Impact of Drug Transporter Studies on Drug Discovery and Development

  title={Impact of Drug Transporter Studies on Drug Discovery and Development},
  author={Naomi Mizuno and Takuro Niwa and Yoshihisa Yotsumoto and Yuichi Sugiyama},
  journal={Pharmacological Reviews},
  pages={425 - 461}
Drug transporters are expressed in many tissues such as the intestine, liver, kidney, and brain, and play key roles in drug absorption, distribution, and excretion. The information on the functional characteristics of drug transporters provides important information to allow improvements in drug delivery or drug design by targeting specific transporter proteins. In this article we summarize the significant role played by drug transporters in drug disposition, focusing particularly on their… 

Role of Membrane Transporters in Drug Delivery, Drug Disposition And Drug-Drug Interactions

Tissues such as liver, kidney, brain and intestine expresses membrane transporters which play a vital role in drug absorption, distribution, metabolism and excretion, so exploring the transporter functionality chances of delivering a therapeutic agent to the target organ enhances.

Role of transport proteins in drug discovery and development: a pharmaceutical perspective

The weight of evidence suggests that only a small number of transport proteins need to be routinely considered in the drug-discovery setting driven by the magnitude of their impact on tissue distribution, pharmacokinetic variability and drug–drug interactions.

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A regulatory viewpoint on transporters and their potential role in drug–drug interactions is provided and criteria that may warrant conduct of in vivo P-gp-mediated drug interaction studies based on in vitro assessment are explained.

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The role of drug transporters in the adaptation and growth of tumors and in their potential usefulness as therapeutic targets in cancer are focused on.

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Hematic drug transporters have gained additional importance in drug clearance by optimization for basic DMPK properties early on in drug research, however, the lack of selective substrates and inhibitors, proper assessment of the kinetic properties due to interfering passive permeability and multiple binding sites, are some of the hurdles in studying active drug transport processes.



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The significant role played by drug transporters in drug disposition is summarized, focusing on their potential use during the drug development process, and high-throughput screening systems using transporter gene transfected cells or computational approaches are efficient tools for assessing transport activity during the early stage of drug development.

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