LGM Pharma

Gabapentin Enacarbil

CAS No: 478296-72-9

Gabapentin Enacarbil

LGM Pharma is a Gabapentin Enacarbil 478296-72-9 active pharmaceutical ingredient supplier distributor, based in the USA.

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Product Details:

CAS No: 478296-72-9
Synonyms: ASP 8825, ASP8825, Gabapentin enacarbil, GSK 1838262, GSK1838262, Horizant, Regnite, Solzira, UNII-75OCL1SPBQ, XP 13512, XP-13512, XP13512
Molecular Weight: 329.3903 g/mol
PubChem: 9883933
Chemical Formula: C16-H27-N-O6
DrugBank: DB08872
Assay/Purity: Typically NLT 98%
IUPAC Name: 1-(((alpha-isobutanoyloxyethoxy)carbonyl)aminomethyl)-1-cyclohexaneacetic acid
SMILES: CC(C)C(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O
InChl: 1S/C16H27NO6/c1-11(2)14(20)22-12(3)23-15(21)17-10-16(9-13(18)19)7-5-4-6-8-16/h11-12H,4-10H2,1-3H3,(H,17,21)(H,18,19)

Additional Details: [+]

Indication:

For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).

Pharmacodynamics:

Since gabapentin enacarbil is a prodrug of gabapentin, it's physiological effects are the same as gabapentin. Concerning PHN, gabapentin prevents allodynia and hyperalgesia.

Mode of Action:

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.

Metabolism:

Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.

Toxicity:

Most common adverse reactions are headache, dizziness, and somnolence.

General Reference:

Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. [PubMed:15146029 ]


Gabapentin Enacarbil News:

  • Gabapentin Enacarbil, CAS# 478296-72-9, is also known as Horizant, which is marketed by GlaxoSmithKline.
  • Gabapentin enacarbil is the first medication in its class to be approved for the treatment of moderate-to-severe primary Restless Legs Syndrome.
  • The once daily dose of gabapentin enacarbil is typically taken at 5pm.
  • Symptoms of RLS tend to occur during periods of rest or inactivity, such as nighttime. There is currently no cure for this chronic condition.
  • Restless legs syndrome may also known as Willis-Ekbom disease, or WED.
  • RLS adversely affects 2-3 percent of the U.S. population.
  • One clinical trial of patients who received gabapentin enacarbil indicated that 67.6 percent of these patients reported a 30 percent reduction in pain associated with their RLS symptoms after being dosed with this drug.

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