brimonidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihypertensives, clonidine derivatives	395	59803-98-4

Description:

Molecule	Description
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

Molecule

Description

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:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Sept. 6, 1996	FDA
March 25, 2020	PMDA	Senju Pharmaceutical Co., Ltd

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Treatment failure	501.11	18.84	330	9414	170062	56112261
Intraocular pressure increased	450.14	18.84	119	9625	5722	56276601
Eye irritation	431.04	18.84	151	9593	18877	56263446
Ocular hyperaemia	409.77	18.84	151	9593	21828	56260495
Eye pain	237.84	18.84	113	9631	30734	56251589
Glaucoma	135.06	18.84	64	9680	17265	56265058
Eye pruritus	118.52	18.84	55	9689	14151	56268172
Vision blurred	112.75	18.84	102	9642	82841	56199482
Corneal opacity	108.53	18.84	25	9719	671	56281652
Iridocyclitis	104.87	18.84	31	9713	2238	56280085
Inappropriate schedule of product administration	96.89	18.84	94	9650	83293	56199030
Visual acuity reduced	96.14	18.84	54	9690	20672	56261651
Dry eye	91.93	18.84	64	9680	35652	56246671
Erythema	86.47	18.84	120	9624	155819	56126504
Foreign body sensation in eyes	83.29	18.84	25	9719	1902	56280421
Erythema of eyelid	82.32	18.84	25	9719	1979	56280344
Rebound effect	77.23	18.84	28	9716	3842	56278481
Scleral hyperaemia	71.68	18.84	15	9729	254	56282069
Ocular surface disease	69.82	18.84	11	9733	30	56282293
Corneal oedema	68.22	18.84	20	9724	1402	56280921
Uveitis	65.68	18.84	34	9710	11061	56271262
Eye swelling	61.39	18.84	41	9703	21335	56260988
Conjunctival hyperaemia	59.48	18.84	20	9724	2196	56280127
Open angle glaucoma	59.48	18.84	13	9731	273	56282050
Choroidal effusion	53.11	18.84	13	9731	455	56281868
Hypotonia	52.54	18.84	27	9717	8650	56273673
Dry mouth	49.06	18.84	58	9686	64147	56218176
Eye discharge	48.24	18.84	22	9722	5431	56276892
Vitreous haemorrhage	46.45	18.84	16	9728	1890	56280433
Lacrimation increased	45.14	18.84	32	9712	18316	56264007
Intraocular pressure test abnormal	44.22	18.84	9	9735	132	56282191
Skin burning sensation	43.83	18.84	26	9718	11005	56271318
Hypersensitivity	43.04	18.84	119	9625	256289	56026034
Visual impairment	42.39	18.84	58	9686	74144	56208179
Iris adhesions	41.90	18.84	10	9734	314	56282009
Eye inflammation	41.50	18.84	19	9725	4732	56277591
Meniscus injury	41.43	18.84	21	9723	6537	56275786
Corneal neovascularisation	40.06	18.84	8	9736	106	56282217
Corneal disorder	39.89	18.84	14	9730	1748	56280575
Eye disorder	39.84	18.84	31	9713	20421	56261902
Conjunctival follicles	39.73	18.84	6	9738	11	56282312
Blepharitis	39.35	18.84	15	9729	2365	56279958
Conjunctivitis	38.76	18.84	29	9715	18031	56264292
Product quality issue	37.22	18.84	36	9708	31700	56250623
Hypothermia	35.99	18.84	24	9720	12446	56269877
Product container issue	34.00	18.84	12	9732	1522	56280801
Cystoid macular oedema	33.95	18.84	12	9732	1529	56280794
Cataract	33.80	18.84	43	9701	51204	56231119
Rosacea	31.44	18.84	15	9729	4098	56278225
Visual field defect	31.34	18.84	17	9727	6072	56276251
Eyelids pruritus	31.30	18.84	10	9734	935	56281388
Conjunctivitis allergic	28.85	18.84	9	9735	779	56281544
Product packaging quantity issue	28.84	18.84	10	9734	1204	56281119
Conjunctival scar	27.11	18.84	5	9739	42	56282281
Product delivery mechanism issue	26.55	18.84	7	9737	331	56281992
Eyelid oedema	26.28	18.84	18	9726	9750	56272573
Pain of skin	25.82	18.84	17	9727	8629	56273694
Abnormal sensation in eye	25.67	18.84	10	9734	1671	56280652
Eyelid irritation	25.11	18.84	7	9737	409	56281914
Arthropathy	24.38	18.84	3	9741	200272	56082051
Photophobia	24.27	18.84	21	9723	16029	56266294
Angle closure glaucoma	23.65	18.84	10	9734	2061	56280262
Bradycardia	23.47	18.84	42	9702	67462	56214861
Eye colour change	23.18	18.84	6	9738	264	56282059
Intraocular pressure fluctuation	22.87	18.84	4	9740	24	56282299
Maternal exposure during pregnancy	22.68	18.84	3	9741	189550	56092773
Blindness unilateral	21.81	18.84	13	9731	5547	56276776
Corneal infiltrates	21.36	18.84	5	9739	144	56282179
Deep anterior chamber of the eye	20.91	18.84	3	9741	3	56282320
Retinal vascular occlusion	20.86	18.84	6	9738	393	56281930
Macular oedema	20.66	18.84	11	9733	3783	56278540
Flat anterior chamber of eye	19.83	18.84	4	9740	56	56282267
Retinal detachment	19.49	18.84	12	9732	5429	56276894
Endocrine ophthalmopathy	19.43	18.84	6	9738	502	56281821

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Treatment failure	557.68	18.89	233	6177	40559	31650375
Intraocular pressure increased	441.43	18.89	118	6292	5069	31685865
Ocular hyperaemia	239.01	18.89	86	6324	9923	31681011
Eye irritation	229.84	18.89	75	6335	6443	31684491
Corneal oedema	148.11	18.89	37	6373	1204	31689730
Eye pain	124.22	18.89	57	6353	12247	31678687
Visual acuity reduced	121.08	18.89	60	6350	15283	31675651
Ocular surface disease	120.19	18.89	19	6391	43	31690891
Choroidal detachment	106.96	18.89	23	6387	379	31690555
Eye pruritus	89.85	18.89	35	6375	5010	31685924
Open angle glaucoma	87.83	18.89	17	6393	160	31690774
Hypotony of eye	82.88	18.89	15	6395	94	31690840
Glaucoma	81.90	18.89	35	6375	6345	31684589
Vision blurred	80.26	18.89	67	6343	41848	31649086
Corneal opacity	78.78	18.89	19	6391	532	31690402
Foreign body sensation in eyes	77.97	18.89	19	6391	556	31690378
Blepharitis	69.40	18.89	20	6390	1127	31689807
Conjunctivitis	65.86	18.89	33	6377	8590	31682344
Corneal neovascularisation	59.19	18.89	10	6400	39	31690895
Iridocyclitis	55.36	18.89	18	6392	1522	31689412
Choroidal effusion	46.31	18.89	10	6400	168	31690766
Scleral hyperaemia	42.60	18.89	8	6402	63	31690871
Rosacea	40.51	18.89	13	6397	1054	31689880
Blindness	39.42	18.89	27	6383	12524	31678410
Punctate keratitis	39.01	18.89	10	6400	361	31690573
Lacrimation increased	38.44	18.89	22	6388	7460	31683474
Conjunctival hyperaemia	38.13	18.89	15	6395	2201	31688733
Product delivery mechanism issue	36.48	18.89	8	6402	145	31690789
Erythema of eyelid	35.65	18.89	11	6399	784	31690150
Cataract	35.40	18.89	33	6377	23774	31667160
Visual impairment	34.75	18.89	37	6373	31242	31659692
Eye discharge	33.92	18.89	13	6397	1778	31689156
Product container issue	33.83	18.89	10	6400	616	31690318
Pyelitis	33.48	18.89	7	6403	100	31690834
Thunderclap headache	32.45	18.89	6	6404	43	31690891
Hyperaemia	32.29	18.89	11	6399	1074	31689860
Retinal detachment	32.05	18.89	17	6393	4969	31685965
Conjunctivitis allergic	31.81	18.89	10	6400	758	31690176
Corneal disorder	30.87	18.89	10	6400	835	31690099
Corneal infiltrates	30.81	18.89	7	6403	150	31690784
Intraocular pressure decreased	30.49	18.89	6	6404	62	31690872
Hypersensitivity	30.06	18.89	46	6364	55697	31635237
Conjunctival follicles	30.03	18.89	4	6406	0	31690934
Cystoid macular oedema	28.46	18.89	9	6401	696	31690238
Anterior chamber inflammation	26.66	18.89	7	6403	278	31690656
Eyelids pruritus	26.39	18.89	6	6404	129	31690805
Keratic precipitates	25.84	18.89	6	6404	142	31690792
Visual acuity tests abnormal	25.65	18.89	5	6405	49	31690885
Inappropriate schedule of product administration	24.70	18.89	40	6370	50783	31640151
Ulcerative keratitis	24.67	18.89	10	6400	1586	31689348
Dry eye	24.49	18.89	17	6393	8055	31682879
Visual field defect	23.25	18.89	13	6397	4215	31686719
Ocular discomfort	23.07	18.89	10	6400	1873	31689061
Keratitis interstitial	23.03	18.89	4	6406	19	31690915
Erythema	22.52	18.89	50	6360	80355	31610579
Angle closure glaucoma	22.44	18.89	8	6402	893	31690041
Hyphaema	22.24	18.89	7	6403	533	31690401
Reversible cerebral vasoconstriction syndrome	20.51	18.89	6	6404	356	31690578
Eye swelling	20.34	18.89	16	6394	9160	31681774
Corneal deposits	19.08	18.89	5	6405	197	31690737

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intraocular pressure increased	676.41	16.27	177	11364	8724	70908179
Ocular hyperaemia	348.04	16.27	136	11405	24503	70892400
Eye irritation	319.29	16.27	117	11424	17671	70899232
Eye pain	203.84	16.27	103	11438	33999	70882904
Corneal oedema	196.73	16.27	51	11490	2409	70914494
Ocular surface disease	180.67	16.27	28	11513	72	70916831
Visual acuity reduced	165.84	16.27	84	11457	27846	70889057
Vision blurred	148.09	16.27	123	11418	94861	70822042
Open angle glaucoma	132.92	16.27	27	11514	419	70916484
Glaucoma	130.04	16.27	62	11479	18030	70898873
Blepharitis	108.91	16.27	33	11508	2760	70914143
Foreign body sensation in eyes	103.93	16.27	29	11512	1813	70915090
Eye pruritus	95.61	16.27	47	11494	14600	70902303
Choroidal detachment	92.05	16.27	21	11520	575	70916328
Erythema	88.86	16.27	134	11407	199429	70717474
Corneal opacity	81.54	16.27	21	11520	965	70915938
Erythema of eyelid	81.26	16.27	25	11516	2200	70914703
Corneal neovascularisation	80.57	16.27	15	11526	143	70916760
Inappropriate schedule of product administration	80.09	16.27	93	11448	107462	70809441
Choroidal effusion	79.61	16.27	19	11522	636	70916267
Conjunctival hyperaemia	77.38	16.27	28	11513	4065	70912838
Hypotony of eye	73.64	16.27	15	11526	236	70916667
Rosacea	68.78	16.27	25	11516	3676	70913227
Conjunctivitis	66.42	16.27	43	11498	22593	70894310
Scleral hyperaemia	65.95	16.27	14	11527	272	70916631
Dry eye	65.76	16.27	49	11492	32233	70884670
Corneal disorder	65.08	16.27	21	11520	2158	70914745
Conjunctival follicles	61.89	16.27	9	11532	12	70916891
Conjunctivitis allergic	59.60	16.27	17	11524	1151	70915752
Iris adhesions	57.14	16.27	14	11527	524	70916379
Eye discharge	56.08	16.27	24	11517	5423	70911480
Uveitis	55.74	16.27	33	11508	14812	70902091
Rebound effect	53.96	16.27	24	11517	5947	70910956
Cystoid macular oedema	47.04	16.27	16	11525	1936	70914967
Iridocyclitis	45.59	16.27	18	11523	3317	70913586
Punctate keratitis	45.19	16.27	13	11528	907	70915996
Cataract	44.57	16.27	50	11491	55595	70861308
Retinal detachment	43.15	16.27	23	11518	8444	70908459
Corneal infiltrates	42.79	16.27	10	11531	305	70916598
Anterior chamber inflammation	41.94	16.27	11	11530	543	70916360
Skin burning sensation	41.85	16.27	25	11516	11401	70905502
Vitreous haemorrhage	41.74	16.27	17	11524	3395	70913508
Angle closure glaucoma	41.52	16.27	16	11525	2763	70914140
Visual field defect	40.42	16.27	22	11519	8416	70908487
Eye inflammation	40.01	16.27	19	11522	5468	70911435
Visual impairment	38.67	16.27	56	11485	80194	70836709
Eyelids pruritus	38.47	16.27	11	11530	751	70916152
Hypotonia	38.44	16.27	24	11517	11841	70905062
Blindness	38.05	16.27	31	11510	23196	70893707
Lacrimation increased	37.85	16.27	29	11512	19870	70897033
Dry mouth	36.65	16.27	51	11490	70406	70846497
Ulcerative keratitis	35.38	16.27	15	11526	3312	70913591
Hyperaemia	34.17	16.27	14	11527	2837	70914066
Corneal deposits	33.99	16.27	9	11532	461	70916442
Corneal scar	33.14	16.27	8	11533	281	70916622
Keratic precipitates	32.41	16.27	8	11533	309	70916594
Flat anterior chamber of eye	32.14	16.27	7	11534	154	70916749
Meniscus injury	32.12	16.27	17	11524	6150	70910753
Keratitis interstitial	29.83	16.27	5	11536	24	70916879
Abnormal sensation in eye	28.94	16.27	11	11530	1831	70915072
Photophobia	28.69	16.27	24	11517	18626	70898277
Eye disorder	28.41	16.27	25	11516	20760	70896143
Pyelitis	27.98	16.27	7	11534	286	70916617
Retinal vascular occlusion	27.74	16.27	8	11533	563	70916340
Intraocular pressure test abnormal	27.60	16.27	6	11535	131	70916772
Eye swelling	27.58	16.27	26	11515	23588	70893315
Eyelid oedema	27.44	16.27	20	11521	12707	70904196
Intraocular pressure fluctuation	27.42	16.27	5	11536	42	70916861
Meibomian gland dysfunction	26.71	16.27	6	11535	153	70916750
Trabeculectomy	26.64	16.27	5	11536	50	70916853
Anterior chamber disorder	26.41	16.27	6	11535	161	70916742
Intraocular pressure decreased	26.17	16.27	6	11535	168	70916735
Reaction to preservatives	25.64	16.27	6	11535	184	70916719
Dermatitis contact	24.92	16.27	17	11524	9732	70907171
Hyphaema	24.86	16.27	8	11533	815	70916088
Eyelid ptosis	24.37	16.27	17	11524	10085	70906818
Thunderclap headache	23.96	16.27	6	11535	246	70916657
Macular oedema	23.46	16.27	13	11528	5149	70911754
Optic nerve cup/disc ratio increased	23.17	16.27	3	11538	0	70916903
Visual acuity tests abnormal	22.67	16.27	5	11536	117	70916786
Bradycardia	22.25	16.27	57	11484	124558	70792345
Dizziness	22.11	16.27	140	11401	464001	70452902
Corneal epithelium defect	21.98	16.27	7	11534	689	70916214
Pain of skin	21.83	16.27	16	11525	10250	70906653
Eyelid irritation	21.56	16.27	6	11535	371	70916532
Photopsia	21.29	16.27	12	11529	4909	70911994
Hypothermia	20.91	16.27	21	11520	20573	70896330
Conjunctival scar	20.59	16.27	5	11536	180	70916723
Product quality issue	20.36	16.27	25	11516	30536	70886367
Vitreous floaters	20.31	16.27	13	11528	6691	70910212
Skin irritation	20.08	16.27	15	11526	9894	70907009
Deep anterior chamber of the eye	19.88	16.27	3	11538	6	70916897
Giant papillary conjunctivitis	19.56	16.27	3	11538	7	70916896
Eyelid disorder	19.46	16.27	8	11533	1636	70915267
Blindness unilateral	19.28	16.27	13	11528	7300	70909603
Corneal infection	19.24	16.27	4	11537	70	70916833
Endocrine ophthalmopathy	19.23	16.27	6	11535	553	70916350
Conjunctival oedema	18.81	16.27	7	11534	1099	70915804
Prostaglandin analogue periorbitopathy	18.35	16.27	3	11538	12	70916891
Floppy iris syndrome	17.50	16.27	5	11536	340	70916563
Panophthalmitis	17.28	16.27	4	11537	117	70916786
Brain stem haematoma	17.21	16.27	4	11537	119	70916784
Eyelid margin crusting	16.82	16.27	6	11535	835	70916068
Drug ineffective	16.65	16.27	229	11312	939523	69977380
Eye complication associated with device	16.58	16.27	3	11538	24	70916879

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.64	Basic
pKa2	1.82	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	AGONIST	EC50	8.47	WOMBAT-PK	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	AGONIST	EC50	7.26	WOMBAT-PK	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	EC50	8.39	WOMBAT-PK	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.07	DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	5.27	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.84	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	5.55	CHEMBL
Alpha-2B adrenergic receptor	GPCR		ADA2B_RAT		Ki	7.28	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	5.59	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		EC50	5.95	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Ki	7.52	CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		Ki	6.13	CHEMBL
Alpha-1B adrenergic receptor	GPCR		G3HDX1_CRIGR		EC50	6.03	CHEMBL

External reference:

ID	Source
E6GNX3HHTE	UNII
D02076	KEGG_DRUG
70359-46-5	SECONDARY_CAS_RN
134615	RXNORM
4021002	VANDF
4024043	VANDF
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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
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
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/Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0591-2422	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	22 sections
Brimonidine Tartrate and Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0781-7186	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	23 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	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
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
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