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timolol

Trade name: blocadren

Small moleculeapproved

Approved

Aug 17, 1978

Timolol is the non-selective Beta antagonist used as eye drops to treat increased pressure inside the eye such as in ocular hypertension and glaucoma. Timolol is also used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines. Timolol is a beta1 and beta2 (non-selective) adrenergic receptor antagonist that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Timolol, when applied topically on the eye, has the action of reducing elevated, as well as normal intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. The precise mechanism of the ocular hypotensive action of Timolol is not clearly established at this time. Tonography and fluorophotometry studies of the timolol maleate ophthalmic solution in man suggest that its predominant action may be related to the reduced aqueous formation. However, in some studies, a slight increase in outflow facility was also observed. In a study of plasma drug concentration in six subjects, the systemic exposure to timolol was determined following once daily administration of Timolol Maleate Ophthalmic Gel Forming Solution 0.5% in the morning. The mean peak plasma concentration following this morning dose was 0.28 ng/mL. Side effects, when given in the eye, include burning sensation, eye redness, superficial punctate keratopathy, corneal numbness. — NCATS

Clinical trial activity

293 trials · 163 clinical orgs · 54 marketing orgs

Phase 1
25
Phase 2
142
Phase 3
97
Phase 4
98

Earliest trial started Nov 1, 1992 (NCT00751062)

Timeline

1970s

  1. Aug 17, 1978

    Earliest FDA Approval

  2. Aug 17, 1978

    Bausch Health Companies — NDA Secondary Org

  3. Aug 17, 1978

    Bausch & Lomb — Marketing Organization

1980s

  1. Nov 25, 1981

    Merck — First NDA Organization

  2. Nov 25, 1981

    Merck — NDA Organization

  3. Apr 13, 1989

    Fosun — Marketing Organization

  4. Apr 13, 1989

    Chartwell Pharmaceuticals — Marketing Organization

1990s

  1. Jun 8, 1990

    Mylan — Marketing Organization

  2. Jul 31, 1991

    Ani Pharmaceuticals — Marketing Organization

  3. Jul 31, 1991

    Watson Pharmaceuticals — Marketing Organization

  4. Jan 1, 1992

    Earliest Phase 3 Sponsor(trial)

  5. Mar 31, 1995

    Thea Pharma — NDA Secondary Org

  6. Mar 31, 1995

    Akorn, Inc. — NDA Secondary Org

  7. Apr 28, 1995

    Sandoz — NDA Secondary Org

  8. Mar 25, 1997

    Akorn, Inc. — Marketing Organization

  9. Mar 25, 1997

    Fougera — Marketing Organization

  10. Mar 25, 1997

    Pacific Pharmaceuticals — Marketing Organization

  11. Mar 25, 1997

    Bausch & Lomb — NDA Secondary Org

  12. Mar 25, 1997

    Sciegen Pharmaceticals — Marketing Organization

  13. Mar 25, 1997

    Saptalis Pharmaceuticals — Marketing Organization

  14. Jan 1, 1998

    Earliest Phase 2 Sponsor(trial)

  15. Oct 21, 1998

    Novartis — NDA Secondary Org

2000s

  1. Sep 8, 2000

    Apotex — Marketing Organization

  2. Sep 10, 2002

    Hi Tech Pharmaceuticals — Marketing Organization

  3. Sep 10, 2002

    Hikma — Marketing Organization

  4. Oct 30, 2007

    Allergan — Marketing Organization

  5. Oct 30, 2007

    AbbVie — NDA Secondary Org

  6. Jan 1, 2008

    Earliest Phase 1 Sponsor(trial)

  7. Apr 30, 2008

    FDC — Marketing Organization

  8. Oct 28, 2008

    Rubicon Research — Marketing Organization

  9. Nov 6, 2008

    Sandoz — Marketing Organization

  10. Nov 6, 2008

    Novartis — Marketing Organization

  11. Sep 28, 2009

    MannKind Corp — Marketing Organization

  12. Sep 28, 2009

    Wockhardt — Marketing Organization

  13. Sep 28, 2009

    Mankind Pharma — Marketing Organization

2010s

  1. Aug 3, 2010

    Alcon — Marketing Organization

  2. Aug 3, 2010

    Nestle — Marketing Organization

  3. Dec 4, 2013

    Zambon — Marketing Organization

  4. Sep 3, 2014

    Indoco Remedies — Marketing Organization

  5. Sep 22, 2014

    Epic Pharma Llc — Marketing Organization

  6. Dec 17, 2014

    Lannett Company, Inc. — Marketing Organization

  7. Jul 24, 2018

    Aurobindo Pharma — Marketing Organization

  8. Jul 24, 2018

    Eugia Pharma — Marketing Organization

  9. May 2, 2019

    Elysium Health — Marketing Organization

  10. May 2, 2019

    Invatech — Marketing Organization

  11. May 2, 2019

    Rising Pharmaceuticals — Marketing Organization

  12. Jun 25, 2019

    Somerset Pharmaceuticals — Marketing Organization

  13. Jun 25, 2019

    ANDA Repository — Marketing Organization

2020s

  1. May 28, 2020

    Micro Labs Ltd India — Marketing Organization

  2. Oct 22, 2020

    Alembic — Marketing Organization

  3. Dec 13, 2021

    Identirx Pharms — Marketing Organization

  4. Dec 13, 2021

    Amring Pharmaceticals — Marketing Organization

  5. Jun 24, 2022

    Gland Pharma Ltd — Marketing Organization

  6. Sep 13, 2022

    Ingenus Pharmaceuticals — Marketing Organization

  7. Sep 22, 2022

    Dr. Reddy's Laboratories — Marketing Organization

  8. Oct 4, 2022

    Teva — Marketing Organization

  9. Oct 4, 2022

    Lachman Consultants — Marketing Organization

  10. Oct 31, 2022

    SENTISS — Marketing Organization

  11. Dec 12, 2022

    Upsher-Smith Laboratories — Marketing Organization

  12. May 16, 2024

    Glenmark Pharmaceuticals — Marketing Organization

  13. May 23, 2024

    Amneal Pharmaceuticals — Marketing Organization

  14. Aug 7, 2024

    Caplin Point Laboratories — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

Approval history

  • approvedPriority reviewAug 17, 1978

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)(C)NC[C@H](O)COc1nsnc1N1CCOCC1
Mol. weight
316.43 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral, Topical
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

Yes

Sources

Also known as

  • agn-207281
  • arutimol
  • betim
  • betim
  • betimol
  • betimol
  • bimatoprost / timolol
  • bimatoprost / timolol
  • blocadren
  • blocadren
  • blocarden
  • brinzolamide / timolol maleate
  • glaucol
  • glau-opt
  • istalol
  • istalol
  • istalol
  • l-timolol
  • nyogel
  • pro-122
  • (s)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
  • (s)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
  • (s)-timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • timolol
  • (-)-timolol
  • timolol anhydrous
  • timolol anhydrous
  • timolol hemihydrate
  • timolol maleate
  • timolol maleate
  • timolol maleate
  • timolol maleate
  • timolol maleate
  • timolol maleate salt
  • timololo
  • timololo
  • timololum
  • timololum
  • timoptic
  • timoptic
  • timoptic in ocudose
  • timoptic in ocudose
  • timoptic xe
  • timoptic xe
  • timoptic-xe
  • timoptic-xe
  • timoptic-xe
  • tiopex
  • travoprost / timolol

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07218796Phase 3Oct 28, 2025SpyGlass Pharma, Inc.
NCT07168902Phase 2Oct 24, 2025Bausch & Lomb
NCT07218783Phase 3Oct 15, 2025SpyGlass Pharma, Inc.
NCT06833788Phase 4Sep 30, 2025Assistance Publique - Hôpitaux de Paris
NCT07075718Phase 2/Phase 3 (Phase 3)Jun 12, 2025Glaukos Corporation
NCT07036510Phase 1Jun 12, 2025EyeD Pharma
NCT06941467Phase 1Jan 3, 2025Icahn School of Medicine at Mount Sinai
NCT06643416Phase 3Oct 9, 2024The University of Hong Kong
NCT06813807Phase 1Jun 15, 2024Auson Pharmaceuticals Inc.
NCT06369077Phase 4Apr 22, 2024CT Glaucoma Associates
NCT06177678Phase 2Feb 29, 2024Kukje Pharma
NCT06016972Phase 2Jan 29, 2024Qlaris Bio, Inc.
NCT06152861Phase 2Nov 15, 2023Glaukos Corporation
NCT06120842Phase 1/Phase 2 (Phase 2)Oct 13, 2023SpyGlass Pharma, Inc.
NCT05913232Phase 2Aug 28, 2023D. Western Therapeutics Institute, Inc.
NCT06140186Phase 3Apr 1, 2023The University of Hong Kong
NCT05857267Phase 4Mar 7, 2023Laboratorios Poen
NCT06321562Phase 1Mar 1, 2023EyeD Pharma
NCT05479123Phase 4Jun 23, 2022University of Texas at Houston
NCT05165082N/ADec 31, 2021Taipei Medical University
Showing 20 of 293 trials
Page 1 / 15

Organizations

Research & Development (163)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
AlconFor profit555032001
AllerganFor profit353251999
PfizerFor profit151431992
Santen Inc.For profit131242009
Aristotle University of ThessalonikiAcademic/Hospital121222006
MerckFor profit10742005
Aerie PharmaceuticalsFor profit8732011
Glaukos CorporationFor profit6632009
Mati Therapeutics Inc.For profit6612008
PRN Pharmacuetical Research Network, LLCFor profit6512005
Bausch & LombFor profit5432012
Laboratorios Sophia S.A de C.V.For profit5542006
Thomas Jefferson UniversityAcademic/Hospital5452011
Harvard UniversityAcademic/Hospital4422009
Novelion TherapeuticsFor profit4012009
Tel Aviv UniversityAcademic/Hospital4422008
University of ViennaAcademic/Hospital4421999
Auson Pharmaceuticals Inc.For profit3322018
ForSight Vision 5For profit3312013
Laboratoires TheaFor profit3322008
163 organizations
Page 1 / 9

Marketing (70)

OrganizationOrg typeRelationshipDate
ANDA RepositoryFor profitMKTGJun 25, 2019
AbbVieFor profitNDA2Oct 30, 2007
Akorn, Inc.For profitMKTGMar 25, 1997
Akorn, Inc.For profitSYNSep 22, 2014
Akorn, Inc.For profitNDA2Mar 31, 1995
AlconFor profitMKTGAug 3, 2010
AlembicFor profitMKTGOct 22, 2020
AlembicFor profitSYNOct 22, 2020
AllerganFor profitMKTGOct 30, 2007
Amneal PharmaceuticalsFor profitMKTGMay 23, 2024
Amring PharmaceticalsFor profitMKTGDec 13, 2021
Ani PharmaceuticalsFor profitMKTGJul 31, 1991
Ani PharmaceuticalsFor profitSYNJul 31, 1991
ApotexFor profitMKTGSep 8, 2000
ApotexFor profitSYNApr 17, 2015
Aurobindo PharmaFor profitMKTGJul 24, 2018
Bausch & LombFor profitMKTGAug 17, 1978
Bausch & LombFor profitNDA2Mar 25, 1997
Bausch Health CompaniesFor profitNDA2Aug 17, 1978
Bausch Health CompaniesFor profitSYNNov 4, 1993
Caplin Point LaboratoriesFor profitMKTGAug 7, 2024
Chartwell PharmaceuticalsFor profitMKTGApr 13, 1989
Chartwell PharmaceuticalsFor profitMKTGDec 17, 2014
Dr. Reddy's LaboratoriesFor profitMKTGSep 22, 2022
Elysium HealthFor profitMKTGMay 2, 2019
Epic Pharma LlcFor profitMKTGSep 22, 2014
Eugia PharmaFor profitMKTGJul 24, 2018
FDCFor profitMKTGApr 30, 2008
FosunFor profitMKTGApr 13, 1989
FougeraFor profitMKTGMar 25, 1997
Gland Pharma LtdFor profitMKTGJun 24, 2022
Glenmark PharmaceuticalsFor profitMKTGMay 16, 2024
Hi Tech PharmaceuticalsFor profitMKTGSep 10, 2002
Hi Tech PharmaceuticalsFor profitSYNApr 6, 2011
HikmaFor profitMKTGSep 10, 2002
Identirx PharmsFor profitMKTGDec 13, 2021
Indoco RemediesFor profitMKTGSep 3, 2014
Ingenus PharmaceuticalsFor profitMKTGSep 13, 2022
InvatechFor profitMKTGMay 2, 2019
Lachman ConsultantsFor profitMKTGOct 4, 2022
Lannett Company, Inc.For profitMKTGDec 17, 2014
Mankind PharmaFor profitMKTGSep 28, 2009
MannKind CorpFor profitMKTGSep 28, 2009
MerckFor profitNDANov 25, 1981
Micro Labs Ltd IndiaFor profitMKTGMay 28, 2020
MylanFor profitMKTGJun 8, 1990
NestleFor profitMKTGAug 3, 2010
NovartisFor profitNDA2Oct 21, 1998
NovartisFor profitMKTGNov 6, 2008
Pacific PharmaceuticalsFor profitMKTGMar 25, 1997
Quantum PharmaceuticalFor profitMKTG—
Rising PharmaceuticalsFor profitMKTGMay 2, 2019
Rubicon ResearchFor profitMKTGOct 28, 2008
SENTISSFor profitMKTGOct 31, 2022
SENTISSFor profitSYNMay 8, 2023
SandozFor profitNDA2Apr 28, 1995
SandozFor profitMKTGNov 6, 2008
Saptalis PharmaceuticalsFor profitMKTGMar 25, 1997
Sciegen PharmaceticalsFor profitMKTGMar 25, 1997
Somerset PharmaceuticalsFor profitSYNJun 25, 2019
Somerset PharmaceuticalsFor profitMKTGJun 25, 2019
TevaFor profitMKTGOct 4, 2022
TevaFor profitMKTGJun 16, 1993
TevaFor profitSYNSep 28, 2009
Thea PharmaFor profitNDA2Mar 31, 1995
Upsher-Smith LaboratoriesFor profitMKTGDec 12, 2022
Watson PharmaceuticalsFor profitMKTGJul 31, 1991
Watson PharmaceuticalsFor profitSYNSep 3, 2014
WockhardtFor profitMKTGSep 28, 2009
ZambonFor profitMKTGDec 4, 2013