Profiling of drug-metabolizing enzymes and transporters in human tissue biopsy samples: A review of the literatures

A. David Rodrigues, Andrew Rowland

Research output: Contribution to journalReview articlepeer-review

15 Citations (Scopus)


Within the drug pharmacokinetics (PK)-absorption, distribution, metabolism, and excretion (ADME) research community, investigators regularly generate in vitro data sets using appropriately vendor-sourced and processed human tissue. Such data enable drug screening, the generation of kinetic parameters, extrapolation of in vitro to in vivo, as well as the modeling and simulation of drug PK. Although there are large numbers of manuscripts describing studies with deceased organ donor tissue, relatively few investigators have published studies utilizing living donor tissue biopsy samples. After a review of the available literature, it was possible to find publications describing the use of tissue biopsy samples to determine enzyme inhibition ex vivo, the study of genotype-phenotype associations, the evaluation of tissue expression profiling following an inducer, and assessment of correlations between tissue expression profiles and in vivo-derived trait measures (e.g., biomarker plasma levels and probe drug PK). Some reports described multiple single-tissue biopsies, whereas others described singlemultiple-organ biopsies. It is concluded that biopsy-derived data can support modeling exercises (as input data and when validating models) and enable the assessment of organ-specific changes in enzyme and transporter profiles resulting from drug interactions, disease (e.g., metabolic disease, fibrosis, inflammation, cancer, infection), age, pregnancy, organ impairment, and genotype. With the emergence of multiorgan axes (e.g., microbiome-gut-liverkidney) and interest in remote sensing (interorgan communication), it is envisioned that there will be increased demand for single- and multiorgan tissue biopsy data to support hypothesis testing and PK-ADME model building.

Original languageEnglish
Pages (from-to)308-319
Number of pages12
JournalJournal of Pharmacology and Experimental Therapeutics
Issue number3
Publication statusPublished - Mar 2020

Bibliographical note

Publisher Copyright:
© 2020 by The American Society for Pharmacology and Experimental Therapeutics.


  • drug-metabolizing enzymes
  • pharmacokinetics (PK) absorption
  • human tissue biopsy samples
  • PK-ADME model
  • ADME


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