Efficacy and safety of a T-type calcium channel blocker in patients with neuropathic pain: A proof-of-concept, randomized, double-blind and controlled trial

Eur J Pain. 2018 Aug;22(7):1321-1330. doi: 10.1002/ejp.1221. Epub 2018 Apr 18.

Abstract

Background: T-type calcium channels have been shown to play an important role in the initiation and maintenance of neuropathic pain and represent a promising therapeutic target for new analgesic treatments. Ethosuximide (ETX), an anticonvulsant and a T-type channel blocker has shown analgesic effect in several chronic pain models but has not yet been evaluated in patients with neuropathic pain.

Methods: This proof-of-concept, multicentre, double-blind, controlled and randomized trial compared the efficacy and safety of ETX (given as add-on therapy) to an inactive control (IC) in 114 patients with non-diabetic peripheral neuropathic pain. After a 7-day run-in period, eligible patients aged over 18 years were randomly assigned (1:1) to ETX or IC for 6 weeks. The primary outcome was the difference between groups in the pain intensity (% of change from the baseline to end of treatment) assessed in the intention-to-treat population. This study is registered with EudraCT (2013-004801-26) and ClinicalTrials.gov (NCT02100046).

Results: The study was stopped during the interim analysis due to the high number of adverse events in the active treatment group. ETX failed to reduce total pain and showed a poor tolerance in comparison to IC. In the per-protocol analysis, ETX significantly reduced pain intensity by 15.6% (95% CI -25.8; -5.4) from baseline compared to IC (-7.8%, 95% CI -14.3; -1.3; p = 0.033), but this result must be interpreted with caution because of a small subgroup of patients.

Conclusion: Ethosuximide did not reduce the severity of neuropathic pain and induces, at the doses used, many adverse events.

Significance: This article shows that ETX is not effective to treat neuropathic pain. Nevertheless, per-protocol analysis suggests a possible analgesic effect of ETX. Thus, our work adds significant knowledge to preclinical and clinical data on the benefits of T-type calcium channel inhibition for the treatment of neuropathic pain.

Publication types

  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Analgesics / therapeutic use
  • Anticonvulsants / therapeutic use
  • Calcium Channel Blockers / therapeutic use*
  • Chronic Pain / drug therapy*
  • Double-Blind Method
  • Ethosuximide / therapeutic use*
  • Female
  • Humans
  • Male
  • Middle Aged
  • Neuralgia / drug therapy*
  • Proof of Concept Study

Substances

  • Analgesics
  • Anticonvulsants
  • Calcium Channel Blockers
  • Ethosuximide

Associated data

  • ClinicalTrials.gov/NCT02100046