Related Experiment Video
Updated: Jul 26, 2026

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 18, 2013
Transporters and drug discovery: why, when, and how
1Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA.
Abstract:
Drug transporters are now increasingly recognized as important determinants of variable drug disposition and response. In addition, transporter associated problems appear to be occurring with greater frequency during the drug discovery and development process. What has not been clear is whether drug transporter related issues are a truly new problem, or whether such issues had existed all along, but were previously unrecognized or ignored. In this review, a brief overview of key drug transporters will be outlined. In addition, a commentary on specific issues of relevance to pharmaceutical sciences in terms of the role and relevance of drug transporters to the drug discovery and development process is provided.
Related Concept Videos
The Significance of Membrane Transport
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
Membrane Transporters
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
Drug Discovery: Overview
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Hepatic Drug Clearance: Role of Transporters
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

