brimonidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihypertensives, clonidine derivatives 395 59803-98-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • UK 14,304
  • mirvaso
  • brimonidine
  • brimonidine tartrate
  • bromoxidine
A quinoxaline derivative and ADRENERGIC ALHPA-2 RECEPTOR AGONIST that is used to manage INTRAOCULAR PRESSURE associated with OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.
  • Molecular weight: 292.14
  • Formula: C11H10BrN5
  • CLOGP: 1.49
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 62.20
  • ALOGS: -3.28
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1.50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Sept. 6, 1996 FDA
March 25, 2020 PMDA Senju Pharmaceutical Co., Ltd

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 548.73 17.60 330 8947 137307 50458540
Eye irritation 426.42 17.60 148 9129 16992 50578855
Ocular hyperaemia 409.42 17.60 150 9127 20142 50575705
Intraocular pressure increased 370.17 17.60 102 9175 5414 50590433
Eye pain 234.25 17.60 111 9166 28338 50567509
Eye pruritus 122.10 17.60 55 9222 12479 50583368
Vision blurred 108.49 17.60 100 9177 78547 50517300
Iridocyclitis 106.23 17.60 31 9246 2018 50593829
Inappropriate schedule of product administration 102.31 17.60 93 9184 71738 50524109
Visual acuity reduced 94.70 17.60 54 9223 20085 50575762
Corneal opacity 92.81 17.60 22 9255 632 50595215
Dry eye 87.71 17.60 61 9216 32034 50563813
Foreign body sensation in eyes 83.40 17.60 25 9252 1786 50594061
Erythema of eyelid 83.11 17.60 25 9252 1808 50594039
Rebound effect 77.10 17.60 27 9250 3162 50592685
Erythema 76.68 17.60 113 9164 146301 50449546
Glaucoma 70.90 17.60 41 9236 15645 50580202
Scleral hyperaemia 70.88 17.60 15 9262 253 50595594
Ocular surface disease 70.02 17.60 11 9266 27 50595820
Corneal oedema 67.58 17.60 20 9257 1367 50594480
Uveitis 63.55 17.60 32 9245 9278 50586569
Eye swelling 61.46 17.60 41 9236 20103 50575744
Conjunctival hyperaemia 59.58 17.60 20 9257 2062 50593785
Choroidal effusion 52.76 17.60 13 9264 441 50595406
Hypotonia 52.73 17.60 27 9250 8107 50587740
Hypersensitivity 51.08 17.60 118 9159 215043 50380804
Dry mouth 49.24 17.60 56 9221 56122 50539725
Vitreous haemorrhage 46.90 17.60 16 9261 1732 50594115
Lacrimation increased 45.70 17.60 32 9245 16960 50578887
Eye discharge 45.21 17.60 21 9256 5102 50590745
Skin burning sensation 44.38 17.60 26 9251 10159 50585688
Intraocular pressure test abnormal 43.71 17.60 9 9268 132 50595715
Visual impairment 43.57 17.60 58 9219 68217 50527630
Eye inflammation 42.67 17.60 19 9258 4189 50591658
Iris adhesions 41.39 17.60 10 9267 312 50595535
Meniscus injury 41.08 17.60 21 9256 6281 50589566
Conjunctivitis 40.18 17.60 29 9248 16116 50579731
Corneal neovascularisation 39.60 17.60 8 9269 106 50595741
Conjunctival follicles 39.38 17.60 6 9271 11 50595836
Corneal disorder 36.39 17.60 13 9264 1613 50594234
Product quality issue 36.33 17.60 36 9241 30822 50565025
Hypothermia 35.55 17.60 24 9253 11992 50583855
Cataract 34.59 17.60 43 9234 47257 50548590
Cystoid macular oedema 34.41 17.60 12 9265 1387 50594460
Eye disorder 34.22 17.60 28 9249 18711 50577136
Product container issue 34.14 17.60 12 9265 1420 50594427
Blepharitis 32.59 17.60 13 9264 2182 50593665
Eyelids pruritus 32.47 17.60 10 9267 782 50595065
Visual field defect 31.26 17.60 17 9260 5762 50590085
Product packaging quantity issue 29.43 17.60 10 9267 1070 50594777
Conjunctivitis allergic 29.16 17.60 9 9268 709 50595138
Product delivery mechanism issue 26.58 17.60 7 9270 311 50595536
Pain of skin 26.24 17.60 17 9260 7930 50587917
Abnormal sensation in eye 25.39 17.60 10 9267 1623 50594224
Eyelid irritation 25.32 17.60 7 9270 374 50595473
Photophobia 24.60 17.60 21 9256 14866 50580981
Eyelid oedema 23.54 17.60 17 9260 9449 50586398
Angle closure glaucoma 23.27 17.60 10 9267 2024 50593823
Eye colour change 23.11 17.60 6 9271 252 50595595
Intraocular pressure fluctuation 22.64 17.60 4 9273 24 50595823
Corneal infiltrates 21.99 17.60 5 9272 119 50595728
Bradycardia 21.88 17.60 41 9236 64385 50531462
Blindness unilateral 21.85 17.60 13 9264 5222 50590625
Endocrine ophthalmopathy 20.92 17.60 6 9271 367 50595480
Retinal vascular occlusion 20.84 17.60 6 9271 372 50595475
Deep anterior chamber of the eye 20.74 17.60 3 9274 3 50595844
Flat anterior chamber of eye 19.60 17.60 4 9273 56 50595791
Maternal exposure during pregnancy 19.49 17.60 3 9274 159775 50436072
Arthropathy 19.18 17.60 3 9274 157903 50437944
Open angle glaucoma 18.53 17.60 5 9272 244 50595603
Ocular discomfort 18.46 17.60 10 9267 3363 50592484
Retinopathy haemorrhagic 18.20 17.60 3 9274 11 50595836
Dizziness 18.16 17.60 117 9160 346252 50249595
Dermatitis contact 18.09 17.60 14 9263 8632 50587215
Vitreous detachment 17.86 17.60 8 9269 1786 50594061
Macular oedema 17.71 17.60 10 9267 3644 50592203

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 574.97 19.36 233 5889 36706 29531699
Intraocular pressure increased 377.12 19.36 103 6019 4686 29563719
Ocular hyperaemia 237.19 19.36 84 6038 9043 29559362
Eye irritation 231.39 19.36 74 6048 5824 29562581
Corneal oedema 130.30 19.36 33 6089 1109 29567296
Ocular surface disease 123.08 19.36 19 6103 33 29568372
Visual acuity reduced 121.52 19.36 60 6062 14816 29553589
Eye pain 116.74 19.36 54 6068 11541 29556864
Choroidal detachment 102.82 19.36 22 6100 345 29568060
Eye pruritus 90.59 19.36 34 6088 4298 29564107
Hypotony of eye 83.38 19.36 15 6107 88 29568317
Corneal opacity 79.69 19.36 19 6103 494 29567911
Vision blurred 79.30 19.36 66 6056 40110 29528295
Foreign body sensation in eyes 78.27 19.36 19 6103 534 29567871
Blepharitis 70.88 19.36 20 6102 1020 29567385
Corneal neovascularisation 60.26 19.36 10 6112 33 29568372
Conjunctivitis 58.63 19.36 30 6092 7968 29560437
Iridocyclitis 56.14 19.36 18 6104 1422 29566983
Glaucoma 51.92 19.36 25 6097 5832 29562573
Choroidal effusion 47.59 19.36 10 6112 143 29568262
Scleral hyperaemia 42.42 19.36 8 6114 63 29568342
Punctate keratitis 39.64 19.36 10 6112 330 29568075
Lacrimation increased 39.39 19.36 22 6100 6958 29561447
Conjunctival hyperaemia 38.26 19.36 15 6107 2130 29566275
Product delivery mechanism issue 36.94 19.36 8 6114 133 29568272
Cataract 34.54 19.36 32 6090 22346 29546059
Eye discharge 34.47 19.36 13 6109 1663 29566742
Visual impairment 33.84 19.36 36 6086 29672 29538733
Pyelitis 33.52 19.36 7 6115 97 29568308
Conjunctivitis allergic 33.23 19.36 10 6112 640 29567765
Hyperaemia 33.09 19.36 11 6111 973 29567432
Erythema of eyelid 32.81 19.36 10 6112 668 29567737
Retinal detachment 32.67 19.36 17 6105 4669 29563736
Thunderclap headache 32.31 19.36 6 6116 43 29568362
Hypersensitivity 31.07 19.36 46 6076 52857 29515548
Corneal disorder 30.97 19.36 10 6112 807 29567598
Blindness 30.67 19.36 23 6099 12000 29556405
Conjunctival follicles 29.93 19.36 4 6118 0 29568405
Product container issue 29.72 19.36 9 6113 588 29567817
Eyelids pruritus 27.58 19.36 6 6116 102 29568303
Anterior chamber inflammation 27.46 19.36 7 6115 241 29568164
Inappropriate schedule of product administration 26.58 19.36 39 6083 44433 29523972
Keratic precipitates 26.12 19.36 6 6116 132 29568273
Corneal infiltrates 25.74 19.36 6 6116 141 29568264
Ulcerative keratitis 25.55 19.36 10 6112 1413 29566992
Visual acuity tests abnormal 25.53 19.36 5 6117 49 29568356
Cystoid macular oedema 24.99 19.36 8 6114 628 29567777
Keratitis interstitial 24.92 19.36 4 6118 10 29568395
Intraocular pressure decreased 24.45 19.36 5 6117 62 29568343
Angle closure glaucoma 22.95 19.36 8 6114 817 29567588
Hyphaema 22.77 19.36 7 6115 481 29567924
Reversible cerebral vasoconstriction syndrome 22.14 19.36 6 6116 263 29568142
Dry eye 20.96 19.36 15 6107 7281 29561124
Eye swelling 20.84 19.36 16 6106 8641 29559764
Open angle glaucoma 20.68 19.36 5 6117 138 29568267
Ocular discomfort 20.59 19.36 9 6113 1680 29566725

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Intraocular pressure increased 557.24 16.24 151 10798 8151 64479632
Ocular hyperaemia 346.96 16.24 134 10815 22430 64465353
Eye irritation 320.07 16.24 115 10834 15741 64472042
Eye pain 198.24 16.24 100 10849 31525 64456258
Ocular surface disease 180.92 16.24 28 10921 67 64487716
Corneal oedema 177.79 16.24 47 10902 2296 64485487
Visual acuity reduced 164.76 16.24 84 10865 27057 64460726
Vision blurred 144.82 16.24 121 10828 90195 64397588
Foreign body sensation in eyes 104.20 16.24 29 10920 1720 64486063
Blepharitis 101.83 16.24 31 10918 2524 64485259
Eye pruritus 97.17 16.24 46 10903 12613 64475170
Inappropriate schedule of product administration 88.58 16.24 93 10856 92193 64395590
Choroidal detachment 87.74 16.24 20 10929 522 64487261
Erythema of eyelid 83.24 16.24 25 10924 1943 64485840
Corneal neovascularisation 80.62 16.24 15 10934 136 64487647
Choroidal effusion 80.09 16.24 19 10930 593 64487190
Erythema 78.43 16.24 125 10824 186945 64300838
Conjunctival hyperaemia 77.55 16.24 28 10921 3871 64483912
Corneal opacity 77.55 16.24 20 10929 885 64486898
Hypotony of eye 74.06 16.24 15 10934 219 64487564
Scleral hyperaemia 65.55 16.24 14 10935 268 64487515
Dry eye 61.77 16.24 46 10903 28973 64458810
Corneal disorder 61.61 16.24 20 10929 2007 64485776
Conjunctival follicles 61.51 16.24 9 10940 12 64487771
Conjunctivitis 61.48 16.24 40 10909 20314 64467469
Conjunctivitis allergic 61.00 16.24 17 10932 1013 64486770
Uveitis 59.21 16.24 33 10916 12675 64475108
Rebound effect 57.47 16.24 24 10925 4893 64482890
Iris adhesions 56.63 16.24 14 10935 521 64487262
Glaucoma 54.01 16.24 34 10915 16314 64471469
Eye discharge 53.39 16.24 23 10926 5061 64482722
Cystoid macular oedema 47.88 16.24 16 10933 1758 64486025
Iridocyclitis 46.44 16.24 18 10931 3027 64484756
Punctate keratitis 45.44 16.24 13 10936 852 64486931
Cataract 44.46 16.24 49 10900 51213 64436570
Vitreous haemorrhage 42.70 16.24 17 10932 3068 64484715
Skin burning sensation 42.65 16.24 25 10924 10558 64477225
Anterior chamber inflammation 42.58 16.24 11 10938 490 64487293
Angle closure glaucoma 41.56 16.24 16 10933 2641 64485142
Eye inflammation 41.45 16.24 19 10930 4838 64482945
Eyelids pruritus 40.04 16.24 11 10938 621 64487162
Dry mouth 39.54 16.24 50 10899 60368 64427415
Lacrimation increased 38.85 16.24 29 10920 18317 64469466
Visual impairment 38.82 16.24 55 10894 74022 64413761
Corneal infiltrates 38.09 16.24 9 10940 276 64487507
Retinal detachment 37.94 16.24 21 10928 7955 64479828
Visual field defect 37.53 16.24 21 10928 8125 64479658
Hypotonia 36.24 16.24 23 10926 11189 64476594
Ulcerative keratitis 35.80 16.24 15 10934 3082 64484701
Corneal deposits 35.58 16.24 9 10940 368 64487415
Hyperaemia 34.29 16.24 14 10935 2695 64485088
Corneal scar 33.26 16.24 8 10941 265 64487518
Keratic precipitates 32.40 16.24 8 10941 296 64487487
Blindness 32.15 16.24 28 10921 21991 64465792
Meniscus injury 32.13 16.24 17 10932 5890 64481893
Flat anterior chamber of eye 31.94 16.24 7 10942 152 64487631
Keratitis interstitial 31.74 16.24 5 10944 14 64487769
Photophobia 29.38 16.24 24 10925 17269 64470514
Abnormal sensation in eye 29.17 16.24 11 10938 1716 64486067
Retinal vascular occlusion 28.09 16.24 8 10941 516 64487267
Eye swelling 27.93 16.24 26 10923 22255 64465528
Pyelitis 27.78 16.24 7 10942 282 64487501
Eye disorder 27.56 16.24 24 10925 18845 64468938
Intraocular pressure test abnormal 27.48 16.24 6 10943 128 64487655
Meibomian gland dysfunction 27.30 16.24 6 10943 132 64487651
Intraocular pressure fluctuation 27.21 16.24 5 10944 42 64487741
Anterior chamber disorder 27.00 16.24 6 10943 139 64487644
Reaction to preservatives 26.88 16.24 6 10943 142 64487641
Trabeculectomy 26.52 16.24 5 10944 49 64487734
Hyphaema 26.32 16.24 8 10941 647 64487136
Open angle glaucoma 25.89 16.24 7 10942 372 64487411
Dermatitis contact 25.50 16.24 17 10932 8983 64478800
Eyelid oedema 25.09 16.24 19 10930 12260 64475523
Eyelid ptosis 24.62 16.24 17 10932 9508 64478275
Thunderclap headache 24.35 16.24 6 10943 220 64487563
Optic nerve cup/disc ratio increased 23.04 16.24 3 10946 0 64487783
Eyelid irritation 22.55 16.24 6 10943 300 64487483
Visual acuity tests abnormal 22.46 16.24 5 10944 117 64487666
Dizziness 22.41 16.24 137 10812 430026 64057757
Pain of skin 22.27 16.24 16 10933 9531 64478252
Corneal epithelium defect 21.80 16.24 7 10942 678 64487105
Bradycardia 21.60 16.24 56 10893 118163 64369620
Photopsia 21.30 16.24 12 10937 4702 64483081
Macular oedema 20.94 16.24 12 10937 4855 64482928
Intraocular pressure decreased 20.86 16.24 5 10944 163 64487620
Hypothermia 20.80 16.24 21 10928 19835 64467948
Endocrine ophthalmopathy 20.68 16.24 6 10943 413 64487370
Skin irritation 20.51 16.24 15 10934 9179 64478604
Giant papillary conjunctivitis 20.50 16.24 3 10946 4 64487779
Vitreous floaters 20.41 16.24 13 10936 6360 64481423
Eyelid disorder 20.20 16.24 8 10941 1423 64486360
Product quality issue 20.02 16.24 25 10924 29774 64458009
Deep anterior chamber of the eye 19.75 16.24 3 10946 6 64487777
Corneal infection 19.35 16.24 4 10945 65 64487718
Conjunctival oedema 18.78 16.24 7 10942 1057 64486726
Prostaglandin analogue periorbitopathy 18.22 16.24 3 10946 12 64487771
Panophthalmitis 17.52 16.24 4 10945 105 64487678
Eyelid margin crusting 17.50 16.24 6 10943 712 64487071
Blindness unilateral 17.32 16.24 12 10937 6749 64481034
Floppy iris syndrome 17.30 16.24 5 10944 340 64487443
Eye complication associated with device 17.21 16.24 3 10946 18 64487765
Brain stem haematoma 17.04 16.24 4 10945 119 64487664
Corneal epithelial microcysts 16.24 16.24 3 10946 26 64487757

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D11AX21 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC S01EA05 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Sympathomimetics in glaucoma therapy
ATC S01GA07 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
FDA MoA N0000000209 Adrenergic alpha-Agonists
FDA EPC N0000175552 alpha-Adrenergic Agonist
CHEBI has role CHEBI:35569 alpha-adrenergic agonists
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:37886 adrenergic agonists
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Open-angle glaucoma indication 84494001 DOID:1067
Rosacea indication 398909004 DOID:8881
Bronchospasm contraindication 4386001
Complete atrioventricular block contraindication 27885002
Orthostatic hypotension contraindication 28651003
Acute cerebrovascular insufficiency contraindication 29322000
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Anaphylaxis contraindication 39579001
Sinus bradycardia contraindication 49710005
General anesthesia contraindication 50697003
Thromboangiitis obliterans contraindication 52403007 DOID:12918
Cerebrovascular disease contraindication 62914000 DOID:6713
Diabetes mellitus contraindication 73211009 DOID:9351
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Myasthenia gravis contraindication 91637004 DOID:437
Acute disease of cardiovascular system contraindication 128487001
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Hypoglycemic disorder contraindication 237630007
Raynaud's phenomenon contraindication 266261006
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.64 Basic
pKa2 1.82 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7030149 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP. DOSE IS ONE DROP OF COMBIGAN IN THE AFFECTED EYE TWICE DAILY
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7320976 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP. DOSE IS ONE DROP OF COMBIGAN IN THE AFFECTED EYE TWICE DAILY
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7642258 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8133890 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8354409 April 19, 2022 REDUCTION OF INTRAOCULAR PRESSURE IN PATIENTS WITH ELEVATED INTRAOCULAR PRESSURE OR GLAUCOMA
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8748425 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9474751 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9770453 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH COMPARABLE EFFICACY, AND A REDUCTION IN SPECIFIED ADVERSE EVENTS, COMPARED TO BRIMONIDINE 0.2% TID
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9907801 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH A REDUCTION IN SPECIFIED ADVERSE EVENTS, COMPARED TO BRIMONIDINE 0.2% TID
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9907802 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH COMPARABLE EFFICACY TO BRIMONIDINE 0.2% TID
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8859551 May 25, 2024 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8410102 May 24, 2025 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8426410 May 24, 2025 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 7439241 Aug. 25, 2025 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 8293742 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 9259425 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8513247 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8513249 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 9861631 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 9861632 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8053427 June 13, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2C adrenergic receptor GPCR AGONIST EC50 8.47 WOMBAT-PK CHEMBL
Alpha-2B adrenergic receptor GPCR AGONIST EC50 7.26 WOMBAT-PK CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST EC50 8.39 WOMBAT-PK CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 6.07 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 5.27 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.84 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR Ki 5.55 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 7.28 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 5.59 CHEMBL
Alpha-1A adrenergic receptor GPCR EC50 5.95 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 7.52 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 6.13 CHEMBL
Alpha-1B adrenergic receptor GPCR EC50 6.03 CHEMBL

External reference:

IDSource
E6GNX3HHTE UNII
D02076 KEGG_DRUG
70359-46-5 SECONDARY_CAS_RN
134615 RXNORM
C0525227 UMLSCUI
CHEBI:3175 CHEBI
J59 PDB_CHEM_ID
CHEMBL844 ChEMBL_ID
2435 PUBCHEM_CID
DB00484 DRUGBANK_ID
CHEMBL2062257 ChEMBL_ID
D000068438 MESH_DESCRIPTOR_UI
6863 INN_ID
520 IUPHAR_LIGAND_ID
14807 MMSL
205316 MMSL
240890 MMSL
31659 MMSL
4297 MMSL
44062 MMSL
46686 MMSL
006196 NDDF
006197 NDDF
108827001 SNOMEDCT_US
372547000 SNOMEDCT_US
386924004 SNOMEDCT_US
4021002 VANDF
4024043 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9177 SOLUTION/ DROPS 1.50 mg OPHTHALMIC NDA 25 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9177 SOLUTION/ DROPS 1.50 mg OPHTHALMIC NDA 25 sections
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 0023-9211 SOLUTION/ DROPS 2 mg OPHTHALMIC NDA 26 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9321 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA 25 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9321 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA 25 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 2 mg OPHTHALMIC NDA 24 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0078-0904 SUSPENSION/ DROPS 2 mg OPHTHALMIC NDA 26 sections
Mirvaso HUMAN PRESCRIPTION DRUG LABEL 1 0299-5980 GEL 5 mg TOPICAL NDA 26 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0781-7186 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 23 sections
Brimonidine Tartrate Human Prescription Drug Label 1 14445-400 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 24 sections
BRIMONIDINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 16590-883 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 12 sections
Brimonidine HUMAN PRESCRIPTION DRUG LABEL 1 17478-715 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 24208-411 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
LUMIFY Redness Reliever Eye Drops HUMAN OTC DRUG LABEL 1 24208-537 SOLUTION/ DROPS 0.25 mg OPHTHALMIC NDA 13 sections
LUMIFY Redness Reliever Eye Drops HUMAN OTC DRUG LABEL 1 24208-537 SOLUTION/ DROPS 0.25 mg OPHTHALMIC NDA 13 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 25685-715 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 12 sections
Brimonidine HUMAN PRESCRIPTION DRUG LABEL 1 50090-1046 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 24 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-1800 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-4224 SOLUTION 2 mg OPHTHALMIC ANDA 24 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 54868-4276 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA 25 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 54868-4690 SOLUTION/ DROPS 1.50 mg OPHTHALMIC NDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 54868-6094 SOLUTION 1.50 mg OPHTHALMIC NDA 10 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 54868-6287 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 54868-6295 SOLUTION/ DROPS 2 mg OPHTHALMIC NDA 23 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 60505-0564 SOLUTION/ DROPS 1.50 mg OPHTHALMIC ANDA 25 sections
Brimonidine Tartrate/Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 60505-6225 SOLUTION/ DROPS 2 mg OPHTHALMIC NDA authorized generic 26 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 61314-143 SOLUTION 2 mg OPHTHALMIC ANDA 23 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 61314-144 SOLUTION 1.50 mg OPHTHALMIC NDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 63629-8792 SOLUTION 1.50 mg OPHTHALMIC NDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 63629-8792 SOLUTION 1.50 mg OPHTHALMIC NDA 25 sections