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flumazenil

Trade name: mazicon

Small moleculeapproved

Approved

Dec 20, 1991

Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system. Fumazenil is used for the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, and where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures. Also for the management of benzodiazepine overdose as an adjunct for appropriate supportive and symptomatic measures. Flumazenil went off patent in 2008 so at present generic formulations of this drug are available. — NCATS

Clinical trial activity

33 trials · 34 clinical orgs · 12 marketing orgs

Phase 1
15
Phase 2
8
Phase 3
1
Phase 4
5

Earliest trial started Jan 1, 1993 (NCT00000246)

Timeline

1990s

  1. Dec 20, 1991

    Roche — Earliest FDA Approval

  2. Dec 20, 1991

    Roche — NDA Organization

  3. Jan 1, 1993

    Earliest Phase 2 Sponsor(trial)

2000s

  1. Oct 12, 2004

    Teva — Marketing Organization

  2. Oct 12, 2004

    West-Ward Pharmaceutical — Marketing Organization

  3. Oct 12, 2004

    Baxalta — Marketing Organization

  4. Oct 12, 2004

    Fresenius — Marketing Organization

  5. Oct 12, 2004

    Dr. Reddy's Laboratories — Marketing Organization

  6. May 3, 2005

    Sandoz — Marketing Organization

  7. May 3, 2005

    Novartis — Marketing Organization

  8. Jan 1, 2006

    Earliest Phase 1 Sponsor(trial)

  9. May 13, 2008

    Rising Pharmaceuticals — Marketing Organization

  10. May 13, 2008

    Mylan — Marketing Organization

  11. Mar 23, 2009

    Hikma — Marketing Organization

2010s

  1. Aug 28, 2012

    Sagent Pharmaceuticals, Inc. — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewDec 20, 1991

Chemistry & pharmacology

Loading structure…

SMILES

CCOC(=O)C1=C2CN(C)C(=O)C3=CC(F)=CC=C3N2C=N1
Mol. weight
303.2884 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warning

Sources

Also known as

  • 11c-flumazenil
  • 11c-flumazenil
  • anexate
  • anexate
  • anexate
  • anexate
  • anexate
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenil
  • flumazenilo
  • flumazenilo
  • flumazenilum
  • flumazenilum
  • flumazepil
  • flumazepil
  • flumazepil
  • flumazepil
  • lanexat
  • lanexat
  • mazicon
  • mazicon
  • mazicon
  • mazicon
  • mazicon
  • ro-151788
  • ro-151788
  • ro-15-1788
  • ro-151788000
  • ro-151788000
  • romazicon
  • romazicon

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07265050N/AJan 1, 2026Seoul National University
NCT07277881Phase 4Dec 31, 2025Medical University of Gdansk
NCT06531369Phase 1Jul 31, 2024Shandong Province Qianfoshan Hospital
NCT06205719Early Phase 1 (Phase 1)Jun 1, 2024Sichuan University
NCT05939674N/ASep 19, 2023Pusan National University
NCT06563063N/AAug 23, 2023Yonsei University
NCT05681377Phase 4Mar 5, 2023Korea University
NCT06513923Phase 4Feb 1, 2023Central South University
NCT05435911N/AAug 2, 2022Seoul National University
NCT05397886N/AAug 1, 2022Seoul National University
NCT05382806N/AJun 1, 2022Konkuk University
NCT05468671Phase 4Jan 4, 2021Chinese Academy of Medical Sciences
NCT04329585N/AMar 25, 2020National Taiwan University
NCT03959189Phase 1May 31, 2019Expansion Therapeutics, Inc., University of California, San Francisco
NCT03743805Early Phase 1 (Phase 1)Jan 1, 2019University of South Carolina
NCT03462641Phase 1/Phase 2 (Phase 2)Mar 9, 2018National Institute of Neurological Disorders and Stroke (NINDS), University of Michigan
NCT04308954Phase 1Nov 1, 2016Stanford University
NCT02899156Phase 4Mar 1, 2016University of California, Davis
NCT02696512Phase 1/Phase 2 (Phase 2)Mar 1, 2016International Brain Research Foundation
NCT02690389N/AJan 1, 2015Sichuan Cancer Hospital and Research Institute, Sichuan University, University of Electronic Science and Technology of China
Showing 20 of 33 trials
Page 1 / 2

Organizations

Research & Development (34)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Seoul National UniversityAcademic/Hospital3312022
AstraZenecaFor profit2212008
Coeruleus Ltd.For profit2222010
Sichuan UniversityAcademic/Hospital2122015
University of South CarolinaAcademic/Hospital2222005
Yale UniversityAcademic/Hospital2211993
Central South UniversityAcademic/Hospital1112023
Chinese Academy of Medical SciencesAcademic/Hospital1112021
Emory UniversityAcademic/Hospital1112010
Expansion Therapeutics, Inc.For profit1112019
Georgia Research AllianceAcademic/Hospital1012010
International Brain Research FoundationAcademic/Hospital1112016
Konkuk UniversityAcademic/Hospital1112022
Korea UniversityAcademic/Hospital1112023
Medical University of GdanskAcademic/Hospital1112025
Medical University of South CarolinaAcademic/Hospital1012005
National Institute of Neurological Disorders and Stroke (NINDS)Government1012018
National Institute on Drug Abuse (NIDA)Government1011993
National Institutes of Health (NIH)Government1012006
National Taiwan UniversityAcademic/Hospital1112020
34 organizations
Page 1 / 2

Marketing (16)

OrganizationOrg typeRelationshipDate
BaxaltaFor profitMKTGOct 12, 2004
Dr. Reddy's LaboratoriesFor profitMKTGOct 12, 2004
FreseniusFor profitMKTGOct 12, 2004
HikmaFor profitSYNOct 12, 2004
HikmaFor profitMKTGMar 23, 2009
HikmaFor profitSYNOct 12, 2004
MylanFor profitMKTGMay 13, 2008
NovartisFor profitMKTGMay 3, 2005
Rising PharmaceuticalsFor profitSYNMay 13, 2008
Rising PharmaceuticalsFor profitMKTGMay 13, 2008
RocheFor profitNDADec 20, 1991
Sagent Pharmaceuticals, Inc.For profitMKTGAug 28, 2012
SandozFor profitMKTGMay 3, 2005
SandozFor profitSYNMay 3, 2005
TevaFor profitMKTGOct 12, 2004
West-Ward PharmaceuticalFor profitMKTGOct 12, 2004