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Horizant (GABAPENTIN ENACARBIL)
Horizant (generic name: GABAPENTIN ENACARBIL) is a Anti-epileptic Agent Small molecule drug developed by Azurity. It is currently FDA-approved (first approved 2011) for Postherpetic neuralgia, Restless legs.
Horizant works by binding to the alpha-2/delta-1 subunit of voltage-dependent calcium channels, reducing the release of excitatory neurotransmitters and alleviating pain.
Horizant, also known as gabapentin enacarbil, is a small molecule that modulates voltage-gated calcium channels. It has been studied in various clinical trials for conditions such as adolescent idiopathic scoliosis, treatment-resistant depression, and blood pressure, among others.
At a glance
| Generic name | GABAPENTIN ENACARBIL |
|---|---|
| Sponsor | Azurity |
| Drug class | Anti-epileptic Agent |
| Target | Voltage-dependent calcium channel subunit alpha-2/delta-1 |
| Modality | Small molecule |
| Therapeutic area | Neuroscience |
| Phase | FDA-approved |
| First approval | 2011 |
Mechanism of action
Gabapentin enacarbil is prodrug of gabapentin and, accordingly, its therapeutic effects in RLS and PHN are attributable to gabapentin.The precise mechanism by which gabapentin is efficacious in RLS and PHN is unknown.The mechanism of action by which gabapentin is efficacious in PHN is unknown but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Gabapentin prevents pain-related responses in several models of neuropathic pain in rats and mice (e.g., spinal nerve ligation models, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formalin test), but does not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase). The relevance of these models to human pain is n
Approved indications
- Postherpetic neuralgia
- Restless legs
Common side effects
- Somnolence/sedation
- Dizziness
- Headache
- Nausea
- Fatigue
- Irritability
- Feeling drunk
- Peripheral edema
- Weight increased
- Increased appetite
- Vertigo
- Blurred vision
Key clinical trials
- Procedural Framing and Epidural Steroid Injection Outcomes (NA)
- Nonopioid Analgesia After Anterior Cruciate Ligament Reconstruction (PHASE2,PHASE3)
- Transcranial Magnetic Stimulation Therapy in Neuropathic Painful Spinal Cord Injury Patients (NA)
- Gabapentin and Oxcarbazepine for Chronic Neuropathic Pain in Children and Adolescents: A Clinical Effectiveness Study (PHASE3)
- High-dose Prophylactic Gabapentin (HOPE) vs. Placebo to Prevent Opioid Use for Oral Mucositis Pain During Concurrent Chemoradiation for Head and Neck Cancer (PHASE3)
- Effect of Gabapentin on Kidney Function Following Laparoscopic Sleeve Gastrectomy(LSG) (PHASE4)
- Efficacy of Gabapentin Combined With Solifenacin for Non-neurogenic Overactive Bladder in Women (PHASE3)
- Biomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin (PHASE4)
Patents
| Patent | Expiry | Type |
|---|---|---|
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Horizant CI brief — competitive landscape report
- Horizant updates RSS · CI watch RSS
- Azurity portfolio CI
Frequently asked questions about Horizant
What is Horizant?
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What does Horizant target?
Related
- Drug class: All Anti-epileptic Agent drugs
- Target: All drugs targeting Voltage-dependent calcium channel subunit alpha-2/delta-1
- Manufacturer: Azurity — full pipeline
- Therapeutic area: All drugs in Neuroscience
- Indication: Drugs for Postherpetic neuralgia
- Indication: Drugs for Restless legs
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing