Background/Purpose: Mirogabalin (DS-5565) is a novel ligand of the α₂δ subunit of voltage-gated calcium channels. Mirogabalin possesses unique binding characteristics to α₂δ subunits, and potent and long-lasting analgesic effects in peripheral neuropathic pain models.  Phase III clinical trials of mirogabalin in patients with postherpetic neuralgia, diabetic peripheral neuropathic pain and fibromyalgia are ongoing.  In the present study, we investigated the analgesic effects of mirogabalin in two animal models of fibromyalgia, the intermittent cold stress model in mice and the intramuscular acid saline injection model in rats.

Methods: Female ddY mice were exposed to intermittent cold stress for three days, and male SD rats received two repeated intramuscular injections of acid saline (pH 4.0) into the gastrocnemius muscle. After development of hyperalgesia, the animals received the test compounds (mirogabalin and pregabalin) orally and the pain responses to mechanical stimulation were determined by von Frey test.

Results: In both models, mechanical hyperalgesia was demonstrated by increased pain scores or decreased pain thresholds to von Frey filaments.  A single oral administration of mirogabalin (1, 3 and 10 mg/kg) significantly inhibited mechanical hyperalgesia in both models.  The effects of mirogabalin were significant up to 6 or 8 hours after administration.  Pregabalin, a standard α₂δ ligand showed similar effects at 30 mg/kg.

Conclusion: Mirogabalin showed potent and long-lasting analgesic effects in two non-clinical models of fibromyalgia.  Mirogabalin may provide effective pain relief for patients with fibromyalgia.

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ACR Meeting Abstracts - https://acrabstracts.org/abstract/analgesic-effects-of-the-novel-alpha-2-delta-ligand-mirogabalin-ds-5565-in-experimental-animal-models-of-fibromyalgia/