Gabapentin enacarbil

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Gabapentin enacarbil
File:XP-13512 structure.png
Systematic (IUPAC) name
1-(((alpha-isobutanoyloxyethoxy)carbonyl)aminomethyl)-1-cyclohexaneacetic acid
Clinical data
Routes of
administration
Oral
Pharmacokinetic data
Excretion Renal
Identifiers
CAS Number 478296-72-9
PubChem CID 9883933
Chemical data
Formula C16H27NO6
Molar mass 329.389 g/mol[[Script error: No such module "String".]]
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Gabapentin enacarbil (Horizant, XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.[1] It was designed for increased oral bioavailability over gabapentin,[2][3] and human trials showed it to produce extended release of gabapentin with almost twice the overall bioavailability,[4] especially when taken with a fatty meal.[5] Gabapentin enacarbil has passed human clinical trials for the treatment of restless legs syndrome, and initial results have shown it to be well tolerated and reasonably effective.[6][7][8]

Gabapentin enacarbil was denied approval by the FDA in February 2010, citing concerns about possible increased cancer risk shown by some animal studies. Similar concerns had been raised about gabapentin itself in the past, but were felt to be outweighed by its clinical utility as an anticonvulsant, whereas the treatment of restless legs syndrome was not seen to justify the same kind of risk.[9]

References

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  1. Landmark CJ, Johannessen SI (2008). "Modifications of antiepileptic drugs for improved tolerability and efficacy". Perspectives in Medicinal Chemistry. 2: 21–39. PMC 2746576Freely accessible. PMID 19787095. 
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  9. GlaxoSmithKline/XenoPort: FDA setback halts gabapentin reformulations