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gabapentin

Trade name: neurontin

Small moleculeapproved

Approved

Dec 30, 1993

Gabapentin enacarbil (Horizant in USA, Regnite in Japan), is a prodrug of gabapentin, an antiepileptic drug (AED). It was designed for increased oral bioavailability over gabapentin and to be transported through two high capacity transporters in the intestine, sodium-dependent multivitamin transporter (SMVT) and MCT1. It was shown that the prodrug is a substrate for both MCT1 and SMVT. The oral bioavailability of gabapentin following the administration of its prodrug was found to be 84.2% compared with 25.4% after a similar oral dose of gabapentin. Discovered and developed by XenoPort, gabapentin enacarbil was approved in the United States in 2011 for the treatment of moderate-to-severe primary restless legs syndrome (RLS) in adults and in June 2012 for the management of postherpetic neuralgia (PHN) in adults. Therapeutic effects of gabapentin enacarbil in RLS and PHN are attributable to gabapentin. The precise mechanism by which gabapentin is efficacious in RLS and PHN is unknown. In vitro studies have shown that gabapentin binds with high affinity to certain parts of voltage-activated calcium channels in the central nervous system. However, the relationship of this binding to the therapeutic effects of gabapentin enacarbil in RLS and PHN is unknown. The most common adverse reactions for adult patients with moderate-to-severe primary RLS and PHN receiving Horizant were somnolence/sedation, dizziness, headache, nausea and fatigue. — NCATS

Clinical trial activity

462 trials · 347 clinical orgs · 56 marketing orgs

Phase 1
51
Phase 2
154
Phase 3
102
Phase 4
129

Earliest trial started May 1, 1995 (NCT00001482)

Timeline

1990s

  1. Dec 30, 1993

    Warner Lambert — Earliest FDA Approval

  2. Dec 30, 1993

    Viatris — Marketing Organization

  3. Dec 30, 1993

    Warner Lambert — NDA Organization

  4. Dec 30, 1993

    Pfizer — NDA Secondary Org

  5. Dec 30, 1993

    Upjohn — Marketing Organization

  6. Dec 30, 1993

    Viatris — NDA Secondary Org

  7. Jan 1, 1995

    Earliest Phase 2 Sponsor(trial)

  8. Jan 1, 1997

    Actavis — Earliest Phase 1 Sponsor(trial)

  9. Jan 1, 1998

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Mar 2, 2000

    Parke-Davis — NDA Secondary Org

  2. Sep 12, 2003

    Actavis — Marketing Organization

  3. Apr 28, 2004

    Teva — Marketing Organization

  4. Mar 23, 2005

    Shijiazhuang Pharma Group (CSPC) — Marketing Organization

  5. Apr 6, 2005

    Apotex — Marketing Organization

  6. Apr 6, 2005

    Sandoz — Marketing Organization

  7. Apr 6, 2005

    Granules India — Marketing Organization

  8. Apr 6, 2005

    Novartis — Marketing Organization

  9. Sep 14, 2005

    Ranbaxy — Marketing Organization

  10. Oct 7, 2005

    Sun Pharmaceuticals — Marketing Organization

  11. Jul 6, 2006

    Invatech — Marketing Organization

  12. Aug 18, 2006

    Glenmark Pharmaceuticals — Marketing Organization

  13. Sep 13, 2006

    Rubicon Research — Marketing Organization

  14. May 11, 2007

    Watson Pharmaceuticals — Marketing Organization

  15. Jul 25, 2007

    Amneal Pharmaceuticals — Marketing Organization

  16. Sep 25, 2007

    Hikma — Marketing Organization

  17. Jan 31, 2008

    Aurobindo Pharma — Marketing Organization

  18. Dec 30, 2009

    Invagen Pharms — Marketing Organization

2010s

  1. Jun 1, 2010

    Mylan — Marketing Organization

  2. Jan 28, 2011

    Alvogen — Marketing Organization

  3. Jan 28, 2011

    Assertio — NDA Secondary Org

  4. Jan 28, 2011

    Alvogen — NDA Secondary Org

  5. Feb 11, 2011

    Zydus Discovery DMCC — Marketing Organization

  6. Feb 18, 2011

    Akorn, Inc. — Marketing Organization

  7. Feb 18, 2011

    Hi Tech Pharmaceuticals — Marketing Organization

  8. Feb 18, 2011

    Mission Pharmacal — Marketing Organization

  9. Apr 6, 2011

    Azurity — Marketing Organization

  10. Apr 6, 2011

    Arbor Pharmaceuticals — NDA Secondary Org

  11. Apr 6, 2011

    Azurity — NDA Secondary Org

  12. Jul 21, 2011

    Marksans Pharma — Marketing Organization

  13. May 1, 2012

    Acella Pharmaceuticals — Marketing Organization

  14. Jul 12, 2013

    ACI Limited — Marketing Organization

  15. Aug 2, 2013

    Taro Pharmaceuticals — Marketing Organization

  16. Dec 23, 2015

    Alkem Labs Ltd — Marketing Organization

  17. Feb 4, 2016

    Sciegen Pharmaceticals — Marketing Organization

  18. Mar 14, 2016

    Belcher Pharmaceuticals — Marketing Organization

  19. Mar 14, 2016

    Tris Pharma, Inc. — Marketing Organization

  20. Mar 24, 2017

    Epic Pharma Llc — Marketing Organization

  21. Mar 24, 2017

    Graviti Pharmaceuticals — Marketing Organization

  22. Oct 26, 2017

    Chartwell Pharmaceuticals — Marketing Organization

  23. Oct 26, 2017

    Hengrui Therapeutics, Inc. — Marketing Organization

  24. Oct 26, 2017

    Jiangsu Wuzhong Pharmaceutical Group Co., Ltd. — Marketing Organization

  25. Aug 24, 2018

    Lupin — Marketing Organization

  26. Oct 16, 2018

    Strides Pharma Science — Marketing Organization

  27. Dec 3, 2019

    Pharmaceutical Associates — Marketing Organization

  28. Dec 3, 2019

    Novitium Pharma — Marketing Organization

  29. Dec 3, 2019

    VistaPharm, Inc. — Marketing Organization

2020s

  1. Aug 17, 2020

    Zhejiang Yongtai — Marketing Organization

  2. May 10, 2021

    Ascent Pharmahealth — Marketing Organization

  3. May 10, 2021

    AbbVie — Marketing Organization

  4. May 12, 2023

    Laurus Labs Ltd — Marketing Organization

  5. Jul 19, 2023

    Rising Pharmaceuticals — Marketing Organization

  6. Nov 20, 2023

    IPCA Laboratories Ltd. — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewDec 30, 1993

Chemistry & pharmacology

Loading structure…

SMILES

NCC1(CC(O)=O)CCCCC1
Mol. weight
171.2368 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Prodrug

Sources

Also known as

  • 1-(((alpha-isobutanoyloxyethoxy)carbonyl)aminomethyl)-1-cyclohexaneacetic acid
  • 1-(aminomethyl)cyclohexaneacetic acid
  • 1-(aminomethyl)cyclohexaneacetic acid
  • 1-(aminomethyl)cyclohexaneacetic acid
  • apo-gabapentin
  • asp8825
  • asp8825
  • carbatin
  • ci-945
  • ci-945
  • convalis
  • f0434
  • gabamox
  • gabapen
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentin
  • gabapentina
  • gabapentina
  • gabapentina enacarbilo
  • gabapentina enacarbilo
  • gabapentine
  • gabapentine
  • gabapentine
  • gabapentine enacarbil
  • gabapentine enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin enacarbil
  • gabapentin gr
  • gabapentin gr
  • gabapentin hexal
  • gabapentino
  • gabapentino
  • gabapentin-ratiopharm
  • gabapentin stada
  • gabapentinum
  • gabapentinum
  • gabapentinum enacarbilum
  • gabapentinum enacarbilum
  • gabapetin
  • gabapetin
  • gavinda
  • goe-3450
  • goe-3450
  • gralise
  • gralise
  • gsk1838262
  • gsk1838262
  • horizant
  • horizant
  • horizant
  • horizant
  • horizant
  • neurontin
  • neurontin
  • neurontin
  • neurontin
  • neurontin
  • novo-gabapentin
  • pms-gabapentin
  • regnite
  • regnite
  • xp10569
  • xp 10569
  • xp-10569
  • xp11084
  • xp 11084
  • xp-11084
  • xp11239
  • xp 11239
  • xp-11239
  • xp12464
  • xp 12464
  • xp-12464
  • xp13512
  • xp13512
  • xp13512
  • xp13512
  • xp 13512
  • xp-13512
  • xp-13512
  • xp-13512

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07158476Phase 4Oct 21, 2025St. Louis University
NCT06997016Phase 4Oct 15, 2025Baylor University
NCT07206680N/AOct 1, 2025Cairo University
NCT07047040Phase 2/Phase 3 (Phase 3)Aug 15, 2025Assiut University
NCT07131527N/AJul 14, 2025Sohag University
NCT07063082N/AJul 7, 2025Cairo University
NCT06975345N/AJul 2, 2025Universitat Internacional de Catalunya, University of Zaragoza, Wroclaw University of Health and Sport Sciences
NCT07029854N/AJun 18, 2025Cairo University
NCT06992427Phase 3Jun 5, 2025National Cancer Institute (NCI)
NCT06991153N/AMay 29, 2025Cairo University
NCT06893172N/AApr 1, 2025Ho Chi Minh City University of Medicine and Pharmacy
NCT06887998Phase 3Mar 31, 2025Cairo University
NCT06882291N/AMar 20, 2025Cairo University
NCT07019103N/AMar 2, 2025Hawler Medical University
NCT06781489Phase 4Feb 19, 2025Universidad Europea de Madrid
NCT06778798Phase 4Feb 19, 2025Universidad Europea de Madrid
NCT06812650N/AFeb 3, 2025Karabuk University
NCT06798662N/AFeb 1, 2025Inner Mongolia Baogang Hospital
NCT07045038N/AJan 20, 2025Cairo University
NCT06849479N/AJan 1, 2025Cairo University
Showing 20 of 462 trials
Page 1 / 24

Organizations

Research & Development (347)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
PfizerFor profit252042002
Cairo UniversityAcademic/Hospital222032015
XenoPort, Inc.For profit211942006
GlaxoSmithKlineFor profit18242006
Mayo ClinicAcademic/Hospital10642001
National Cancer Institute (NCI)Government10532001
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government10332001
Tanta UniversityAcademic/Hospital101042016
AssertioFor profit9842006
Department of Veteran AffairsGovernment8741998
Medical University of South CarolinaAcademic/Hospital8332001
National Institute on Drug Abuse (NIDA)Government8132006
AstellasFor profit7742007
Harvard UniversityAcademic/Hospital7722012
University of CopenhagenAcademic/Hospital7622005
University of RochesterAcademic/Hospital7542001
ActavisFor profit6611997
Ain Shams UniversityAcademic/Hospital6642016
Columbia UniversityAcademic/Hospital6522000
PRACSFor profit6011997
347 organizations
Page 1 / 18

Marketing (72)

OrganizationOrg typeRelationshipDate
ACI LimitedFor profitMKTGJul 12, 2013
ACI LimitedFor profitMKTGJul 12, 2013
AbbVieFor profitMKTGMay 10, 2021
Acella PharmaceuticalsFor profitMKTGMay 1, 2012
ActavisFor profitMKTGSep 12, 2003
Akorn, Inc.For profitMKTGFeb 18, 2011
Alkem Labs LtdFor profitMKTGDec 23, 2015
Alkem Labs LtdFor profitSYNDec 17, 2010
AlvogenFor profitMKTGJan 28, 2011
AlvogenFor profitNDA2Jan 28, 2011
Amneal PharmaceuticalsFor profitSYNMar 23, 2012
Amneal PharmaceuticalsFor profitMKTGJul 25, 2007
ApotexFor profitMKTGApr 6, 2005
Arbor PharmaceuticalsFor profitNDA2Apr 6, 2011
Ascent PharmahealthFor profitMKTGMay 10, 2021
AssertioFor profitNDA2Jan 28, 2011
Aurobindo PharmaFor profitMKTGJan 31, 2008
Aurobindo PharmaFor profitSYNJan 31, 2008
AzurityFor profitMKTGApr 6, 2011
AzurityFor profitNDA2Apr 6, 2011
Belcher PharmaceuticalsFor profitMKTGMar 14, 2016
Chartwell PharmaceuticalsFor profitMKTGOct 26, 2017
Epic Pharma LlcFor profitMKTGMar 24, 2017
GlaxoSmithKlineFor profitSYNApr 6, 2011
Glenmark PharmaceuticalsFor profitMKTGAug 18, 2006
Granules IndiaFor profitSYNApr 6, 2005
Granules IndiaFor profitMKTGApr 6, 2005
Graviti PharmaceuticalsFor profitMKTGMar 24, 2017
Hengrui Therapeutics, Inc.For profitMKTGOct 26, 2017
Hi Tech PharmaceuticalsFor profitMKTGFeb 18, 2011
HikmaFor profitMKTGSep 25, 2007
HikmaFor profitSYNJul 21, 2011
IPCA Laboratories Ltd.For profitMKTGNov 20, 2023
Invagen PharmsFor profitMKTGDec 30, 2009
InvatechFor profitMKTGJul 6, 2006
Jiangsu Wuzhong Pharmaceutical Group Co., Ltd.For profitMKTGOct 26, 2017
Laurus Labs LtdFor profitMKTGMay 12, 2023
LupinFor profitMKTGAug 24, 2018
Marksans PharmaFor profitMKTGJul 21, 2011
Mission PharmacalFor profitMKTGFeb 18, 2011
MylanFor profitSYNFeb 14, 2011
MylanFor profitMKTGJun 1, 2010
NovartisFor profitMKTGApr 6, 2005
Novitium PharmaFor profitMKTGDec 3, 2019
Parke-DavisFor profitNDA2Mar 2, 2000
PfizerFor profitNDA2Dec 30, 1993
Pharmaceutical AssociatesFor profitMKTGDec 3, 2019
RanbaxyFor profitMKTGSep 14, 2005
Rising PharmaceuticalsFor profitMKTGJul 19, 2023
Rubicon ResearchFor profitMKTGSep 13, 2006
SandozFor profitMKTGApr 6, 2005
Sciegen PharmaceticalsFor profitMKTGFeb 4, 2016
Shijiazhuang Pharma Group (CSPC)For profitMKTGMar 23, 2005
Strides Pharma ScienceFor profitMKTGOct 16, 2018
Sun PharmaceuticalsFor profitMKTGOct 7, 2005
Sun PharmaceuticalsFor profitSYNJun 30, 2005
Taro PharmaceuticalsFor profitSYNJul 3, 2013
Taro PharmaceuticalsFor profitMKTGAug 2, 2013
TevaFor profitSYNDec 15, 2004
TevaFor profitSYNApr 28, 2004
TevaFor profitSYNOct 8, 2004
TevaFor profitSYNMar 10, 2017
TevaFor profitMKTGApr 28, 2004
Tris Pharma, Inc.For profitMKTGMar 14, 2016
UpjohnFor profitMKTGDec 30, 1993
ViatrisFor profitMKTGDec 30, 1993
ViatrisFor profitNDA2Dec 30, 1993
VistaPharm, Inc.For profitMKTGDec 3, 2019
Warner LambertFor profitNDADec 30, 1993
Watson PharmaceuticalsFor profitMKTGMay 11, 2007
Zhejiang YongtaiFor profitMKTGAug 17, 2020
Zydus Discovery DMCCFor profitMKTGFeb 11, 2011