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Gralise
- Development stage
- Approved
- Lead developer
- Assertio
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Gralise is an oral, once-daily, gastric-retentive extended-release formulation of gabapentin developed by Depomed (now Assertio Therapeutics). It is specifically indicated for the management of postherpetic neuralgia (PHN). The formulation utilizes Depomed's proprietary Acuform technology, which allows the tablet to swell in the stomach and provide a controlled release of the drug to the upper small intestine, optimizing absorption. Gabapentin's mechanism of action involves high-affinity binding to the alpha-2-delta-1 subunit of voltage-gated calcium channels in the central nervous system. This binding reduces calcium influx into nerve terminals, thereby inhibiting the release of excitatory neurotransmitters such as glutamate and substance P, which are involved in the transmission of neuropathic pain signals.
- Brand names
- Gralise
- Other names
- gabapentin extended-releasegabapentin ER
02
Targets
CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)
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