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dorzolamide

Trade name: trusopt

Small moleculeapproved

Approved

Dec 9, 1994

Dorzolamide is a sulfonamide and a highly specific carbonic anhydrase II (CA-II) inhibitor, which is the main CA isoenzyme involved in aqueous humor secretion. Dorzolamide is marketed under the trade name Trusopt, indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II), found primarily in red blood cells (RBCs), but also in other tissues. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure (IOP). TRUSOPT Ophthalmic Solution contains dorzolamide hydrochloride, an inhibitor of human carbonic anhydrase II. Following topical ocular administration, TRUSOPT reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. — NCATS

Clinical trial activity

74 trials · 63 clinical orgs · 31 marketing orgs

Phase 1
2
Phase 2
23
Phase 3
19
Phase 4
36

Earliest trial started May 1, 1999 (NCT00991822)

Timeline

1990s

  1. Dec 9, 1994

    Merck — Earliest FDA Approval

  2. Dec 9, 1994

    Merck — NDA Organization

  3. Dec 9, 1994

    Merck — Marketing Organization

  4. Apr 7, 1998

    Akorn, Inc. — NDA Secondary Org

  5. Apr 7, 1998

    Thea Pharma — NDA Secondary Org

  6. Jan 1, 1999

    Earliest Phase 2 Sponsor(trial)

2000s

  1. Jan 1, 2005

    Merck — Earliest Phase 3 Sponsor(trial)

  2. Oct 28, 2008

    Apotex — Marketing Organization

  3. Oct 28, 2008

    Hi Tech Pharmaceuticals — Marketing Organization

  4. Oct 28, 2008

    Rubicon Research — Marketing Organization

  5. Oct 28, 2008

    Hikma — Marketing Organization

  6. Nov 6, 2008

    Sandoz — Marketing Organization

  7. Nov 6, 2008

    Novartis — Marketing Organization

  8. Dec 4, 2008

    Teva — Marketing Organization

  9. Jun 25, 2009

    Bausch & Lomb — Marketing Organization

  10. Nov 18, 2009

    Sankyo — Marketing Organization

  11. Nov 18, 2009

    Lutipold — Marketing Organization

  12. Nov 18, 2009

    Daiichi Sankyo — Marketing Organization

2010s

  1. Dec 4, 2013

    Zambon — Marketing Organization

  2. Sep 3, 2014

    Indoco Remedies — Marketing Organization

  3. Sep 3, 2014

    Watson Pharmaceuticals — Marketing Organization

  4. Sep 22, 2014

    Akorn, Inc. — Marketing Organization

  5. Sep 22, 2014

    Epic Pharma Llc — Marketing Organization

  6. Dec 17, 2014

    Lannett Company, Inc. — Marketing Organization

  7. Dec 17, 2014

    Chartwell Pharmaceuticals — Marketing Organization

  8. Jan 1, 2016

    Earliest Phase 1 Sponsor(trial)

  9. Jul 24, 2018

    Aurobindo Pharma — Marketing Organization

  10. Jul 24, 2018

    Eugia Pharma — Marketing Organization

  11. Jan 24, 2019

    FDC — Marketing Organization

  12. Jun 25, 2019

    Somerset Pharmaceuticals — Marketing Organization

  13. Jun 25, 2019

    ANDA Repository — Marketing Organization

  14. Jun 25, 2019

    Mylan — Marketing Organization

  15. Aug 9, 2019

    Alembic — Marketing Organization

  16. Nov 8, 2019

    Micro Labs Ltd India — Marketing Organization

2020s

  1. Jan 27, 2022

    Gland Pharma Ltd — Marketing Organization

  2. Jan 27, 2022

    Fosun — Marketing Organization

  3. May 1, 2023

    Ingenus Pharmaceuticals — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • cosopt

    with timolol

    Also known as cosopt pf

Approval history

  • approvedPriority reviewDec 9, 1994

Chemistry & pharmacology

Loading structure…

SMILES

CCN[C@H]1C[C@H](C)S(=O)(=O)c2sc(S(N)(=O)=O)cc21
Mol. weight
324.45 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Sources

Also known as

  • 4-ethylamino-5,6-dihydro-6-methyl-7,7-dioxide-4h-thieno(2,3-b)thiopyran-2-sulfonamide
  • 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • (4s,6s)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • (4s,6s)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4s,6s-dorzolamide
  • 4s,6s-dorzolamide
  • (4s-trans)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
  • (4s-trans)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
  • (4s,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide
  • (4s,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide
  • 5,6-dihydro-4-ethylamino-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
  • cosopt
  • cosopt
  • cosopt pf
  • de-111
  • dorzant
  • dorzolamid
  • dorzolamid
  • dorzolamida
  • dorzolamida
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide
  • dorzolamide chibret
  • dorzolamide hcl
  • dorzolamide hcl
  • dorzolamide hcl
  • dorzolamide hydrochloride
  • dorzolamide hydrochloride
  • dorzolamide hydrochloride
  • dorzolamide hydrochloride
  • dorzolamide hydrochloride
  • dorzolamide hydrochloride
  • dorzolamide maleate
  • dorzolamide, (trans)-isomer
  • dorzolamidum
  • dorzolamidum
  • l 671152
  • l-671,152
  • mk0507
  • mk 507
  • mk-507
  • mk-507
  • mk-507
  • trusopt
  • trusopt
  • trusopt
  • trusopt

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06883123Phase 4May 14, 2025Prairie Eye Center, Sengi
NCT06369077Phase 4Apr 22, 2024CT Glaucoma Associates
NCT06177678Phase 2Feb 29, 2024Kukje Pharma
NCT05857267Phase 4Mar 7, 2023Laboratorios Poen
NCT05083689Phase 2/Phase 3 (Phase 3)Oct 6, 2021Shahid Beheshti University of Medical Sciences
NCT04702789Phase 4May 1, 2021Laboratorios Sophia S.A de C.V.
NCT04676126Phase 4Jan 31, 2021Guardion Health Sciences, Inc., Sponsel Foundation, University of the Incarnate Word
NCT04448223Phase 2Jun 11, 2020Chong Kun Dang Pharmaceutical, Seoul National University
NCT03193333Phase 3Aug 4, 2017Laboratorios Sophia S.A de C.V.
NCT02852057Phase 1May 1, 2017University of Florida
NCT05973318Phase 3Apr 10, 2017Government of Tatarstan, University Hospital, Rijeka
NCT05973305Phase 3Apr 5, 2017Government of Tatarstan, University Hospital, Rijeka
NCT03034772Phase 2/Phase 3 (Phase 3)Feb 8, 2017Mid-Atlantic Retina Consultations, Inc., Thomas Jefferson University
NCT02967614Phase 1Dec 1, 2016Kukje Pharma, Seoul National University
NCT02802137Phase 4Mar 1, 2015Aristotle University of Thessaloniki
NCT02325518Phase 4Dec 1, 2014Alcon, Novartis
NCT02571972Phase 2Oct 1, 2014J. Arch McNamara Research Fund, Mid-Atlantic Retina Consultations, Inc., Thomas Jefferson University
NCT02390284Phase 3Sep 1, 2014National Eye Institute (NEI), University of Miami
NCT02522039N/AMay 1, 2014University of Copenhagen
NCT03966560Phase 4Jan 31, 2014Afyon Kocatepe University
Showing 20 of 74 trials
Page 1 / 4

Organizations

Research & Development (63)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
AlconFor profit111022005
MerckFor profit9542005
AllerganFor profit4322005
PRN Pharmacuetical Research Network, LLCFor profit4412005
Aristotle University of ThessalonikiAcademic/Hospital3312006
Laboratorios Sophia S.A de C.V.For profit3332006
Mid-Atlantic Retina Consultations, Inc.Academic/Hospital3132010
Santen Inc.For profit3312011
Thomas Jefferson UniversityAcademic/Hospital3232011
Government of TatarstanGovernment2012017
Johannes Gutenburg UniversityAcademic/Hospital2122009
Kukje PharmaFor profit2222016
Seoul National UniversityAcademic/Hospital2022016
University Hospital, RijekaAcademic/Hospital2212017
University of ViennaAcademic/Hospital2221999
Aarhus UniversityAcademic/Hospital1112007
Advanced Glaucoma SpecialistsAcademic/Hospital1112006
Afyon Kocatepe UniversityAcademic/Hospital1112014
Alfred E. Tiefenbacher (GmbH & Co. KG)For profit1112009
Alleanza Pharmaceuticals, Inc.For profit1112013
63 organizations
Page 1 / 4

Marketing (38)

OrganizationOrg typeRelationshipDate
ANDA RepositoryFor profitMKTGJun 25, 2019
Akorn, Inc.For profitSYNApr 7, 1998
Akorn, Inc.For profitMKTGSep 22, 2014
Akorn, Inc.For profitNDA2Apr 7, 1998
AlembicFor profitMKTGAug 9, 2019
AlembicFor profitSYNAug 9, 2019
ApotexFor profitMKTGOct 28, 2008
Aurobindo PharmaFor profitMKTGJul 24, 2018
Bausch & LombFor profitMKTGJun 25, 2009
Chartwell PharmaceuticalsFor profitMKTGDec 17, 2014
Daiichi SankyoFor profitMKTGNov 18, 2009
Epic Pharma LlcFor profitMKTGSep 22, 2014
Eugia PharmaFor profitMKTGJul 24, 2018
FDCFor profitMKTGJan 24, 2019
FosunFor profitMKTGJan 27, 2022
Gland Pharma LtdFor profitMKTGJan 27, 2022
Hi Tech PharmaceuticalsFor profitMKTGOct 28, 2008
HikmaFor profitMKTGOct 28, 2008
Indoco RemediesFor profitMKTGSep 3, 2014
Ingenus PharmaceuticalsFor profitMKTGMay 1, 2023
Lannett Company, Inc.For profitMKTGDec 17, 2014
LutipoldFor profitMKTGNov 18, 2009
MerckFor profitSYNDec 9, 1994
MerckFor profitNDADec 9, 1994
MerckFor profitMKTGDec 9, 1994
Micro Labs Ltd IndiaFor profitMKTGNov 8, 2019
MylanFor profitMKTGJun 25, 2019
NovartisFor profitMKTGNov 6, 2008
Rubicon ResearchFor profitMKTGOct 28, 2008
SandozFor profitMKTGNov 6, 2008
SandozFor profitSYNNov 6, 2008
SankyoFor profitMKTGNov 18, 2009
Somerset PharmaceuticalsFor profitMKTGJun 25, 2019
Somerset PharmaceuticalsFor profitSYNJun 25, 2019
TevaFor profitMKTGDec 4, 2008
Thea PharmaFor profitNDA2Apr 7, 1998
Watson PharmaceuticalsFor profitMKTGSep 3, 2014
ZambonFor profitMKTGDec 4, 2013