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

Stem definitionDrug idCAS RN
humanized origin 5363 1531589-13-5

Description:

MoleculeDescription

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:

DateAgencyCompanyOrphan
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 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
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 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
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 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
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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Vascular endothelial growth factor A Secreted INHIBITOR Kd 8.80 IUPHAR DRUG LABEL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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