Timolol
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1978
- First approval year
- 1978
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Timolol
- Molecular weight
- 316.43
- Structure (SMILES)
- CC(C)(C)NC[C@H](O)COc1nsnc1N1CCOCC1
- betim
- Betim
- betimol
- Betimol
- blocadren
- Blocadren
- glau opt
- Glau-opt
- glaucol
- Glaucol
- nyogel
- Nyogel
- timolol
- Timolol
- tiopex
- Tiopex
- timolol
- Timolol
- TIMOLOL [HSDB]
- timolol [INN]
- TIMOLOL [MI]
- Timolol [WHO-DD]
- timolol anhydrous
- Timolol anhydrous
- timolol hemihydrate
- Timolol hemihydrate
- timolol hsdb
- timolol inn
- timolol mi
- timolol who dd
- CAS registry numbers
- 26839-75-8
- ChEMBL ID
- CHEMBL499
- InChIKey
- BLJRIMJGRPQVNF-JTQLQIEISA-N
- PubChem compound IDs
- 33624
- FDA ingredient codes (UNII)
- 5JKY92S7BR
- C07AA06
- S01ED01
- S01ED51
Sources for recorded values
- 10600
- 1546004
- Applicant
- BAUSCH AND LOMB INC
- Approval date
- 17 Aug 1978
- Application number
- NDA018086
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- Pharmacology name
- timolol
- Type
- Synthetic organic
- Drug name stem
- -olol
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- topical
- Action
- Antagonist
- Action type
- Antagonist
- Target
- β2-adrenoceptor
- Gene symbol
- ADRB2
- Protein identifier
- P07550
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Antagonist
- Action type
- Antagonist
- Target
- β1-adrenoceptor
- Gene symbol
- ADRB1
- Protein identifier
- P08588
- Affinity units
- pA2
- Action
- Antagonist
- Action type
- Antagonist
- Target
- β1-adrenoceptor
- Gene symbol
- ADRB1
- Protein identifier
- P08588
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- β3-adrenoceptor
- Gene symbol
- ADRB3
- Protein identifier
- P13945
- Affinity units
- pA2
- Action
- Antagonist
- Action type
- Antagonist
- Target
- β3-adrenoceptor
- Gene symbol
- ADRB3
- Protein identifier
- P13945
- Median affinity
- 6.8
- Affinity units
- pKi
- Mechanism
- Beta-1 adrenergic receptor antagonist
- Action type
- Antagonist
- Target
- Beta-1 adrenergic receptor
- Protein identifier
- P08588
- Mechanism
- Beta-2 adrenergic receptor antagonist
- Action type
- Antagonist
- Target
- Beta-2 adrenergic receptor
- Protein identifier
- P07550
- Mechanism
- Beta-1 adrenergic receptor antagonist
- Action type
- Antagonist
- Target
- Beta-1 adrenergic receptor
- Mechanism
- Beta-2 adrenergic receptor antagonist
- Action type
- Antagonist
- Target
- Beta-2 adrenergic receptor
- Action type
- Antagonist
- Gene symbol
- ADRB2
- Protein identifier
- P07550
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- ADRB1
- Protein identifier
- P08588
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Cardiovascular Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000319
- Subject identifier
- D002318
- Condition
- Wounds and Injuries
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000546
- Subject identifier
- D014947
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Macular Degeneration
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001365
- Subject identifier
- D008268
- Condition
- Glaucoma, Open-Angle
- Highest recorded phase
- 4
- Condition identifier
- EFO:0004190
- Subject identifier
- D005902
- Condition
- Exfoliation Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004235
- Subject identifier
- D017889
- Condition
- Wet Macular Degeneration
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004683
- Subject identifier
- D057135
- Condition
- Paronychia
- Highest recorded phase
- 3
- Condition identifier
- EFO:0007421
- Subject identifier
- D010304
- Condition
- Hemangioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000635
- Subject identifier
- D006391
- Condition
- Ocular Hypertension
- Highest recorded phase
- 4
- Condition identifier
- EFO:1001069
- Subject identifier
- D009798
- Condition
- Varicose Ulcer
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001923
- Subject identifier
- D014647
- Condition
- Glaucoma
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005041
- Subject identifier
- D005901
- Condition
- Migraine Disorders
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005277
- Subject identifier
- D008881
- Condition
- Sturge-Weber Syndrome
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008501
- Subject identifier
- D013341
- Condition
- Telangiectasia, Hereditary Hemorrhagic
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0019180
- Subject identifier
- D013683
- Condition identifier
- EFO_0000319
- Condition identifier
- EFO_0000537
- Condition identifier
- EFO_0000546
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003895
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004190
- Condition identifier
- EFO_0004235
- Highest recorded phase
- 3
- Condition identifier
- EFO_0007067
- Condition identifier
- EFO_0007421
- Highest recorded phase
- 3
- Condition identifier
- EFO_1000635
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001069
- Condition identifier
- EFO_1001459
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001923
- Highest recorded phase
- 2
- Condition identifier
- GO_0042060
- Highest recorded phase
- 2
- Condition identifier
- HP_0011499
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001868
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002407
- Condition identifier
- MONDO_0002407
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003005
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004728
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004995
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005041
- Condition identifier
- MONDO_0005041
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005044
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005148
- Highest recorded phase
- 2
And 13 more, listed on the interactive page.
- Event
- arthralgia
- Reports
- 1
- Reporting signal score
- 21.9758
- Event
- asthma
- Reports
- 32
- Reporting signal score
- 27.721
- Event
- atrioventricular block complete
- Reports
- 11
- Reporting signal score
- 17.9934
- Event
- back pain
- Reports
- 1
- Reporting signal score
- 10.9014
- Event
- blood pressure systolic increased
- Reports
- 29
- Reporting signal score
- 59.5141
- Event
- bradycardia
- Reports
- 53
- Reporting signal score
- 60.8841
- Event
- cataract subcapsular
- Reports
- 4
- Reporting signal score
- 12.0977
- Event
- choroidal detachment
- Reports
- 4
- Reporting signal score
- 11.6636
- Event
- chronotropic incompetence
- Reports
- 4
- Reporting signal score
- 19.038
- Event
- conjunctival hyperaemia
- Reports
- 9
- Reporting signal score
- 19.9958
- Event
- corneal deposits
- Reports
- 5
- Reporting signal score
- 15.4035
- Event
- corneal disorder
- Reports
- 5
- Reporting signal score
- 11.3562
- Event
- corneal epithelium defect
- Reports
- 5
- Reporting signal score
- 16.2391
- Event
- corneal oedema
- Reports
- 12
- Reporting signal score
- 33.0845
- Event
- depressed mood
- Reports
- 15
- Reporting signal score
- 12.6926
- Event
- diarrhoea
- Reports
- 2
- Reporting signal score
- 37.8765
- Event
- dry mouth
- Reports
- 19
- Reporting signal score
- 13.5871
- Event
- eye irritation
- Reports
- 39
- Reporting signal score
- 80.5774
- Event
- eye pain
- Reports
- 39
- Reporting signal score
- 73.1774
- Event
- eye pruritus
- Reports
- 26
- Reporting signal score
- 52.149
- Event
- eyelid margin crusting
- Reports
- 6
- Reporting signal score
- 18.6907
- Event
- fatigue
- Reports
- 20
- Reporting signal score
- 11.3987
- Event
- flat anterior chamber of eye
- Reports
- 4
- Reporting signal score
- 15.0955
- Event
- forced expiratory volume decreased
- Reports
- 24
- Reporting signal score
- 82.6272
- Event
- forced vital capacity decreased
- Reports
- 9
- Reporting signal score
- 35.8478
And 39 more, listed on the interactive page.
- NCT00051155
- NCT00061542
- NCT00150267
- NCT00159653
- NCT00219596
- NCT00230763
- NCT00277498
- NCT00293787
- NCT00293800
- NCT00311389
- NCT00314158
- NCT00314171
- NCT00332059
- NCT00332072
- NCT00332345
- NCT00332384
- NCT00332436
- NCT00332540
- NCT00333125
- NCT00751127
- NCT01217606
- NCT01292460
- NCT01652664
- NCT01655758
- NCT01749904
And 57 more, listed on the interactive page.
- Dose
- One drop
- Route
- Topical
- How often
- Twice daily
Conditions of use
- Instilled at least 5 minutes apart when using with other ophthalmic products
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 79.74
- Calculated partition coefficient (ALogP)
- 0.5
- Calculated partition coefficient (XLogP)
- 1.8
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 21
- Molecular formula
- C13H24N4O3S
- Monoisotopic mass
- 316.15691181
- Natural product
- Yes
- 70069-696
- 70069-697
- 70069-698
- Recorded assays
- 3,651
- Active assays
- 83
- Confirmatory
- Other
- Summary
- Adrenergic beta-Antagonists
- Anti-Arrhythmia Agents
- Antihypertensive Agents
These details could not be displayed.
Related records
Trials (182)
- 24-hour Control of Intraocular Pressure (IOP) in Ocular Hypertension
- 24-hour Efficacy and Ocular Surface With Talfuprost and Triple Combined Therapy
- 24-hour Efficacy and Tolerability of the Tafluprost-timolol Fixed Association Without Preservatives in Glaucomatous or Ocular Hypertensive Patients Already Treated With Latanoprost Preserved With BAK. A Prospective, Open Study of 3 Months Duration.
- 24-Hour Intraocular Pressure (IOP) And Blood Pressure Control In Glaucoma And Ocular Hypertension Patients
- 24-Hour Intraocular Pressure (IOP) Control With Travoprost/Timolol Fixed Combination
- 24-Hour Intraocular Pressure Control With Bimatoprost/Timolol Versus Latanoprost as First Choice
- 24-hour Intraocular Pressure Control With Travoprost/Timolol Fixed Combination Versus Travoprost
- 24-hour Study of Dorzolamide/Timolol and Latanoprost/Timolol Fixed Combinations
- A 12 Week Comparison of DuoTrav and Xalacom in Open-Angle Glaucoma
- A 12-Month Study to Evaluate the Efficacy and Safety of Once-Daily Instillation of Combination Glaucoma Therapy in Patients With Open-Angle Glaucoma or Ocular Hypertension
- A 12-week, Randomized, Double-masked, Parallel Group Comparison of Evening Dosing With Xalacom in Subjects With Glaucoma
- A 12-Week, Randomized, Double-Masked, Parallel Group Comparison Of Evening Dosing With Xalacom In Subjects With Glaucoma
- A 6 Month Study Comparing Latanoprost With Timolol in Patients With Open Angle Glaucoma or Ocular Hypertension
- A 6-Week Safety and Efficacy Study of Travatan Compared to Xalcom in Subjects With Open-Angle Glaucoma(OAG) or Ocular Hypertension(OHT)
- A Comparison of the Effect of Dorzolamide and Timolol on Optic Disk Blood Flow in Patients With Open Angle Glaucoma
- A Long Term Study of STN1012600 in Subjects With Open Angle Glaucoma or Ocular Hypertension
- A Long-term Study of DE-117 Ophthalmic Solution Monotherapy and Concomitant Use of DE-117 Ophthalmic Solution With Timolol Ophthalmic Solution in Patients With OAG or OH: RENGE Study
- A Phase 3 Prospective, Randomized, Double-Masked, 12-Week, Parallel Group Study In Pediatric Subjects With Glaucoma.
- A Phase II Study to Evaluate the Additivity of Trabodenoson to Latanoprost in Adults With Ocular Hypertension or Primary Open-Angle Glaucoma
- A Phase III Study of Travoprost/Timolol Combination in Patients With Open-Angle Glaucoma or Ocular Hypertension
Approved for (5)
In development for (19)
- Acne Phase 1
- Age-related macular degeneration Phase 2
- Capillary hemangioma Phase 1
- Diabetic macular edema Phase 2
- Exfoliation syndrome Phase 3
- Familial multiple nevi flammei Phase 3
- Hemangioma Phase 2
- Hereditary hemorrhagic telangiectasia Phase 2
- Injury Phase 2
- Low tension glaucoma Phase 2
- Macular retinal edema Phase 2
- Melanoma Phase 3
- Migraine disorder Phase 2
- Paronychia Phase 3
- Primary angle-closure glaucoma Phase 3
- Rosacea Phase 1
- Sturge-Weber syndrome Phase 1
- Type 2 diabetes mellitus Phase 2
- Wet macular degeneration Phase 2