Evidence mapPaperPMID 35945682Full record

ArticleNephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association2023

Tacrolimus induces a pro-fibrotic response in donor-derived human proximal tubule cells dependent on common variants of the CYP3A5 and ABCB1 genes.

Noël Knops, Yasaman Ramazani, Henriëtte De Loor, Roel Goldschmeding, Tri Q Nguyen, Lambert P van den Heuvel, Elena Levtchenko, Dirk J Kuypers

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In one paragraph

Article in Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.7field-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

6 citing papers in PubMed, 8 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

8 authors at 4 institutions in 3 countries.

Noël KnopsDepartment of Pediatric Nephrology and Solid Organ Transplantation, UZ Leuven, University Hospitals Leuven, Leuven, Belgium.
Yasaman RamazaniLaboratory of Pediatric Nephrology, Department of Growth and Regeneration, University of Leuven, Leuven, Belgium.
Henriëtte De LoorDepartment of Nephrology and Renal Transplantation, University Hospitals Leuven, Leuven, Belgium.
Roel GoldschmedingDepartment of Pathology, University Medical Center Utrecht, Utrecht, The Netherlands.
Tri Q NguyenDepartment of Pathology, University Medical Center Utrecht, Utrecht, The Netherlands.
Lambert P van den HeuvelLaboratory of Pediatric Nephrology, Department of Growth and Regeneration, University of Leuven, Leuven, Belgium.
Elena LevtchenkoDepartment of Pediatric Nephrology and Solid Organ Transplantation, UZ Leuven, University Hospitals Leuven, Leuven, Belgium.
Dirk J KuypersDepartment of Nephrology and Renal Transplantation, University Hospitals Leuven, Leuven, Belgium.
KU Leuven · BEUniversity Medical Center Utrecht · NLRadboud University Nijmegen · NLUniversitair Ziekenhuis Leuven · BE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundCommon genetic variants of the enzymes and efflux pump involved in tacrolimus disposition have been associated with calcineurin inhibitor nephrotoxicity, but their importance is unclear because of the multifactorial background of renal fibrosis. This study explores the pro-fibrotic response of tacrolimus exposure in relation to the differential capacity for tacrolimus metabolism in proximal tubule cells (PTCs) with a variable (pharmaco)genetic background.

methodsPTCs were obtained from protocol allograft biopsies with different combinations of CYP3A5 and ABCB1 variants and were incubated with tacrolimus within the concentration range found in vivo. Gene and protein expression, CYP3A5 and P-glycoprotein function, and tacrolimus metabolites were measured in PTC. Connective tissue growth factor (CTGF) expression was assessed in protocol biopsies of kidney allograft recipients.

resultsPTCs produce CTGF in response to escalating tacrolimus exposure, which is approximately 2-fold higher in cells with the CYP3A5*1 and ABCB1 TT combination in vitro. Increasing tacrolimus exposure results in relative higher generation of the main tacrolimus metabolite {13-O-desmethyl tacrolimus [M1]} in cells with this same genetic background. Protocol biopsies show a larger increase in in vivo CTGF tissue expression over time in TT vs. CC/CT but was not affected by the CYP3A5 genotype.

conclusionsTacrolimus exposure induces a pro-fibrotic response in a PTC model in function of the donor pharmacogenetic background associated with tacrolimus metabolism. This finding provides a mechanistic insight into the nephrotoxicity associated with tacrolimus treatment and offers opportunities for a tailored immunosuppressive treatment.

Indexed as

Kidney DiseasesKidney TransplantationATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1Cytochrome P-450 CYP3AGenotypeHumansImmunosuppressive AgentsPolymorphism, Single NucleotideTacrolimusABCB1 protein, humanATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1CYP3A5 protein, humanCytochrome P-450 CYP3AImmunosuppressive AgentsTacrolimuscalcineurin inhibitor toxicityconnective tissue growth factorgenetic-dependent pro-fibrotic responsehuman donor proximal tubule cellstacrolimus

Identifiers

PMID35945682
PMCPMC9976759
OpenAlexW4292449032

What Socratic holds

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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 Socratic graph.