All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

brolucizumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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
Retinal vasculitis	1417.43	111.71	206	4478	1335	90622428
Vitreous floaters	1333.80	111.71	244	4440	7305	90616458
Vitritis	1228.59	111.71	183	4501	1431	90622332
Eye inflammation	1013.63	111.71	195	4489	7656	90616107
Uveitis	848.89	111.71	190	4494	15713	90608050
Keratic precipitates	832.16	111.71	107	4577	216	90623547
Visual acuity reduced	811.61	111.71	197	4487	23213	90600550
Anterior chamber cell	808.08	111.71	115	4569	621	90623142
Vitreous opacities	666.96	111.71	92	4592	378	90623385
Vision blurred	517.75	111.71	199	4485	110094	90513669
Retinal artery occlusion	508.78	111.71	90	4594	2181	90621582
Visual impairment	485.96	111.71	200	4484	132165	90491598
Retinal vascular occlusion	444.64	111.71	64	4620	377	90623386
Iridocyclitis	435.10	111.71	85	4599	3576	90620187
Eye pain	387.35	111.71	127	4557	44041	90579722
Anterior chamber inflammation	329.65	111.71	49	4635	371	90623392
Blindness	326.92	111.71	99	4585	26469	90597294
Subretinal fluid	311.59	111.71	50	4634	654	90623109
Iritis	308.91	111.71	64	4620	3622	90620141
Anterior chamber flare	300.69	111.71	39	4645	86	90623677
Ocular hyperaemia	275.31	111.71	92	4592	33706	90590057
Vitreal cells	266.33	111.71	35	4649	89	90623674
Retinal perivascular sheathing	255.14	111.71	31	4653	28	90623735
Retinal haemorrhage	232.63	111.71	55	4629	5709	90618054
Retinal oedema	210.23	111.71	38	4646	1038	90622725
Vitreous haze	203.86	111.71	26	4658	47	90623716
Blindness transient	202.53	111.71	47	4637	4496	90619267
Retinal exudates	185.45	111.71	32	4652	664	90623099
Retinal occlusive vasculitis	166.03	111.71	25	4659	208	90623555
Retinal ischaemia	163.05	111.71	27	4657	433	90623330
Intraocular pressure increased	143.54	111.71	39	4645	7054	90616709
Chorioretinitis	140.60	111.71	26	4658	807	90622956
Detachment of retinal pigment epithelium	126.29	111.71	22	4662	483	90623280
Intra-ocular injection complication	120.28	111.71	16	4668	46	90623717
Metamorphopsia	114.48	111.71	24	4660	1433	90622330

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	836.76	199.00	117	2962	359	42617897
Vitreous floaters	783.43	199.00	150	2929	4080	42614176
Retinal vasculitis	681.45	199.00	102	2977	561	42617695
Eye inflammation	607.10	199.00	116	2963	3102	42615154
Vitritis	602.79	199.00	100	2979	1149	42617107
Keratic precipitates	562.27	199.00	76	3003	164	42618092
Anterior chamber cell	550.41	199.00	81	2998	387	42617869
Visual acuity reduced	508.83	199.00	137	2942	17413	42600843
Subretinal fluid	390.08	199.00	64	3015	679	42617577
Uveitis	382.96	199.00	96	2983	9162	42609094
Vision blurred	361.73	199.00	138	2941	53561	42564695
Anterior chamber inflammation	345.22	199.00	53	3026	351	42617905
Iritis	315.55	199.00	61	3018	1721	42616535
Retinal perivascular sheathing	313.82	199.00	39	3040	25	42618231
Visual impairment	287.08	199.00	110	2969	43003	42575253
Retinal oedema	285.69	199.00	51	3028	917	42617339
Visual acuity reduced transiently	227.97	199.00	32	3047	100	42618156
Blindness	227.32	199.00	74	3005	17904	42600352
Retinal haemorrhage	219.35	199.00	56	3023	5714	42612542
Blindness transient	215.29	199.00	48	3031	2741	42615515
Iridocyclitis	215.00	199.00	46	3033	2165	42616091

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	1785.13	156.68	326	5926	8808	110574239
Retinal vasculitis	1674.44	156.68	250	6002	1799	110581248
Vitritis	1417.40	156.68	224	6028	2429	110580618
Eye inflammation	1343.78	156.68	257	5995	8914	110574133
Vitreous opacities	1279.29	156.68	178	6074	711	110582336
Keratic precipitates	1139.43	156.68	152	6100	404	110582643
Anterior chamber cell	1128.64	156.68	166	6086	1055	110581992
Visual acuity reduced	1087.72	156.68	270	5982	31903	110551144
Uveitis	937.09	156.68	222	6030	21488	110561559
Vision blurred	732.62	156.68	274	5978	128748	110454299
Anterior chamber inflammation	604.83	156.68	91	6161	684	110582363
Subretinal fluid	590.41	156.68	96	6156	1248	110581799
Visual impairment	576.26	156.68	233	6019	134195	110448852
Retinal artery occlusion	571.30	156.68	111	6141	4138	110578909
Iritis	555.20	156.68	110	6142	4542	110578505
Iridocyclitis	515.14	156.68	106	6146	5302	110577745
Retinal vascular occlusion	507.33	156.68	76	6176	552	110582495
Retinal perivascular sheathing	488.10	156.68	60	6192	55	110582992
Eye pain	422.23	156.68	143	6109	49956	110533091
Retinal oedema	421.61	156.68	74	6178	1553	110581494
Blindness	412.49	156.68	130	6122	36229	110546818
Retinal haemorrhage	392.73	156.68	94	6158	9407	110573640
Anterior chamber flare	373.95	156.68	51	6201	167	110582880
Blindness transient	342.10	156.68	77	6175	5879	110577168
Vitreal cells	315.22	156.68	43	6209	141	110582906
Visual acuity reduced transiently	314.87	156.68	46	6206	274	110582773
Ocular hyperaemia	291.38	156.68	102	6150	39184	110543863
Vitreous haze	280.26	156.68	37	6215	87	110582960
Intraocular pressure increased	243.58	156.68	66	6186	10810	110572237
Idiopathic orbital inflammation	187.74	156.68	30	6222	345	110582702
Retinal ischaemia	183.49	156.68	34	6218	973	110582074
Retinal exudates	169.10	156.68	33	6219	1251	110581796
Retinal occlusive vasculitis	168.80	156.68	26	6226	231	110582816
Detachment of retinal pigment epithelium	164.49	156.68	31	6221	974	110582073

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	S01LA06	SENSORY ORGANS OPHTHALMOLOGICALS OCULAR VASCULAR DISORDER AGENTS Antineovascularisation agents
CHEBI has role	CHEBI:66981	ophthalmology drug

Related Drugs by ATC class:

S01LA Antineovascularisation agents 7 drugs

afliberceptanecortavebevacizumabfaricimabpegaptanibranibizumabverteporfin

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
4038779	VANDF
4038780	VANDF
CHEBI:755824	CHEBI
CHEMBL3707357	ChEMBL_ID
D11083	KEGG_DRUG
C000622091	MESH_SUPPLEMENTAL_RECORD_UI
8713	IUPHAR_LIGAND_ID
DB14864	DRUGBANK_ID
819963008	SNOMEDCT_US
819985002	SNOMEDCT_US
C4550124	UMLSCUI
10053	INN_ID
324861	MMSL
37505	MMSL
37526	MMSL
018166	NDDF
XSZ53G39H5	UNII
2204915	RXNORM

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	26 sections
BEOVU	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0827	INJECTION, SOLUTION	6 mg	INTRAVITREAL	BLA	26 sections