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Updated: Sep 18, 2025

Human Liver Microphysiological System for Assessing Drug-Induced Liver Toxicity In Vitro
Published on: January 31, 2022
Emerging evidence of inter-organ interaction on drug transporters under liver injury
Ling Jiang1, Ying Deng1, Ruijing Mu1
1Center of Drug Metabolism and Pharmacokinetics, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Abstract:
Dysfunction of drug transporters significantly affects therapeutic outcomes and drug efficacy in patients with liver injury. Clinical and experimental evidence demonstrates that liver injury involves complex inter-organ interactions among the brain, eye, liver, intestine, and kidney. Recent advances in basic and clinical research have illuminated the physiologic and molecular mechanisms underlying transporter alterations in liver injury, particularly those associated with bilirubin, reactive oxygen species, ammonia, bile acid, and inflammatory factors. Notably, the influence of these transporter modifications on drug pharmacokinetics in liver injury patients remains inadequately understood. Additional research is necessary to fully comprehend these effects and their therapeutic implications. The documented alterations of transporters in distant organs across various liver diseases indicate that dosage modifications may be required when administering transporter-substrate drugs, including both traditional Chinese and Western medicines, to patients with liver dysfunction. This strategy helps maintain drug concentrations within therapeutic ranges while reducing adverse reactions. Furthermore, when utilizing transporter inducers or inhibitors clinically, consideration of their long-term effects on transporters and subsequent therapeutic impact is essential. Careful attention must be paid to avoid compromising the elimination of toxic metabolites and proteins when inhibiting these transporters. Similarly, prudent use of inducers or inducer-type therapeutic drugs is necessary to prevent enhanced drug resistance. This review examines recent clinical and experimental findings regarding the inter-organ interaction of drug transporters in liver injury conditions and their clinical relevance.
Insights
Liver injury disrupts drug transporters, impacting treatment effectiveness. Understanding these changes across organs is crucial for safe medication dosing and managing drug interactions.
Area of Science:
- Pharmacology
- Hepatology
- Physiology
Background:
- Drug transporter dysfunction is a key factor in liver injury, affecting patient outcomes.
- Liver injury involves complex inter-organ communication affecting drug transport.
- Alterations in transporters for bilirubin, ammonia, and bile acids are noted in liver disease.
Purpose of the Study:
- To review recent findings on drug transporter alterations in liver injury.
- To explore the impact of inter-organ interactions on drug pharmacokinetics.
- To discuss clinical implications for drug therapy in liver dysfunction.
Main Methods:
- Review of clinical and experimental research findings.
- Analysis of physiological and molecular mechanisms of transporter changes.
- Examination of inter-organ interactions in liver injury models.
Main Results:
- Liver injury causes significant drug transporter alterations across multiple organs.
- These changes impact drug pharmacokinetics, though not fully understood.
- Inter-organ transporter modifications necessitate careful drug dosage adjustments.
Conclusions:
- Drug transporter alterations in liver injury require therapeutic strategy modifications.
- Dosage adjustments for transporter-substrate drugs are essential in liver dysfunction.
- Careful use of transporter inducers/inhibitors is needed to optimize therapy and avoid adverse effects.
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