Drug intelligence / Profile preview

gabapentin enacarbil + morphine

Development stage
Phase 1
Lead developer
Azurity Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Gabapentin enacarbil + morphine is a combination drug regimen composed of gabapentin enacarbil, a prodrug of gabapentin, and morphine, a classic opioid analgesic. This combination is studied for its enhanced analgesic efficacy in neuropathic pain compared to either drug alone, achieving better analgesia at lower doses. Gabapentin enacarbil primarily acts by binding to the α2δ subunit of voltage-gated calcium channels, decreasing neuronal excitability, while morphine is a mu-opioid receptor agonist. The combination can increase adverse CNS effects, including sedation, dizziness, nausea, and may increase the risk of respiratory depression. The combination is not marketed as a fixed-dose product but is sometimes investigated or used as concomitant therapy in clinical settings for conditions such as neuropathic pain or postherpetic neuralgia[1][2][4][5][6].

02

Targets

MOR (Mu opioid receptor)SLC16A1 (Mitochondrial Pyruvate Carrier)SLC5A6 (Sodium-dependent multivitamin transporter)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)CACNA2D2 (α2δ-2)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)

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