Gabapentin enacarbil – clinical efficacy in restless legs syndrome

References

• NicholsDAAllenRPGraukeJHRestless legs syndrome symptoms in primary care: a prevalence studyArch Intern Med20031632323232914581252
   PubMed Web of Science ®Google Scholar
• AllenRPWaltersASMontplaisirJRestless legs syndrome prevalence and impact: REST general population studyArch Intern Med20051651286129215956009
   PubMed Web of Science ®Google Scholar
• HöglBKiechlSWilleitJRestless legs syndrome: a community-based study of prevalence, severity, and risk factorsNeurology2005641920192415955944
   PubMed Web of Science ®Google Scholar
• AllenRPicchierttiDHeningWRestless leg syndrome: diagnostic criteria, special considerations, and epidemiology A report from the restless legs syndrome diagnosis and epidemiology workshop at the National Institute of HealthSleep Med2003410111914592341
   PubMed Web of Science ®Google Scholar
• YeeBKillickRRestless legs SyndromeAustralian Family Physician20093829630019458798
   PubMedGoogle Scholar
• TrenkwalderCHeninigWAMontagnaPTreatment of restless legs syndrome: An evidence-based review and implications for clinical practiceMov Disord2008232267230218925578
   PubMed Web of Science ®Google Scholar
• Pfizer IncNeurontin Prescribing Information20071 http://www.pfizer.com/files/products/uspi_neurontin.pdfAccessed February 16, 2010
   Google Scholar
• McLeanMJGabapentin in the management of convulsive disordersEpilepsia199940Suppl 6S3950 discussion S73–7410530682
   PubMed Web of Science ®Google Scholar
• AnhutHAshmanPFeuersteinTJGabapentin (Neurontin) as add-on therapy in patients with partial seizures:a double-blind, placebo-controlled study. The International Gabapentin Study GroupEpilepsia1994357958018082624
   PubMed Web of Science ®Google Scholar
• IVAX launches gabapentin tablets. IVAX Corp Press Release . August 18, 2004.
   Google Scholar
• ThorpMLMorrisCDBagbySPA crossover study of gabapentin in treatment of restless legs syndrome among hemodialysis patientsAm J Kidney Dis20013810410811431189
   PubMed Web of Science ®Google Scholar
• MicozkadiogluHOzdemirFNKutASezerSSaatciUHaberalMGabapentin versus levodopa for the treatment of Restless Legs Syndrome in hemodialysis patients: an open-label studyRen Fail20042639339715462107
   PubMed Web of Science ®Google Scholar
• Garcia-BorregueroDLarrosaOde la LlaveYVergerKMasramonXHernandezGTreatment of restless legs syndrome with gabapentin: a double-blind, cross-over studyNeurology2002591573157912451200
   PubMed Web of Science ®Google Scholar
• HappeSKloschGSaletuBZeitlhoferJTreatment of idiopathic restless legs syndrome (RLS) with gabapentinNeurology2001571717171911706121
   PubMed Web of Science ®Google Scholar
• HappeSSauterCKloschGSaletuBZeitlhoferJGabapentin versus ropinirole in the treatment of idiopathic restless legs syndromeNeuropsychobiology200348828614504416
   PubMed Web of Science ®Google Scholar
• MellickGAMellickLBManagement of restless legs syndrome with gabapentin (Neurontin)Sleep1996192242268723380
   PubMed Web of Science ®Google Scholar
• MellickLBMellickGASuccessful treatment of reflex sympathetic dystrophy with gabapentinAm J Emerg Med199513967832967
   PubMed Web of Science ®Google Scholar
• BackonjaMBeydounAEdwardsKRGabapentin for the symptomatic treatment of painful neuropathy in patients with diabetes mellitus: a randomized controlled trialJAMA1998280183118369846777
   PubMed Web of Science ®Google Scholar
• PollackMHMatthewsJScottELGabapentin as a potential treatment for anxiety disordersAm J Psychiatry19981559929939659873
   PubMed Web of Science ®Google Scholar
• BockbraderHNBreslinEMUnderwoodBAMultiple-dose, dose-proportionality study of neurontin (gabapentin) in healthy volunteersEpilepsia199637Suppl 5159
   Google Scholar
• GidalBEDeCerceJBockbraderHNGabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsyEpilepsy Res19983191999714500
   PubMed Web of Science ®Google Scholar
• GidalBERadulovicLLKrugerSInter- and intra-subject variability in gabapentin absorption and absolute bioavailabilityEpilepsy Res20004012312710863139
   PubMed Web of Science ®Google Scholar
• BoydRATurckDAbelRBEffects of age and gender on single-dose pharmacokinetics of gabapentinEpilepsia19994047447910219274
   PubMed Web of Science ®Google Scholar
• Neurontin (gabapentin) capsule [package insert]. April 2009.
   Google Scholar
• StewartBHKuglerARThompsonPRA saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasmaPharm Res1993102762818456077
   PubMed Web of Science ®Google Scholar
• UchinoHKanaiYKim doKTransport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognitionMol Pharmacol20026172973711901210
   PubMed Web of Science ®Google Scholar
• RiceASMatonSPostherpetic Neuralgia Study GroupGabapentin in postherpetic neuralgia: a randomised, double blind, placebo controlled studyPain20019421522411690735
   PubMed Web of Science ®Google Scholar
• CundyKCBranchRChernov-RoganTXP13512 [(±)-1-([(α-Isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transportersJ Pharmacol Exp Ther200431131532315146028
   PubMed Web of Science ®Google Scholar
• RichterAAntonSEKochPThe impact of reducing dose frequency on health outcomesClin Ther2003252307233514512137
   PubMed Web of Science ®Google Scholar
• RiceASMatonSPostherpetic Neuralgia Study GroupGabapentin in postherpetic neuralgia: a randomised, double blind, placebo controlled studyPain20019421522411690735
   PubMed Web of Science ®Google Scholar
• EnersonBEDrewesLRMolecular features, regulation and function of monocarboxylate transporters: implications for drug deliveryJ Pharm Sci2003921531154412884241
   PubMed Web of Science ®Google Scholar
• WangHHuangWFeiYJHuman placental Na+-dependent multivitamin transporter: cloning, functional expression, gene structure and chromosomal localizationJ Biol Chem1999274148751488310329687
   PubMed Web of Science ®Google Scholar
• CundyKCSastrySLuoWClinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentinJ Clin Pharmacol2008481378138818827074
   PubMed Web of Science ®Google Scholar
• MerlinoGSerafiniAYoungJJGabapentin enacarbil, a gabapentin prodrug for the treatment of the neurological symptoms associated with disorders such as restless legs syndromeCurr Opin Investig Drugs20091091102
   PubMed Web of Science ®Google Scholar
• CundyKCAnnamalaiTBuLXP13512 [(±)-1-([(α-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 MonkeysJ Pharmacol Exp Ther200431132433315146029
   PubMed Web of Science ®Google Scholar
• BaillieJKPowerIThe mechanism of action of gabapentin in neuropathic painCurr Opin Investig Drugs2006713339
   Google Scholar
• TaylorCPGeeNSSuTZA summary of mechanistic hypotheses of gabapentin pharmacologyEpilepsy Res1998292332499551785
   PubMed Web of Science ®Google Scholar
• Suman-ChauhanNWebdaleLHillDRWoodruffGNCharacterisation of [3H]gabapentin binding to a novel site in rat brain: Homogenate binding studiesEur J Pharmacol19932442933018384570
   PubMed Web of Science ®Google Scholar
• JensenAAMosbacherJElgSThe anticonvulsant gabapentin (Neurontin) does not act through γ-aminobutyric acid-B receptorsMol Pharmacol2002611377138412021399
   PubMed Web of Science ®Google Scholar
• LanneauCGreenAHirstWDGabapentin is not a GABAB receptor agonistNeuropharmacology20014196597511747901
   PubMed Web of Science ®Google Scholar
• NgGYBertrandSSullivanRγ-Aminobutyric acid type B receptors with specific heterodimer composition and postsynaptic actions in hippocampal neurons are targets of anticonvulsant gabapentin actionMol Pharmacol20015914415211125035
   PubMed Web of Science ®Google Scholar
• BertrandSNgGYPurisaiMGThe anticonvulsant, antihyperalgesic agent gabapentin is an agonist at brain γ-aminobutyric acid type B receptors negatively coupled to voltage-dependent calcium channelsJ Pharmacol Exp Ther2001298152411408520
   PubMed Web of Science ®Google Scholar
• BertrandSNouelDMorinFGabapentin actions on Kir3 currents and N-type Ca2+ channels via GABAB receptors in hippocampal pyramidal cellsSynapse2003509510912923812
   PubMed Web of Science ®Google Scholar
• Mixcoatl-ZecuatlTMedina-SantillanRReyes-GarciaGEffect of K+ channel modulators on the antiallodynic effect of gabapentinEur J Pharmacol200448420120814744604
   PubMed Web of Science ®Google Scholar
• LeeC-HTsaiT-SLiouH-HGabapentin activates ROMK1 channels by a protein kinase A (PKA)-dependent mechanismBr J Pharmacol200815421622518311184
   PubMed Web of Science ®Google Scholar
• SinghLFieldMJFerrisPThe antiepileptic agent gabapentin (Neurontin) possesses anxiolytic-like and antinociceptive actions that are reversed by D-serinePsychopharmacology (Berl)1996127198880937
   PubMed Web of Science ®Google Scholar
• DissanayakeVUGeeNSBrownJPWoodruffGNSpermine modulation of specific [3H]-gabapentin binding to the detergent solubilized porcine cerebral cortex α2δ calcium channel subunitBr J Pharmacol19971208338409138689
   PubMed Web of Science ®Google Scholar
• FinkKDooleyDJMederWPInhibition of neuronal Ca2+ influx by gabapentin and pregabalin in the human neocortexNeuropharmacology20024222923611804619
   PubMed Web of Science ®Google Scholar
• ChenSREisenachJCMcCaslinPPPanHLSynergistic effect between intrathecal non-NMDA antagonist and gabapentin on allodynia induced by spinal nerve ligation in ratsAnesthesiology20009250050610691238
   PubMed Web of Science ®Google Scholar
• HayashidaKObataHNakajimaKEisenbachJCGabapentin acts within the locus coeruleus to alleviate neuropathic painAnesthesiology20081091077108419034104
   PubMed Web of Science ®Google Scholar
• TaylorCPLevyRHMattsonRHMeldrumBSPeruccaEGabapentin. Mechanism of actionAntiepileptic Drugs5th edPhiladelphiaLippincott Williams & Wilkins2002321334
   Google Scholar
• GeeNSBrownJPDissanayakeVUThe novel anticonvulsant drug, gabapentin (Neurontin), binds to the α2δ subunit of a calcium channelJ Biol Chem1996271576857768621444
   PubMed Web of Science ®Google Scholar
• HendrichJVan MinhATHeblichFPharmacological disruption of calcium channel trafficking by the α2δ ligand gabapentinPNAS20081053628363318299583
   PubMed Web of Science ®Google Scholar
• LalRSukbuntherngJLuoWPharmacokinetics and tolerability of single escalating doses of gabapentin enacarbil: a randomized-sequence, double-blind, placebo-controlled crossover study in healthy volunteersClin Ther2009311776178619808136
   PubMed Web of Science ®Google Scholar
• CanafaxDMMoorsTLCundyKCSingle- and multi-dose phase I studies of XP13512, a transported prodrug of gabapentin, demonstrate safety, tolerability and dose-proportional gabapentin pharmacokineticsInt Conf Mech Treatment Neuropathic Pain20041146
   Google Scholar
• CundyKSastryCKLuoWClinical pharmacokinetics of XP13512: A novel transported prodrug of gabapentinNeurology200870Suppl 1A293
   Google Scholar
• CundyKSastryCKLuoWClinical pharmacokinetics of XP13512: A summary of four healthy volunteer studiesSleep200831Suppl A268Abs 818
   Google Scholar
• FennerLJCanafaxDMMoorsTLA phase 1 randomized, cross over, single dose study of the safety, tolerability, and pharmacokinetics of XP13512 sustained released tablets vs Neurontin in healthy adult subjectsInt Conf Mech Treatment Neuropathic Pain20041146
   Google Scholar
• LalRSukbuntherngJLuoWClinical pharmacokinetic drug-interaction studies of XP13512, a novel transported prodrug of gabapentin, with naproxen and cimetidine [abstract]Neurology20087011Suppl 1A295
   Web of Science ®Google Scholar
• LalRSukbuntherngJLuoWClinical pharmacokinetics of gabapentin after oral administration of XP13512/GSK1838262 tablets and naproxen in healthy adultsJ Clin Pharmacol20084891124
   Web of Science ®Google Scholar
• KushidaCBeckerPPerkinsTXP13512 improves symptoms and sleep disturbance in RLS patients: Results of a 2-week, randomized, double blind, placebo controlled cross-over polysomnographic trialSleep200629Suppl SA278
   Google Scholar
• KushidaCAWaltersASBeckerPA randomized, double-blind, placebo-controlled, crossover study of XP13512/GSK1838262 in the treatment of patients with primary restless legs syndromeSleep20093215916819238802
   PubMed Web of Science ®Google Scholar
• EllenbogenALKushidaCABeckerPMXP13512/GSK1838262 1200 mg provides symptomatic relief in restless legs syndrome patients: A randomized, double-blind, placebo-controlled studyMov Disord2008231 Suppl S364Abs 1113
   Web of Science ®Google Scholar
• BeckerPKushidaCEllenbogenAXP13512 reduces restless legs syndrome symptoms and associated sleep impairment: Results of double blind, randomized, placebo-controlled studySleep200831Suppl A268Abs 817
   Google Scholar
• Xenoport and GlaxoSmithKline report positive top-line results of second phase III restless legs syndrome trial for XP13512/GSK1838262. XenoPort Inc. Press Release, Jan 15, 2008.
   Google Scholar
• XenoPort and GlaxoSmithKline report positive top-line results of final pivotal trail of XP13512/GSK1838262 for restless legs syndrome. XenoPort Inc. Press Release, Feb 28, 2008
   Google Scholar
• www.xenoport.com.
   Google Scholar