Gabapentin treatment in a patient with KCNQ2 developmental epileptic encephalopathy

Pharmacol Res. 2020 Oct:160:105200. doi: 10.1016/j.phrs.2020.105200. Epub 2020 Sep 15.

Abstract

De novo variants in KCNQ2 encoding for Kv7.2 voltage-dependent neuronal potassium (K+) channel subunits are associated with developmental epileptic encephalopathy (DEE). We herein describe the clinical and electroencephalographic (EEG) features of a child with early-onset DEE caused by the novel KCNQ2 p.G310S variant. In vitro experiments demonstrated that the mutation induces loss-of-function effects on the currents produced by channels incorporating mutant subunits; these effects were counteracted by the selective Kv7 opener retigabine and by gabapentin, a recently described Kv7 activator. Given these data, the patient started treatment with gabapentin, showing a rapid and sustained clinical and EEG improvement over the following months. Overall, these results suggest that gabapentin can be regarded as a precision therapy for DEEs due to KCNQ2 loss-of-function mutations.

Keywords: Gabapentin; KCNQ2; developmental and epileptic encephalopathy; epilepsy; loss-of-function; precision medicine.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Age of Onset
  • Animals
  • Anticonvulsants / therapeutic use*
  • CHO Cells
  • Carbamates / therapeutic use
  • Cells, Cultured
  • Child
  • Cricetinae
  • Cricetulus
  • Electroencephalography
  • Epilepsy / drug therapy*
  • Epilepsy / genetics*
  • Female
  • Gabapentin / therapeutic use*
  • Humans
  • KCNQ2 Potassium Channel / genetics*
  • Mutation
  • Phenylenediamines / therapeutic use
  • Precision Medicine
  • Rats
  • Treatment Outcome

Substances

  • Anticonvulsants
  • Carbamates
  • KCNQ2 Potassium Channel
  • KCNQ2 protein, human
  • Phenylenediamines
  • ezogabine
  • Gabapentin