Evidence map›Paper›PMID 32529309›Full record

ArticlePharmaceutical research2020

Physiologically-Based Pharmacokinetic Predictions of the Effect of Curcumin on Metabolism of Imatinib and Bosutinib: In Vitro and In Vivo Disconnect.

Jeffry Adiwidjaja, Alan V Boddy, Andrew J McLachlan

Abstract read
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In one paragraph

Article in Pharmaceutical research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.6field-weighted citation impact, top 14% 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, 20 citations in OpenAlex.

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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

3 authors at 2 institutions in 1 country.

Jeffry AdiwidjajaSydney Pharmacy School, The University of Sydney, Sydney, NSW, 2006, Australia. andrew.mclachlan@sydney.edu.au.
Alan V BoddySchool of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, 5001, Australia.
Andrew J McLachlanSydney Pharmacy School, The University of Sydney, Sydney, NSW, 2006, Australia.
University of Sydney · AUCentre for Cancer Biology · AU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeThis study aimed to investigate the potential pharmacokinetic interactions between curcumin, imatinib and bosutinib, combining In Vitro and in silico methods.

methodsIn Vitro metabolism of imatinib and bosutinib were investigated in pooled human liver microsomes and recombinant CYP3A4 enzyme in the presence and absence of curcumin and curcumin glucuronide using an LC-MS/MS assay for N-desmethyl metabolites. A physiologically-based pharmacokinetic (PBPK) model for curcumin formulated as solid lipid nanoparticles (SLN) was constructed using In Vitro glucuronidation kinetics and published clinical pharmacokinetic data. The potential effects of curcumin coadministration on systemic exposures of imatinib and bosutinib were predicted in silico using PBPK simulations.

resultsCurcumin demonstrated potent reversible inhibition of cytochrome P450 (CYP)3A4-mediated N-demethylation of imatinib and bosutinib and CYP2C8-mediated metabolism of imatinib with inhibitory constants (k

conclusionA PBPK model for curcumin in a SLN formulation was successfully developed. Although curcumin possesses a strong In Vitro inhibitory activity towards CYP3A4 and CYP2C8 enzymes, its interactions with imatinib and bosutinib were unlikely to be of clinical importance due to curcumin's poor bioavailability.

Indexed as

Aniline CompoundsChromatography, High Pressure LiquidCurcuminCytochrome P-450 CYP2C8Cytochrome P-450 CYP3ACytochrome P-450 Enzyme InhibitorsDrug InteractionsGlucuronidesHumansHydroxylationImatinib MesylateMicrosomes, LiverModels, BiologicalModels, MolecularNitrilesPaclitaxelAniline CompoundsbosutinibCurcumincurcumin glucuronideCytochrome P-450 CYP2C8Cytochrome P-450 CYP3ACytochrome P-450 Enzyme InhibitorsGlucuronidesImatinib MesylateNitrilesPaclitaxelQuinolinesbosutinibcurcuminimatinibmodelling and simulationnatural product-drug interactionsphysiologically-based pharmacokinetic (PBPK)

Identifiers

PMID32529309
OpenAlexW3034310684

What OpenQuestion holds

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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.