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

Stem definition	Drug id	CAS RN
humanized origin	5363	1531589-13-5

Description:

Molecule	Description
Synonyms: brolucizumab brolucizumab-dbll beovu ESBA1008 ESBA-1008 RTH258 RTH-258 brolucizumab (genetical recombination)	Brolucizumab-dbll is a humanized monoclonal single-chain Fv (scFv) antibody fragmentand a human VEGF inhibitor. Brolucizumab binds to the three major isoforms of VEGF-A (e.g., VEGF110, VEGF121, and VEGF165), thereby preventing interaction with receptors VEGFR-1 and VEGFR-2. By inhibiting VEGF-A, brolucizumab suppresses endothelial cell proliferation, neovascularization, and vascular permeability. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

brolucizumab
brolucizumab-dbll
beovu
ESBA1008
ESBA-1008
RTH258
RTH-258
brolucizumab (genetical recombination)

Brolucizumab-dbll is a humanized monoclonal single-chain Fv (scFv) antibody fragmentand a human VEGF inhibitor. Brolucizumab binds to the three major isoforms of VEGF-A (e.g., VEGF110, VEGF121, and VEGF165), thereby preventing interaction with receptors VEGFR-1 and VEGFR-2. By inhibiting VEGF-A, brolucizumab suppresses endothelial cell proliferation, neovascularization, and vascular permeability.

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
Feb. 13, 2020	EMA	Novartis Europharm Limited
Oct. 7, 2019	FDA	NOVARTIS PHARMS CORP
March 25, 2020	PMDA	Novartis Pharma K.K.

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
Vitreous floaters	1225.25	133.86	226	3805	5740	63479251
Retinal vasculitis	1187.89	133.86	171	3860	803	63484188
Vitritis	1042.69	133.86	153	3878	839	63484152
Eye inflammation	827.22	133.86	161	3870	5438	63479553
Anterior chamber cell	786.92	133.86	111	3920	433	63484558
Uveitis	729.87	133.86	167	3864	12386	63472605
Keratic precipitates	690.56	133.86	87	3944	95	63484896
Visual acuity reduced	618.77	133.86	163	3868	21663	63463328
Vitreous opacities	597.93	133.86	82	3949	245	63484746
Retinal artery occlusion	465.14	133.86	82	3949	1571	63483420
Visual impairment	447.49	133.86	176	3855	84270	63400721
Vision blurred	443.38	133.86	179	3852	91745	63393246
Retinal vascular occlusion	402.61	133.86	60	3971	367	63484624
Iridocyclitis	362.49	133.86	71	3960	2451	63482540
Eye pain	334.43	133.86	112	3919	33742	63451249
Iritis	299.61	133.86	63	3968	3112	63481879
Blindness	288.51	133.86	90	3941	21609	63463382
Vitreal cells	273.24	133.86	34	3997	30	63484961
Anterior chamber inflammation	262.76	133.86	40	3991	287	63484704
Ocular hyperaemia	235.51	133.86	80	3951	25064	63459927
Anterior chamber flare	229.17	133.86	30	4001	54	63484937
Retinal perivascular sheathing	222.53	133.86	26	4005	3	63484988
Retinal haemorrhage	208.99	133.86	51	3980	4918	63480073
Blindness transient	207.30	133.86	48	3983	3696	63481295
Subretinal fluid	199.01	133.86	33	3998	429	63484562
Vitreous haze	187.69	133.86	24	4007	32	63484959
Retinal exudates	171.44	133.86	31	4000	685	63484306
Retinal oedema	146.15	133.86	27	4004	674	63484317
Intra-ocular injection complication	140.11	133.86	17	4014	9	63484982

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
Vitreous opacities	754.92	213.88	104	2514	263	34954050
Vitreous floaters	746.30	213.88	141	2477	3444	34950869
Retinal vasculitis	610.69	213.88	88	2530	338	34953975
Eye inflammation	548.57	213.88	101	2517	2117	34952196
Vitritis	517.01	213.88	84	2534	807	34953506
Anterior chamber cell	509.95	213.88	74	2544	301	34954012
Keratic precipitates	494.74	213.88	65	2553	95	34954218
Visual acuity reduced	435.63	213.88	120	2498	16029	34938284
Uveitis	348.25	213.88	86	2532	7449	34946864
Vision blurred	337.63	213.88	127	2491	45836	34908477
Anterior chamber inflammation	314.07	213.88	47	2571	245	34954068
Retinal perivascular sheathing	291.34	213.88	35	2583	7	34954306
Iritis	288.54	213.88	55	2563	1386	34952927
Subretinal fluid	276.17	213.88	44	2574	366	34953947
Visual impairment	244.65	213.88	94	2524	35708	34918605

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
Vitreous floaters	1647.37	162.54	302	5078	6954	79732054
Retinal vasculitis	1451.00	162.54	214	5166	1139	79737869
Vitritis	1189.51	162.54	187	5193	1607	79737401
Eye inflammation	1130.84	162.54	216	5164	6197	79732811
Vitreous opacities	1124.19	162.54	157	5223	518	79738490
Anterior chamber cell	1055.06	162.54	155	5225	794	79738214
Keratic precipitates	935.16	162.54	124	5256	239	79738769
Visual acuity reduced	850.45	162.54	226	5154	29243	79709765
Uveitis	828.71	162.54	198	5182	16632	79722376
Vision blurred	655.10	162.54	251	5129	105647	79633361
Anterior chamber inflammation	523.66	162.54	79	5301	495	79738513
Iritis	520.35	162.54	104	5276	3751	79735257
Retinal artery occlusion	518.21	162.54	101	5279	3193	79735815
Visual impairment	504.00	162.54	200	5180	91931	79647077
Retinal vascular occlusion	466.51	162.54	72	5308	535	79738473
Retinal perivascular sheathing	450.11	162.54	54	5326	17	79738991
Iridocyclitis	440.79	162.54	90	5290	3614	79735394
Subretinal fluid	372.86	162.54	62	5318	770	79738238
Blindness	363.19	162.54	116	5264	28267	79710741
Eye pain	354.47	162.54	122	5258	37456	79701552
Retinal haemorrhage	349.05	162.54	86	5294	8131	79730877
Blindness transient	340.07	162.54	76	5304	4700	79734308
Vitreal cells	326.55	162.54	41	5339	37	79738971
Anterior chamber flare	320.61	162.54	44	5336	121	79738887
Retinal oedema	282.49	162.54	50	5330	915	79738093
Visual acuity reduced transiently	267.06	162.54	40	5340	236	79738772
Vitreous haze	261.50	162.54	35	5345	74	79738934
Ocular hyperaemia	244.31	162.54	86	5294	28120	79710888
Intraocular pressure increased	197.01	162.54	56	5324	9149	79729859

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	S01LA06	SENSORY ORGANS OPHTHALMOLOGICALS OCULAR VASCULAR DISORDER AGENTS Antineovascularisation agents

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Macular edema due to diabetes mellitus	indication	312912001	DOID:9191
Exudative age-related macular degeneration	indication	414173003	DOID:10873
Eye infection	contraindication	128351009
Uveitis	contraindication	128473001	DOID:13141

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Vascular endothelial growth factor A	Secreted	P15692	VEGFA_HUMAN	INHIBITOR	Kd	8.80		IUPHAR	DRUG LABEL

External reference:

ID	Source
CHEMBL3707357	ChEMBL_ID
D11083	KEGG_DRUG
C000622091	MESH_SUPPLEMENTAL_RECORD_UI
8713	IUPHAR_LIGAND_ID
DB14864	DRUGBANK_ID
018166	NDDF
819963008	SNOMEDCT_US
819985002	SNOMEDCT_US
4038779	VANDF
4038780	VANDF
C4550124	UMLSCUI
10053	INN_ID
2204915	RXNORM
324861	MMSL
37505	MMSL
37526	MMSL
XSZ53G39H5	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BEOVU	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0827	INJECTION, SOLUTION	6 mg	INTRAVITREAL	BLA	27 sections
BEOVU	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0827	INJECTION, SOLUTION	6 mg	INTRAVITREAL	BLA	27 sections
BEOVU	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0827	INJECTION, SOLUTION	6 mg	INTRAVITREAL	BLA	27 sections