Evidence map›Paper›PMID 33232579›Full record

ArticleBasic & clinical pharmacology & toxicology2021

Drug-drug interaction of atazanavir on UGT1A1-mediated glucuronidation of molidustat in human.

Dorina van der Mey, Michael Gerisch, Natalia A Jungmann, Andreas Kaiser, Kenichi Yoshikawa, Simone Schulz, Martin Radtke, Silvia Lentini

Open access · hybridAbstract read
In one paragraph

Article in Basic & clinical pharmacology & toxicology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.9field-weighted citation impact, top 23% 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

3 citing papers in PubMed, 12 citations in OpenAlex.

  1. Article
  2. Review
  3. 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

8 authors at 2 institutions in 3 countries.

Dorina van der MeyClinical Pharmacology Cardiovascular/Haematology, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.ORCID https://orcid.org/0000-0003-2779-9388
Michael GerischDrug Metabolism and Pharmacokinetics, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.ORCID https://orcid.org/0000-0003-3807-9036
Natalia A JungmannDrug Metabolism and Pharmacokinetics, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.
Andreas KaiserStatistics and Data Insights, Data Sciences & Analytics, Research & Development, Bayer AG, Berlin, Germany.ORCID https://orcid.org/0000-0002-7758-6500
Kenichi YoshikawaClinical Pharmacology, Clinical Sciences, Research & Development, Bayer Yakuhin Ltd, Osaka, Japan.
Simone SchulzDrug Metabolism and Pharmacokinetics, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.
Martin RadtkeDrug Metabolism and Pharmacokinetics, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.
Silvia LentiniClinical Pharmacology Cardiovascular/Haematology, Translational Sciences, Research & Development, Bayer AG, Wuppertal, Germany.
Bayer (Germany) · DEBayer (United States) · US

Funding

Bayer AG
6 · The paper itself

Abstract

Molidustat is an oral inhibitor of hypoxia-inducible factor (HIF) prolyl-hydroxylase enhancing the erythropoietin (EPO) response to HIF; it is in clinical development for the treatment of anaemia related to chronic kidney disease. The predominant role of glucuronidation for molidustat clearance (formation of N-glucuronide metabolite M1) and subsequent renal excretion was confirmed in a human mass balance study, with about 85% of the drug being excreted as M1 in urine. The inhibitory effects of 176 drugs and xenobiotics from various compound classes on the UGT-mediated glucuronidation of molidustat in human liver microsomes (HLMs) were investigated. Based on preclinical findings, glucuronidation of molidustat was predominantly mediated by the 5'-diphospho-glucuronosyltransferase (UGT) isoform UGT1A1. Therefore, atazanavir, which is a potent inhibitor of UGT1A1, was chosen for the evaluation of pharmacokinetics and EPO release following a single oral dose of 25 mg molidustat. Molidustat exposure increased about twofold upon coadministration with atazanavir when considering area under plasma concentration-time curve from zero to infinity (AUC) and maximum plasma concentration (C

Indexed as

AdultAtazanavir SulfateDrug InteractionsErythropoietinGlucuronidesGlucuronosyltransferaseHumansMaleMiddle AgedPyrazolesTriazolesUGT1A1 EnzymeYoung AdultAtazanavir SulfateErythropoietinGlucuronidesGlucuronosyltransferasemolidustatPyrazolesTriazolesUGT1A1 Enzymeatazanavirdrug-drug interactionHIF-PH inhibitormolidustatUGT

Identifiers

PMID33232579
PMCPMC7983974
OpenAlexW3107302406

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.