Evidence map›Paper›PMID 38363422›Full record

ArticleEJNMMI research2024

Synthesis and preclinical evaluation of [

Antonia A Högnäsbacka, Alex J Poot, Christophe Plisson, Jonas Bergare, David R Bonsall, Stuart P McCluskey, Lisa A Wells, Esther Kooijman, Robert C Schuit, Mariska Verlaan and 6 more

Open access · goldAbstract read
In one paragraph

Article in EJNMMI research, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
1.3field-weighted citation impact, top 21% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. Article
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

16 authors at 4 institutions in 3 countries.

Antonia A HögnäsbackaDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands. a.hognasbacka@amsterdamumc.nl.ORCID http://orcid.org/0000-0002-5258-6619
Alex J PootDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Christophe PlissonInvicro LLC, London, W12 0NN, UK.
Jonas BergareEarly Chemical Development, Pharmaceutical Sciences, R&D AstraZeneca, Gothenburg, Sweden.
David R BonsallInvicro LLC, London, W12 0NN, UK.
Stuart P McCluskeyInvicro LLC, London, W12 0NN, UK.
Lisa A WellsInvicro LLC, London, W12 0NN, UK.
Esther KooijmanDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Robert C SchuitDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Mariska VerlaanDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Wissam BeainoDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Guus A M S van DongenDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Danielle J VugtsDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Charles S ElmoreEarly Chemical Development, Pharmaceutical Sciences, R&D AstraZeneca, Gothenburg, Sweden.
Jan PasschierInvicro LLC, London, W12 0NN, UK.
Albert D WindhorstDepartment Radiology and Nuclear Medicine, Vrije Universiteit Amsterdam, Amsterdam UMC, De Boelelaan 1117, 1081HV, Amsterdam, The Netherlands.
Amsterdam University Medical Centers · NLInvicro (United Kingdom) · GBAstraZeneca (Sweden) · SEAmsterdam Neuroscience · NL

Funding

H2020 Marie Skłodowska-Curie Actions 675417
6 · The paper itself

Abstract

backgroundMutations in the epidermal growth factor receptor (EGFR) kinase domain are common in non-small cell lung cancer. Conventional tyrosine kinase inhibitors target the mutation site in the ATP binding pocket, thereby inhibiting the receptor's function. However, subsequent treatment resistance mutations in the ATP binding site are common. The EGFR allosteric inhibitor, EAI045, is proposed to have an alternative mechanism of action, disrupting receptor signaling independent of the ATP-binding site. The antibody cetuximab is hypothesized to increase the number of accessible allosteric pockets for EAI045, thus increasing the potency of the inhibitor. This work aimed to gain further knowledge on pharmacokinetics, the EGFR mutation-targeting potential, and the influence of cetuximab on the uptake by radiolabeling EAI045 with carbon-11 and tritium.

results2-(5-fluoro-2-hydroxyphenyl)-2-((2-iodobenzyl)amino)-N-(thiazol-2-yl)acetamide and 2-(5-fluoro-2-hydroxyphenyl)-N-(5-iodothiazol-2-yl)-2-(1-oxoisoindolin-2-yl)acetamide were synthesized as precursors for the carbon-11 and tritium labeling of EAI045, respectively. [

conclusionsEAI045 was successfully labeled with tritium and carbon-11, and the in vivo results indicated [

Indexed as

EAI045EGFREpidermal growth factor receptorTKITyrosine kinase inhibitor

Identifiers

PMID38363422
PMCPMC10873260
OpenAlexW4391881271

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.