Gabapentin enacarbil - CAS 478296-72-9
Catalog number: 478296-72-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Calcium Channel
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
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Horizant; Regnite; XP-13512
1.Modified-Release Formulations of Second-Generation Antiepileptic Drugs: Pharmacokinetic and Clinical Aspects.
Anderson GD1, Saneto RP2. CNS Drugs. 2015 Aug;29(8):669-81. doi: 10.1007/s40263-015-0268-5.
Modified-release or extended-release (XR) formulations are used to decrease the frequency of dosing for drugs with rapid elimination, to improve convenience and adherence. Use of a modified-release formulation can decrease the peak to trough fluctuations in serum concentrations and theoretically improve the therapeutic benefit of the drug, by decreasing adverse events associated with the higher peak concentrations. Once-daily formulations of lamotrigine (Lamictal XR(®)), levetiracetam (Keppra XR(®)), oxcarbazepine (Oxtellar XR(®), Apydan(®) extent) and topiramate (Qudexy XR™, Trokendi XR™) are approved for the treatment of focal and/or generalized onset seizures. Other seizure medications have been approved for non-epileptic symptoms. Gabapentin XR (Gralise(®)) is approved for the treatment of post-herpetic neuralgias. Gabapentin enacarbil XR (Horizant(®)) is a prodrug of gabapentin and is indicated for treatment of post-herpetic neuralgia and restless leg syndrome, a novel indication.
2.Gabapentin enacarbil and morphine administered in combination versus alone: a double-blind, randomized, pharmacokinetic, and tolerability comparison.
Chen C1, Upward J2, Arumugham T3, Stier B3, Davy M2. Clin Ther. 2015 Feb 1;37(2):349-57. doi: 10.1016/j.clinthera.2014.10.015. Epub 2014 Nov 20.
PURPOSE: Coadministration of morphine with oral gabapentin has been shown to increase plasma gabapentin concentrations. This study evaluated whether there was any interaction between gabapentin enacarbil (GEn), which is a prodrug of gabapentin, and morphine in terms of pharmacokinetics, pharmacodynamics, safety, and tolerability.
3.The Effect of Gabapentin Enacarbil on Quality of Life and Mood Outcomes in a Pooled Population of Adult Patients with Moderate-to-Severe Primary Restless Legs Syndrome.
Avidan AY1, Lee D2, Park M3, Jaros MJ4, Shang G5, Kim R5. CNS Drugs. 2016 Apr 11. [Epub ahead of print]
OBJECTIVE: The aim was to assess gabapentin enacarbil (GEn) treatment effects on quality of life (QOL) and mood in adults with moderate-to-severe primary restless legs syndrome (RLS).
4.Impact of Data Imputation Methodology on Pain Assessment over 24 Hours in a Randomized, Placebo-Controlled Study of Gabapentin Enacarbil in Patients with Neuropathic Pain Associated with Postherpetic Neuralgia.
Calkins AM1, Gudin J2, Gidal B3, Jaros MJ4, Kim R5, Shang G6. Pain Med. 2016 Jan 6. pii: pnv072. [Epub ahead of print]
OBJECTIVE: To assess the impact of gabapentin enacarbil on primary and secondary pain endpoints using three data imputation methodologies in a randomized phase II study of adult patients with postherpetic neuralgia.
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CAS 478296-72-9 Gabapentin enacarbil

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