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Gabapentin Enacarbil (GEn)
Gabapentin enacarbil is a prodrug of gabapentin that enhances GABA neurotransmission in the central nervous system by increasing inhibitory signaling.
Gabapentin enacarbil is a prodrug of gabapentin that enhances GABA neurotransmission in the central nervous system by increasing inhibitory signaling. Used for Restless legs syndrome (RLS), Postherpetic neuralgia (PHN).
At a glance
| Generic name | Gabapentin Enacarbil (GEn) |
|---|---|
| Also known as | HORIZANT |
| Sponsor | Cleveland Sleep Research Center |
| Drug class | Gabapentinoid; anticonvulsant/neuropathic pain agent |
| Target | Voltage-gated calcium channel alpha-2-delta subunit |
| Modality | Small molecule |
| Therapeutic area | Neurology |
| Phase | FDA-approved |
Mechanism of action
Gabapentin enacarbil is converted to gabapentin in vivo and binds to the alpha-2-delta subunit of voltage-gated calcium channels, reducing calcium influx and decreasing excitatory neurotransmitter release. This mechanism reduces neuronal hyperexcitability and provides symptomatic relief in conditions characterized by abnormal nerve activity, particularly restless legs syndrome and postherpetic neuralgia.
Approved indications
- Restless legs syndrome (RLS)
- Postherpetic neuralgia (PHN)
Common side effects
- Dizziness
- Somnolence
- Headache
- Peripheral edema
- Ataxia
Key clinical trials
- Effect of Gabapentin on Kidney Function Following Laparoscopic Sleeve Gastrectomy(LSG) (PHASE4)
- Effectiveness of AI-Guided Exercise and Pain Neuroscience Education for Fibromyalgia (FIBROIA) (NA)
- The Effect of Preoperative Gabapentin on Postoperative Pain Control and Analgesic Requirements Following Bariatric Surgery (NA)
- Opioid Sparing Effect of an ISP Nerve Block on Post-Op Pain Control in Posterior Cervical Spine Surgery (NA)
- PECS Block vs. Multimodal Analgesia for Prevention of Persistent Postoperative Pain in Breast Surgery (PHASE2)
- Effect of Multimodal Opioid-free Anesthesia on Return of Bowel Function in Laparoscopic Colorectal Surgery (PHASE3)
- Optimization of Pre-operative Oral Analgesics in Patients Undergoing Ambulatory Minimally Invasive Hysterectomy (NA)
- Nighttime Agitation and Restless Legs Syndrome in People With Alzheimer's Disease (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Gabapentin Enacarbil (GEn) CI brief — competitive landscape report
- Gabapentin Enacarbil (GEn) updates RSS · CI watch RSS
- Cleveland Sleep Research Center portfolio CI