin, Germany.
K ZimmermannDrug Discovery, Bayer Pharma AG, Berlin, Germany.
L ToschiDrug Discovery, Bayer Pharma AG, Berlin, Germany.
R NeuhausDrug Discovery, Bayer Pharma AG, Berlin, Germany.
A HaegebarthDrug Discovery, Bayer Pharma AG, Berlin, Germany.
H RehwinkelDrug Discovery, Bayer Pharma AG, Berlin, Germany.
H Hess-StumppDrug Discovery, Bayer Pharma AG, Berlin, Germany.
M BauserDrug Discovery, Bayer Pharma AG, Berlin, Germany.
T BochtlerClinical Cooperation Unit Molecular Hematology/Oncology, German Cancer Research Center (DKFZ) and Department of Internal Medicine V, University of Heidelberg, Heidelberg, Germany.
E A StruysDepartment of Clinical Chemistry, VU University Medical Center, Amsterdam, The Netherlands.
A SharmaDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
A BakkaliDepartment of Clinical Chemistry, VU University Medical Center, Amsterdam, The Netherlands.
R GeffersGenome Analysis, Helmholtz Centre for Infection Research, Braunschweig, Germany.
M M Araujo-CruzDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
F TholDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
R GabdoullineDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
A GanserDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
A D HoDepartment of Internal Medicine V, University of Heidelberg, Heidelberg, Germany.
A von DeimlingDepartment of Neuropathology, University of Heidelberg, Heidelberg, Germany.
K RippeResearch Group Genome Organization &Function, German Cancer Research Center (DKFZ) and Bioquant Center, Heidelberg, Germany.
M HeuserDepartment of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hannover, Germany.
A KrämerClinical Cooperation Unit Molecular Hematology/Oncology, German Cancer Research Center (DKFZ) and Department of Internal Medicine V, University of Heidelberg, Heidelberg, Germany.
Bayer (Germany) · DEMedizinische Hochschule Hannover · DEGerman Cancer Research Center · DEAmsterdam UMC Location Vrije Universiteit Amsterdam · NLHeidelberg University · DEHelmholtz Centre for Infection Research · DE

Funding

European Research Council 638035
6 · The paper itself

Abstract

Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are frequently found in several human cancer types including acute myeloid leukemia (AML) and lead to the production of high levels of the oncometabolite (R)-2-hydroxyglutarate (R-2HG). Here we report the characterization of BAY1436032, a novel pan-mutant IDH1 inhibitor, both in vitro and in vivo. BAY1436032 specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells carrying IDH1R132H, IDH1R132C, IDH1R132G, IDH1R132L and IDH1R132S mutations. In addition, the compound impacts on DNA methylation and attenuates histone hypermethylation. Oral administration of BAY1436032 led to leukemic blast clearance, myeloid differentiation, depletion of leukemic stem cells and prolonged survival in two independent patient-derived xenograft IDH1 mutant AML mouse models. Together, BAY1436032 is highly effective against all major types of IDH1 mutant AML.

Indexed as

Aniline CompoundsAnimalsAntineoplastic AgentsBenzimidazolesCell Line, TumorDNA MethylationEnzyme InhibitorsGlutaratesHistone CodeHumansIsocitrate DehydrogenaseLeukemia, Myeloid, AcuteMethylationMiceMolecular Targeted TherapyMutationalpha-hydroxyglutarateAniline CompoundsAntineoplastic AgentsBAY 1436032BenzimidazolesEnzyme InhibitorsGlutaratesIDH1 protein, humanIsocitrate DehydrogenaseNeoplasm Proteins

Identifiers

PMID28232670
PMCPMC5629366
OpenAlexW2585000600

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

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.