Gabapentin enacarbil

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[[]]

Gabapentin enacarbil (Horizant, XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. It was designed for increased oral bioavailability over gabapentin, and human trials showed it to produce extended release of gabapentin with almost twice the overall bioavailability, especially when taken with a fatty meal. 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.

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.