Product Details:

CasNo： 478296-72-9

Molecular Formula： C16H27NO6

Appearance： Light yellow to brown

Packing： Bottle

Throughput： 100KG/Month

Purity： 99%

Gabapentin Enacarbil

Brand name: Horizant (US), Regnite (Japan)

Indications (FDA Approved)

1. Treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults
2. Management of postherpetic neuralgia (PHN) in adults

Note: Gabapentin enacarbil is NOT approved for epilepsy, unlike immediate-release gabapentin.

Product Introduction (English, for API / Brochure)

Gabapentin enacarbil is an extended-release oral prodrug of gabapentin. After oral administration, it is rapidly hydrolyzed in the gastrointestinal tract to release active gabapentin. It acts by binding to the α₂δ subunit of voltage-gated calcium channels in the central nervous system, reducing the release of excitatory neurotransmitters to produce neuropathic analgesic effects.

As a prodrug, it circumvents the saturable absorption limitation of immediate-release gabapentin. It uses intestinal amino acid transporters to achieve more consistent, dose-proportional absorption and stable plasma gabapentin concentrations.

The commercial formulation is extended-release tablet, available in 300 mg and 600 mg strengths.

• For RLS: 600 mg once daily, taken with food at approximately 5 PM.
• For PHN: Initiate 600 mg once daily in the morning for 3 days, then titrate to 600 mg twice daily (1200 mg/day). Doses above 1200 mg/day show no additional efficacy but higher adverse events.

It has minimal CYP450-mediated drug interactions. The active metabolite gabapentin is excreted unchanged via the kidney; dose adjustment is required for patients with renal impairment. Common adverse reactions include somnolence, dizziness, headache and fatigue. There is a black-box warning for increased risk of suicidal thoughts and behaviours with antiepileptic agents.

Short version (for product list / COA header)

Gabapentin enacarbil is an extended-release prodrug of gabapentin, FDA-approved for adult moderate-to-severe primary restless legs syndrome and postherpetic neuralgia. It provides improved absorption profile compared with immediate-release gabapentin, delivering predictable systemic exposure of gabapentin.