Evidence map›Paper›PMID 38689161›Full record

ReviewEuropean journal of drug metabolism and pharmacokinetics2024

The Use of Microdosing for In vivo Phenotyping of Cytochrome P450 Enzymes: Where Do We Stand? A Narrative Review.

Lisa T van der Heijden, Frans L Opdam, Jos H Beijnen, Alwin D R Huitema

Abstract readReview
In one paragraph

Review 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. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
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.

  1. Article
  2. Article
  3. Frontiers in pharmacology · 2025
    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

4 authors.

Lisa T van der HeijdenDepartment of Pharmacology and Pharmacy, Antoni van Leeuwenhoek/The Netherlands Cancer Institute, Amsterdam, The Netherlands. l.vd.heijden@nki.nl.ORCID http://orcid.org/0000-0001-8538-8101
Frans L OpdamDepartment of Medical Oncology, The Netherlands Cancer Institute, Amsterdam, The Netherlands.
Jos H BeijnenDepartment of Pharmacology and Pharmacy, Antoni van Leeuwenhoek/The Netherlands Cancer Institute, Amsterdam, The Netherlands.
Alwin D R HuitemaDepartment of Pharmacology and Pharmacy, Antoni van Leeuwenhoek/The Netherlands Cancer Institute, Amsterdam, The Netherlands.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Cytochrome P450 (CYP) enzymes play a central role in the elimination of approximately 80% of all clinically used drugs. Differences in CYP enzyme activity between individuals can contribute to interindividual variability in exposure and, therefore, treatment outcome. In vivo CYP enzyme activity could be determined with phenotyping. Currently, (sub)therapeutic doses are used for in vivo phenotyping, which can lead to side effects. The use of microdoses (100 µg) for in vivo phenotyping for CYP enzymes could overcome the limitations associated with the use of (sub)therapeutic doses of substrates. The aim of this review is to provide a critical overview of the application of microdosing for in vivo phenotyping of CYP enzymes. A literature search was performed to find drug-drug interaction studies of CYP enzyme substrates that used microdoses of the respective substrates. A substrate was deemed sensitive to changes in CYP enzyme activity when the pharmacokinetics of the substrate significantly changed during inhibition and induction of the enzyme. On the basis of the currently available evidence, the use of microdosing for in vivo phenotyping for subtypes CYP1A2, CYP2C9, CYP2D6, and CYP2E1 is not recommended. Microdosing can be used for the in vivo phenotyping of CYP2C19 and CYP3A. The recommended microdose phenotyping test for CYP2C19 is measuring the omeprazole area-under-the-concentration-time curve over 24 h (AUC

Indexed as

Cytochrome P-450 Enzyme SystemDrug InteractionsPhenotypeAnimalsCytochrome P-450 Enzyme InhibitorsDose-Response Relationship, DrugHumansPharmaceutical PreparationsCytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemPharmaceutical Preparations

Identifiers

PMID38689161
PMCPMC11199305

What Socratic 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 Socratic graph.