> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/timolol-2f8e126f-b46e-4e1f-8b8c-f29bd226070c
> Record changed: 2026-11-04

# Timolol

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

First approval year

1978

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

## Development status

**First approval year**

1978

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**Drug name**

Timolol

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**Molecular weight**

316.43

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**Structure (SMILES)**

CC(C)(C)NC\[C@H\](O)COc1nsnc1N1CCOCC1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

### Brand names (16)

- betim
- Betim
- betimol
- Betimol
- blocadren
- Blocadren
- glau opt
- Glau-opt
- glaucol
- Glaucol
- nyogel
- Nyogel
- timolol
- Timolol
- tiopex
- Tiopex

### Other names (14)

- 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

## Identifiers

**CAS registry numbers**

- 26839-75-8

**ChEMBL ID**

CHEMBL499

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**InChIKey**

BLJRIMJGRPQVNF-JTQLQIEISA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

**PubChem compound IDs**

- 33624

**FDA ingredient codes (UNII)**

- 5JKY92S7BR

### ATC classification codes (3)

- C07AA06
- S01ED01
- S01ED51

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL499)

### RxNorm IDs (RxCUI) (2)

- 10600
- 1546004

## Regulatory information

### United States

**Applicant**

BAUSCH AND LOMB INC

**Approval date**

17 Aug 1978

**Application number**

NDA018086

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

## Approval status

**United States (FDA)**

Approved

## Pharmacology

### Drug classification

**Pharmacology name**

timolol

**Type**

Synthetic organic

**Drug name stem**

\-olol

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral
- topical

### Mechanisms of action (7)

- **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

### Open Targets mechanisms (2)

- **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

### DrugCentral mechanisms (2)

- **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

### Investigated indications (15)

- **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

### Open Targets indications (38)

- **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.

### Reported adverse events (64)

- **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.

### Trial references (82)

- NCT00051155  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00051155)
- NCT00061542  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00061542)
- NCT00150267  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00150267)
- NCT00159653  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00159653)
- NCT00219596  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00219596)
- NCT00230763  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00230763)
- NCT00277498  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00277498)
- NCT00293787  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00293787)
- NCT00293800  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00293800)
- NCT00311389  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00311389)
- NCT00314158  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00314158)
- NCT00314171  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00314171)
- NCT00332059  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332059)
- NCT00332072  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332072)
- NCT00332345  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332345)
- NCT00332384  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332384)
- NCT00332436  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332436)
- NCT00332540  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00332540)
- NCT00333125  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00333125)
- NCT00751127  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00751127)
- NCT01217606  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01217606)
- NCT01292460  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01292460)
- NCT01652664  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01652664)
- NCT01655758  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01655758)
- NCT01749904  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01749904)

And 57 more, listed on the interactive page.

## Dosing

**Dose**

One drop

**Route**

Topical

**How often**

Twice daily

### Conditions of use

- Instilled at least 5 minutes apart when using with other ophthalmic products

## Chemical properties

**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

## National Drug Codes

- 70069-696
- 70069-697
- 70069-698

## Evidence counts

**Recorded assays**

3,651

**Active assays**

83

### Active assay types (3)

- Confirmatory
- Other
- Summary

## Pharmacologic actions

- Adrenergic beta-Antagonists  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000319.html)
- Anti-Arrhythmia Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000889.html)
- Antihypertensive Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000959.html)

## Biological measurements

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)

- [Cardiovascular disorder](https://trialight.com/data/condition/cardiovascular-disorder-362e433e-88a4-575f-90af-50fe7239dec0.md)
- [Glaucoma](https://trialight.com/data/condition/glaucoma-7a3c05c0-9871-55db-af74-962761181784.md)
- [Hypertensive disorder](https://trialight.com/data/condition/hypertensive-disorder-6d786557-b9e8-5afc-80f3-89a1995f9da5.md)
- [Ocular hypertension](https://trialight.com/data/condition/ocular-hypertension-754666dc-b494-5a18-a3ee-6a2d941c65dd.md)
- [Open-angle glaucoma](https://trialight.com/data/condition/open-angle-glaucoma-fb887921-4122-599b-b8a0-928b40ddc7a2.md)

### In development for (19)

- [Acne](https://trialight.com/data/condition/acne-02478aa3-966b-5ffb-a257-6dbe85c14e58.md) Phase 1
- [Age-related macular degeneration](https://trialight.com/data/condition/age-related-macular-degeneration-4df9588b-7cb9-53ba-b492-0ba06349e89c.md) 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](https://trialight.com/data/condition/injury-4a894a73-b8a8-55e6-acf3-6e0f96e895c1.md) Phase 2
- Low tension glaucoma Phase 2
- [Macular retinal edema](https://trialight.com/data/condition/macular-retinal-edema-893472dc-a81c-5efb-b457-9a4c0884e5e5.md) Phase 2
- [Melanoma](https://trialight.com/data/condition/melanoma-457e9de6-dcd9-56fb-be48-0290fb4386ef.md) Phase 3
- [Migraine disorder](https://trialight.com/data/condition/migraine-disorder-0a28e77d-6415-5582-980f-2d0721f95f76.md) Phase 2
- Paronychia Phase 3
- Primary angle-closure glaucoma Phase 3
- [Rosacea](https://trialight.com/data/condition/rosacea-1b019103-cfbb-5749-8481-b31c0be0feed.md) Phase 1
- Sturge-Weber syndrome Phase 1
- [Type 2 diabetes mellitus](https://trialight.com/data/condition/type-2-diabetes-mellitus-98e14a90-bb06-5174-90c7-901a0a259fb9.md) Phase 2
- [Wet macular degeneration](https://trialight.com/data/condition/wet-macular-degeneration-fce04054-9f5d-5a0b-8ba9-fb08ba7393ba.md) Phase 2

### Targets (3)

- [ADRB1](https://trialight.com/data/target/adrb1-6e315eb7-4a1a-5347-bacb-acfe97cbc2b5.md) Beta-1 adrenergic receptor antagonist
- [ADRB2](https://trialight.com/data/target/adrb2-dd50b672-19f0-5015-be62-c6f5861dc510.md) Beta-2 adrenergic receptor antagonist
- [ADRB3](https://trialight.com/data/target/adrb3-61a0c2dc-6d50-5bea-b1a9-be13f4623617.md)

---

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