Gabapentin enacarbil (XP13512/GSK1838262) as an alternative treatment to dopaminergic agents for restless legs syndrome.

IMPORTANCE TO THE FIELD: Gabapentin enacarbil (XP13512/GSK1838262) is being explored as an alternative treatment for restless legs syndrome (RLS), which currently relies heavily on dopaminergic agents; however, these latter medications have the reported complications of augmentation. Gabapentin enacarbil shows promising data that it may be equally to more efficacious and have an improved side effect profile than treatment with dopaminergic agents. AREAS COVERED IN THIS REVIEW: Gabapentin enacarbil, examined in studies from 2004 to 2009, is a precursor to gabapentin and overcomes gabapentin's unfavorable pharmacokinetic profile and dose-dependent bioavailability. Randomized, controlled studies published in 2009 showed that gabapentin enacarbil outperformed placebo in improving quality and duration of sleep based on subjective report, investigator observation and objective measures in clinical trials. These trials show gabapentin enacarbil is well tolerated and safe, with a side-effect profile similar to gabapentin. WHAT THE READER WILL GAIN: The reader will gain a thorough understanding of the current treatments available for RLS and how gabapentin enacarbil offers a potential breakthrough in expanding on these treatment options for both improved efficacy and tolerability. TAKE HOME MESSAGE: Based on these findings, gabapentin enacarbil offers a promising alternative treatment for individuals requiring pharmacological intervention for their RLS symptoms.