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Assessing transporter-mediated rifampin-linezolid interaction using physiologically-based pharmacokinetic modelling.

Hoang Dat Nguyen1, Vinh Hoa Pham2, Richard M Hoglund3,4

  • 1Master of Science Program in Biopharmaceutical Sciences, Department of Biochemistry, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.

British Journal of Clinical Pharmacology
|January 27, 2026
PubMed
Summary
This summary is machine-generated.

The ATP-binding cassette sub-family B member 1 (ABCB1) transporter primarily drives the drug-drug interaction between rifampin and linezolid. High-dose rifampin does not significantly alter linezolid exposure compared to standard doses.

Keywords:
drug–drug interactionlinezolidphysiologically‐based pharmacokinetic modelrifampintransporter

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Area of Science:

  • Pharmacokinetics and Drug Metabolism
  • Computational Biology and Modeling
  • Infectious Disease Pharmacology

Background:

  • Drug-drug interactions (DDIs) involving rifampin and linezolid can alter linezolid's efficacy and safety.
  • Understanding the role of specific transporters, like ABCB1 and ABCG2, is crucial for predicting and managing these interactions.
  • Physiologically-based pharmacokinetic (PBPK) modeling offers a quantitative approach to investigate complex DDIs.

Purpose of the Study:

  • To develop and validate a PBPK model for linezolid.
  • To quantitatively assess the contribution of ABCB1 and ABCG2 transporters to the rifampin-linezolid DDI.
  • To predict the impact of high-dose rifampin on linezolid pharmacokinetics (PK).

Main Methods:

  • A PBPK model for linezolid was constructed and verified using clinical PK data.
  • A PK-SIM PBPK model for rifampin, incorporating ABCB1 and ABCG2 transporter activity, was utilized.
  • PBPK simulations predicted linezolid PK during co-administration with rifampin, including high-dose scenarios.

Main Results:

  • The linezolid PBPK model demonstrated good predictive performance across multiple clinical studies.
  • PBPK simulations indicated that ABCB1 plays a more significant role than ABCG2 in the rifampin-linezolid DDI.
  • Predicted DDI ratios for standard-dose rifampin closely matched observed clinical data.
  • Increasing rifampin dosage did not substantially change linezolid exposure.

Conclusions:

  • ABCB1 is identified as the primary transporter mediating the DDI between rifampin and linezolid.
  • The DDI effect of high-dose rifampin on linezolid exposure is comparable to that of standard-dose rifampin.
  • PBPK modeling provides a valuable tool for predicting transporter-mediated DDIs.