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Updated: May 17, 2026

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
Published on: September 29, 2023
Renal transporters in drug development
Kari M Morrissey1, Sophie L Stocker, Matthias B Wittwer
1Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, California 94158, USA. kari.morrissey@ucsf.edu
The kidney eliminates toxic substances and drugs via proximal tubule transporters, crucial for drug interactions and clearance. Understanding these renal transporters impacts drug safety and efficacy.
Area of Science:
- Pharmacology
- Nephrology
- Drug Metabolism
Background:
- The kidney is essential for eliminating xenobiotics and metabolic waste.
- Proximal tubule secretory transporters significantly influence xenobiotic and drug disposition.
- Recent advancements highlight the role of renal transporters in drug-drug interactions.
Purpose of the Study:
- To review renal drug handling, clearance calculations, and the impact of transporters.
- To provide data on renal drug transporter localization, expression, substrates, and inhibitors.
- To discuss regulatory guidance, special populations, and transporter variants in renal drug elimination.
Main Methods:
- Literature review of renal drug handling and transporter function.
- Tabulation of data on renal drug transporters (localization, expression, substrates, inhibitors).
- Discussion of regulatory guidelines and special population considerations.
Main Results:
- Detailed description of renal drug handling and clearance equations (filtration and secretory).
- Comprehensive tables summarizing key characteristics of renal drug transporters.
- Analysis of the implications of renal transporters in drug-drug interactions and special populations.
Conclusions:
- Renal transporters are critical determinants of drug disposition and are sites of drug-drug interactions.
- Understanding renal transporter function is vital for optimizing drug therapy and predicting interactions.
- This review provides a comprehensive overview for researchers and clinicians studying renal drug transport.
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