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Related Concept Videos

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...
The Significance of Membrane Transport01:44

The Significance of Membrane Transport

The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu01:29

Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu

Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...
Hepatic Drug Clearance: Role of Transporters01:14

Hepatic Drug Clearance: Role of Transporters

In the liver and bile canaliculi, influx and efflux transporters modification can influence intrinsic clearance. Transporters play a significant role in moving drugs within liver cells. Elaborate models, such as the Biopharmaceutical Classification System (BCS), are essential to relate transporters to drug disposition. This system categorizes drugs into four classes based on solubility and permeability, providing insights into elimination routes and the effects of transporters following oral...
Pharmacogenetics of Drug Metabolism: Overview01:27

Pharmacogenetics of Drug Metabolism: Overview

Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...
Nonlinear Pharmacokinetics: Role of Transporters01:27

Nonlinear Pharmacokinetics: Role of Transporters

A drug's nonlinear kinetics can be influenced by a diverse range of transporter proteins that serve as crucial players in drug distribution. These transporters, found within cells, can enhance or reduce local drug concentrations by facilitating the influx or efflux of drugs. For instance, the expression of xenobiotic transporters can be influenced by factors such as age and gender, potentially impacting the linearity of drug response.
Polymorphisms occurring in drug transporters can alter...

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High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
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High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies

Published on: September 29, 2023

International Transporter Consortium commentary on clinically important transporter polymorphisms.

K M Giacomini1, P V Balimane, S K Cho

  • 1Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA. kathy.giacomini@ucsf.edu

Clinical Pharmacology and Therapeutics
|June 20, 2013
PubMed
Summary
This summary is machine-generated.

Genetic variations in membrane transporters like OATP1B1 and BCRP significantly impact drug response. Understanding these genetic polymorphisms is crucial for personalized medicine and effective drug development.

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Area of Science:

  • Pharmacogenomics
  • Molecular biology
  • Drug metabolism

Background:

  • Genetic polymorphisms in membrane transporters influence drug efficacy and safety.
  • Specific polymorphisms in OATP1B1 (rs4149056) and BCRP (rs2231142) have established clinical relevance.
  • Understanding transporter genetics is key to explaining inter-individual variability in drug pharmacokinetics and pharmacodynamics.

Purpose of the Study:

  • To review the clinical significance of OATP1B1 and BCRP genetic polymorphisms.
  • To summarize evidence linking these polymorphisms to pharmacokinetic and pharmacodynamic variations.
  • To provide recommendations for integrating transporter polymorphism studies into drug development.

Main Methods:

  • Literature review focusing on studies of OATP1B1 (c.521T>C) and BCRP (c.421C>A) polymorphisms.
  • Analysis of clinical evidence for their impact on drug disposition and action.
  • Examination of allele frequencies across diverse ethnic populations.

Main Results:

  • Compelling evidence supports the clinical relevance of OATP1B1 (rs4149056) and BCRP (rs2231142) polymorphisms.
  • These genetic variations demonstrably affect drug pharmacokinetics and pharmacodynamics.
  • Allele frequencies vary significantly among different ethnic groups.

Conclusions:

  • Genetic polymorphisms in membrane transporters are critical determinants of drug response.
  • Incorporating transporter polymorphism data into drug development is recommended.
  • Regulatory considerations for pharmacogenetic studies are highlighted.