Evidence map›Paper›PMID 31633365›Full record

ArticleMolecular pharmaceutics2019

Brivanib Exhibits Potential for Pharmacokinetic Drug-Drug Interactions and the Modulation of Multidrug Resistance through the Inhibition of Human ABCG2 Drug Efflux Transporter and CYP450 Biotransformation Enzymes.

Jakub Hofman, Ales Sorf, Dimitrios Vagiannis, Simona Sucha, Sarah Kammerer, Jan-Heiner Küpper, Si Chen, Lei Guo, Martina Ceckova, Frantisek Staud

Abstract read
In one paragraph

Article in Molecular pharmaceutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
2.0field-weighted citation impact, top 11% 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

19 citing papers in PubMed, 28 citations in OpenAlex.

  1. Article
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  5. Natural medicinal compounds target signal transduction pathways to overcome ABC drug efflux transporter-mediated multidrug resistance in cancer.Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy · 2023
    Review
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  15. A nontoxic fungal natural product modulates fin regeneration in zebrafish larvae upstream of FGF-WNT developmental signaling.Developmental dynamics : an official publication of the American Association of Anatomists · 2021
    Article
  16. Article
  17. Article
  18. Characterization of cytochrome P450s (CYP)-overexpressing HepG2 cells for assessing drug and chemical-induced liver toxicity.Journal of environmental science and health. Part C, Toxicology and carcinogenesis · 2021
    Article
  19. 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

10 authors at 3 institutions in 3 countries.

Jakub HofmanDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.ORCID 0000-0002-4285-7681
Ales SorfDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.
Dimitrios VagiannisDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.
Simona SuchaDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.ORCID 0000-0001-9190-458X
Sarah KammererInstitute of Biotechnology , Brandenburg University of Technology Cottbus-Senftenberg , Universitätsplatz 1 , 01968 Senftenberg , Germany.
Jan-Heiner KüpperInstitute of Biotechnology , Brandenburg University of Technology Cottbus-Senftenberg , Universitätsplatz 1 , 01968 Senftenberg , Germany.
Si ChenDivision of Biochemical Toxicology , National Center for Toxicological Research/U.S. FDA , Jefferson , Arkansas 72079 , United States.
Lei GuoDivision of Biochemical Toxicology , National Center for Toxicological Research/U.S. FDA , Jefferson , Arkansas 72079 , United States.
Martina CeckovaDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.
Frantisek StaudDepartment of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove , Charles University , Akademika Heyrovskeho 1203 , 500 05 Hradec Kralove , Czech Republic.
Charles University · CZBrandenburg University of Technology Cottbus-Senftenberg · DENational Center for Toxicological Research · US

Funding

Intramural FDA HHS FD999999
6 · The paper itself

Abstract

Brivanib, a promising tyrosine kinase inhibitor, is currently undergoing advanced stages of clinical evaluation for solid tumor therapy. In this work, we investigated possible interactions of this novel drug candidate with ABC drug efflux transporters and cytochrome P450 (CYP450) drug-metabolizing enzymes that participate in cancer multidrug resistance (MDR) and pharmacokinetic drug-drug interactions (DDIs). First, in accumulation experiments with various model substrates, we identified brivanib as an inhibitor of the ABCB1, ABCG2, and ABCC1 transporters. However, in subsequent combination studies employing 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2

Indexed as

AlanineAnimalsATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily G, Member 2BiotransformationCell LineCytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemDogsDrug InteractionsDrug Resistance, MultipleDrug Resistance, NeoplasmHumansMadin Darby Canine Kidney CellsNeoplasm ProteinsTriazinesABCG2 protein, humanAlanineATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily G, Member 2brivanibCytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemNeoplasm ProteinsTriazinesABC drug efflux transporterbrivanibcytochrome P450drug−drug interactionmultidrug resistance

Identifiers

PMID31633365
PMCPMC12379003
OpenAlexW2981440981

What OpenQuestion holds

Textmetadata
LicenceTDM
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.