No additive effect of combining sumatriptan and olcegepant in the GTN mouse model of migraine

Cephalalgia. 2021 Mar;41(3):329-339. doi: 10.1177/0333102420963857. Epub 2020 Oct 15.

Abstract

Introduction: Despite recent advances in migraine treatment there is a need for therapies with higher clinical efficacy and/or fewer side effects. Triptans (5-HT1B/1D/1F agonists) are essential in the present treatment regime and gepants (CGRP-receptor antagonists) are recognized as effective in acute migraine treatment. Triptans and gepants have different mechanisms of action and here we tested the hypothesis that a combination of these drugs (sumatriptan and olcegepant) would result in an additive effect.

Methods: Using the validated glyceryl trinitrate mouse model of migraine, we initially tested dose-response relationships of sumatriptan (0.1, 0.3, and 0.6 mg/kg IP) and olcegepant (0.25, 0.50, and 1.0 mg/kg IP) to find suitable high and low doses. Subsequently, we performed a combination study of the two drugs with a low and a high dose. All experiments were vehicle (placebo) controlled and blinded.

Results: Sumatriptan significantly reduced glyceryl trinitrate-induced allodynia (F(4,54) = 13.51, p < 0.0001) at all doses. Olcegepant also reduced glyceryl trinitrate-induced allodynia (F(4,53) = 16.11, p < 0.0001) with the two higher doses being significantly effective. Combining 0.50 mg/kg olcegepant with 0.1 or 0.6 mg/kg sumatriptan did not have any improved effect compared to either drug alone (p > 0.50 on all days) in our mouse model.

Conclusion: Combining olcegepant and sumatriptan did not have an additive effect compared to single-drug treatment in this study. Triptan-gepant combinations will therefore most likely not improve migraine treatment. Nevertheless, further studies are necessary, and combinations should also be examined in patients with migraine.

Keywords: CGRP; CGRP receptor antagonists; Headache; additivity; pain; triptans.

MeSH terms

  • Animals
  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • Disease Models, Animal
  • Hyperalgesia
  • Mice
  • Migraine Disorders* / chemically induced
  • Migraine Disorders* / drug therapy
  • Nitroglycerin
  • Pharmaceutical Preparations
  • Piperazines
  • Quinazolines
  • Sumatriptan
  • Tryptamines

Substances

  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • Pharmaceutical Preparations
  • Piperazines
  • Quinazolines
  • Tryptamines
  • Sumatriptan
  • Nitroglycerin
  • olcegepant