Gralise (gabapentin; Depomed) is an extended-release formulation of gabapentin, an analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), and is used for treatment of restless leg syndrome and post-herpetic neuralgia (PHN). The exact mechanism of Gralise remains unclear, although it is thought to bind to α2δ subunits of voltage-gated calcium channels. This inhibits high-threshold neuronal Ca2+ currents in cultured dorsal root ganglion cells, which is a suggested factor of its mechanism of action. Current hypotheses suggest that gabapentin-mediated Ca2+ appears to preferentially affect presynaptic P/Q-type voltagegated Ca2+ channels, reducing the release of the excitatory amino acids glutamate and aspartate, leading to a reduction in the release of nociceptive neurotransmitters, calcitonin gene-related peptide (CGRP) and substance P.
LIST OF FIGURES
8 Figure 1: Gralise for neuropathic pain – SWOT analysis
9 Figure 2: Datamonitor Healthcare’s drug assessment summary of Gralise for neuropathic pain
10 Figure 3: Datamonitor Healthcare’s drug assessment summary of Gralise for neuropathic pain
12 Figure 4: Gralise sales for neuropathic pain in the US, 2017–26
LIST OF TABLES 6 Table 1: Gralise drug profile
7 Table 2: Gralise Phase III data in post-herpetic neuralgia
12 Table 3: Gralise sales for neuropathic pain in the US ($m), 2017–26
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