Evidence map›Paper›PMID 37148323›Full record

ArticleCancer chemotherapy and pharmacology2023

Comparative biochemical kinase activity analysis identifies rivoceranib as a highly selective VEGFR2 inhibitor.

Seong Jang, Bill Strickland, Lynda Finis, Jeffrey J Kooijman, Janneke J T M Melis, Guido J R Zaman, Jan Van Tornout

Open access · hybridAbstract read
In one paragraph

Article in Cancer chemotherapy and pharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 2 of them syntheses that pooled it.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed, 2 pooled it
1.5field-weighted citation impact, top 18% 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

9 citing papers in PubMed, 2 syntheses or guidelines pooled it, 10 citations in OpenAlex.

  1. Pooled it
  2. Pooled it
  3. Review
  4. Article
  5. Review
  6. Review
  7. Article
  8. Article
  9. Small Molecule Tyrosine Kinase Inhibitors (TKIs) for Glioblastoma Treatment.International journal of molecular sciences · 2024
    Review
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

7 authors at 1 institution in 1 country.

Seong JangElevar Therapeutics, Fort Lee, NJ, USA. sjang@elevartherapeutics.com.ORCID http://orcid.org/0000-0002-4347-8712
Bill StricklandElevar Therapeutics, Fort Lee, NJ, USA.
Lynda FinisElevar Therapeutics, Fort Lee, NJ, USA.
Jeffrey J KooijmanOncolines B.V., Oss, The Netherlands.
Janneke J T M MelisOncolines B.V., Oss, The Netherlands.
Guido J R ZamanOncolines B.V., Oss, The Netherlands.
Jan Van TornoutElevar Therapeutics, Fort Lee, NJ, USA.
Institut de l’Elevage · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Vascular endothelial growth factor receptor 2 (VEGFR2), a key regulator of tumor angiogenesis, is highly expressed across numerous tumor types and has been an attractive target for anti-cancer therapy. However, clinical application of available VEGFR2 inhibitors has been challenged by limited efficacy and a wide range of side effects, potentially due to inadequate selectivity for VEGFR2. Thus, development of potent VEGFR2 inhibitors with improved selectivity is needed. Rivoceranib is an orally administered tyrosine kinase inhibitor that potently and selectively targets VEGFR2. A comparative understanding of the potency and selectivity of rivoceranib and approved inhibitors of VEGFR2 is valuable to inform rationale for therapy selection in the clinic. Here, we performed biochemical analyses of the kinase activity of VEGFR2 and of a panel of 270 kinases to compare rivoceranib to 10 FDA-approved kinase inhibitors ("reference inhibitors") with known activity against VEGFR2. Rivoceranib demonstrated potency within the range of the reference inhibitors, with a VEGFR2 kinase inhibition IC

Indexed as

Angiogenesis InhibitorsVascular Endothelial Growth Factor Receptor-2Cell Line, TumorCell ProliferationHumansProtein Kinase InhibitorsPyridinesVascular Endothelial Growth Factor AAngiogenesis InhibitorsapatinibProtein Kinase InhibitorsPyridinesVascular Endothelial Growth Factor AVascular Endothelial Growth Factor Receptor-2AngiogenesisComparative kinase activityOral kinase inhibitorRivoceranibVEGFR2

Identifiers

PMID37148323
PMCPMC10192158
OpenAlexW4372351205

What OpenQuestion holds

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LicenceCC BY
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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.