Evidence map›Paper›PMID 38642299›Full record

ArticleEuropean journal of drug metabolism and pharmacokinetics2024

Uridine 5'-Diphospho-glucuronosyltransferase 1A3 (UGT1A3) Prediction of Hepatic Clearance of Organic Anion Transporting Polypeptide 1B3 (OATP1B3) Substrate Telmisartan by Glucuronidation Using In Vitro-In Vivo Extrapolation (IVIVE).

Ewelina Gabor-Worwa, Anna Kowal-Chwast, Nilesh Gaud, Dawid Gogola, Peter Littlewood, Marek Smoluch, Krzysztof Brzózka, Kamil Kus

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Article in European journal of drug metabolism and pharmacokinetics, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed
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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

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

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

8 authors at 2 institutions in 1 country.

Ewelina Gabor-WorwaDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland. ewelina.gabor-worwa@ryvu.com.ORCID http://orcid.org/0009-0008-5465-0873
Anna Kowal-ChwastDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Nilesh GaudDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Dawid GogolaDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Peter LittlewoodDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Marek SmoluchDepartment of Analytical Chemistry and Biochemistry, Faculty of Materials Science and Ceramics, AGH University of Krakow, Mickiewicza 30 Street, 30-059, Krakow, Poland.
Krzysztof BrzózkaDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Kamil KusDepartment of Drug Metabolism and Pharmacokinetics, Ryvu Therapeutics S.A., Sternbacha 2 Street, 30-394, Krakow, Poland.
Jagiellonian University · PLUniversity School of Physical Education in Kraków · PL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

BACKGROUND AND

objectiveThe prediction of pharmacokinetic parameters for drugs metabolised by cytochrome P450 enzymes has been the subject of active research for many years, while the application of in vitro-in vivo extrapolation (IVIVE) techniques for non-cytochrome P450 enzymes has not been thoroughly evaluated. There is still no established quantitative method for predicting hepatic clearance of drugs metabolised by uridine 5'-diphospho-glucuronosyltransferases (UGTs), not to mention those which undergo hepatic uptake. The objective of the study was to predict the human hepatic clearance for telmisartan based on in vitro metabolic stability and hepatic uptake results.

methodsTelmisartan was examined in liver systems, allowing to estimate intrinsic clearance (CL

resultsThe in vitro scaled CL

conclusionsThe study showed that taking into consideration hepatic uptake of a drug allows us to obtain satisfactory scaling factors, hence enabling the prediction of in vivo hepatic glucuronidation from in vitro data.

Indexed as

GlucuronidesGlucuronosyltransferaseMicrosomes, LiverSolute Carrier Organic Anion Transporter Family Member 1B3TelmisartanBenzoatesChromatography, LiquidHepatocytesHumansLiverMetabolic Clearance RateModels, BiologicalTandem Mass SpectrometryBenzoatesGlucuronidesGlucuronosyltransferaseSLCO1B3 protein, humanSolute Carrier Organic Anion Transporter Family Member 1B3TelmisartanUDP-glucuronosyltransferase, UGT1A3

Identifiers

PMID38642299
OpenAlexW4394989015

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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.