Drug intelligence / Profile preview

gabapentin enacarbil + oxycodone

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

Overview

Gabapentin enacarbil + oxycodone is a **combination of two pharmaceutical drugs**, each with distinct mechanisms of action. **Gabapentin enacarbil** is a prodrug of gabapentin, with improved and more predictable gastrointestinal absorption, and is FDA-approved mainly for moderate-to-severe restless legs syndrome and postherpetic neuralgia. Its mechanism is thought to involve *modulation of voltage-gated calcium channels (specifically the alpha-2-delta subunit),* leading to reduced synaptic release of excitatory neurotransmitters. **Oxycodone** is a semi-synthetic opioid analgesic that exerts its effects primarily as an *agonist at the mu-opioid receptor*, producing analgesia, sedation, and euphoria. This combination is sometimes used off-label for pain management, but carries a **high risk of central nervous system and respiratory depression, excessive sedation, and overdose**, and requires strict medical supervision[1][3]. There is no evidence of an approved, uniquely branded or marketed co-formulation of gabapentin enacarbil and oxycodone; any use is based on co-prescription, not a fixed-dose product.

02

Targets

CACNA2D2 (Voltage-gated calcium channel subunit alpha-2/delta-2)MOR (Mu opioid receptor)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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