Gabapentin enacarbil

DB08872ApprovedSmall moleculeAnti-epileptic Agent

Gabapentin enacarbil is a gabapentin prodrug used to treat Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). Gabapentin enacarbil is marketed under the name Horizant.

Mechanism: Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Curator reviewed
Primary indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).Curator reviewed · 2 structured indications
Formula / weight: C₁₆H₂₇NO₆ · 329.393 g/mol (avg)
First approval: United States, 2011
Code names: ASP-8825 · GSK-1838262 · XP-13512
Brand names: Horizant

Resolves to

Compound

UNII75OCL1SPBQCAS478296-72-9ChEMBLCHEMBL1628502ChEBI68840PubChem9883933KEGGD09539

Clinical / RWD

RxNorm1101333

Structure

InChIKeyTZDUHAJSIBHXDL-UHFFFAOYSA-NSMILESCC(C)C(=O)OC(C)OC(=O)NCC1(CC(O)=O)CCCCC1

Targets

P54289CACNA2D1Q9NY47CACNA2D2Q9Y289SLC5A6

Transporters

Q8N695SLC5A8Q9Y289SLC5A6

What you can answer from here — as of September 12, 2026

3Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

2TransportersSubstrate / inhibitor direction, not just membership

Listed above

1,308Drug interactionsStructured to mechanism, not free text

26Clinical trialsPhase, status and sponsor resolved per trial

2Structured indicationsCondition, population, route and combination as fields, not prose

1ContraindicationEach with its own population and attribute set

6Marketed productsAcross 1 country and 4 labellers

8+ReferencesStructured and connected to the statements they support

Which drugs share a target with Gabapentin enacarbil, and which of those have an active Phase 3 trial?

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