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Study of the Functions and Activities of Neuronal K-Cl Co-Transporter KCC2 Using Western Blotting
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A comprehensive functional and clinical analysis of ABCC2 and its impact on treatment response to carbamazepine

S Rädisch1, D Dickens1, T Lang2

  • 1Department of Molecular and Clinical Pharmacology, The Wolfson Centre for Personalised Medicine, Institute of Translational Medicine, University of Liverpool, Liverpool, UK.

The Pharmacogenomics Journal
|February 26, 2014
PubMed

Insights

This study found that carbamazepine (CBZ) is not transported by the ABCC2 transporter. Genetic variations in ABCC2 do not influence the effectiveness of CBZ for epilepsy treatment.

Area of Science:

  • Pharmacology
  • Genetics
  • Neuroscience

Background:

  • The drug efflux transporter ABCC2 (MRP2) is implicated in carbamazepine (CBZ) treatment resistance in epilepsy.
  • Previous studies on ABCC2 polymorphisms and CBZ efficacy have yielded conflicting results.

Purpose of the Study:

  • To determine if carbamazepine (CBZ) is a substrate of the ABCC2 transporter.
  • To investigate the association between common ABCC2 genetic variants and CBZ treatment outcomes in epilepsy patients.

Main Methods:

  • In vitro cell efflux and plasma membrane vesicle uptake assays were performed to assess CBZ-ABCC2 interaction.
  • Clinical data from the SANAD trial were analyzed to evaluate the impact of three ABCC2 polymorphisms (-24C>T, c.1249G>A, c.3972C>T) on seizure control and remission.

Main Results:

  • Carbamazepine (CBZ) was not identified as a substrate for human ABCC2 in in vitro experiments.
  • No statistically significant association was found between the studied ABCC2 genetic variants and CBZ treatment efficacy, including time to first seizure and time to 12-month remission.

Conclusions:

  • The findings do not support a role for the ABCC2 transporter in carbamazepine (CBZ) treatment response or resistance in epilepsy.
  • ABCC2 polymorphisms are unlikely to be a major factor influencing the clinical effectiveness of carbamazepine for epilepsy management.

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