aflibercept indications/contra

Stem definitionDrug idCAS RN
vascular endothelial growth factor (VEGF) receptors 4916 862111-32-8

Description:

MoleculeDescription

Synonyms:

  • aflibercept
  • eylea
  • AVE0005
  • ziv-aflibercept
  • zaltrap
  • VEGF Trap
has antiangiogenic activity; consists of the second and third Ig domains of VEGFR1 and VEGFR2, respectively, fusion to the Fc region of IgG1; putative antineoplastic agent that binds all VEGF-A isoforms; possible medicine for eye disorders
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 2012 EMA
Nov. 18, 2011 FDA REGENERON PHARMACEUTICALS

FDA Adverse Event Reporting System

scroll-->
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
Death 1352.26 45.75 600 3292 151724 3230243
Endophthalmitis 975.28 45.75 176 3716 1343 3380624
Visual acuity reduced 919.16 45.75 228 3664 8786 3373181
Blindness 569.98 45.75 142 3750 5507 3376460
Retinal haemorrhage 561.78 45.75 119 3773 2201 3379766
Blindness transient 466.90 45.75 93 3799 1245 3380722
Visual impairment 465.81 45.75 148 3744 13998 3367969
Vitritis 439.43 45.75 71 3821 245 3381722
Non-infectious endophthalmitis 389.29 45.75 56 3836 60 3381907
Eye pain 336.47 45.75 95 3797 5952 3376015
Eye haemorrhage 323.48 45.75 73 3819 1819 3380148
Vitreous floaters 318.54 45.75 68 3824 1298 3380669
Vitreous haemorrhage 304.95 45.75 62 3830 922 3381045
Vitrectomy 299.20 45.75 45 3847 81 3381886
Eye inflammation 287.07 45.75 59 3833 928 3381039
Blindness unilateral 282.66 45.75 66 3826 1918 3380049
Diarrhoea 261.79 45.75 182 3710 104166 3277801
Macular hole 251.26 45.75 45 3847 321 3381646
Neovascular age-related macular degeneration 235.53 45.75 36 3856 76 3381891
Vision blurred 230.45 45.75 96 3796 19493 3362474
Hypertension 221.98 45.75 115 3777 38351 3343616
Uveitis 219.63 45.75 54 3838 1959 3380008
Cataract 202.69 45.75 67 3825 7109 3374858
Cataract operation 201.27 45.75 44 3848 940 3381027
Retinal oedema 186.66 45.75 36 3856 400 3381567
Intraocular pressure increased 185.54 45.75 49 3843 2373 3379594
Multiple use of single-use product 172.83 45.75 28 3864 98 3381869
Vitreous opacities 169.10 45.75 28 3864 116 3381851
Anterior chamber inflammation 165.46 45.75 27 3865 100 3381867
Detachment of retinal pigment epithelium 164.49 45.75 32 3860 373 3381594

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC L01XX44 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
ATC S01LA05 SENSORY ORGANS
OPHTHALMOLOGICALS
OCULAR VASCULAR DISORDER AGENTS
Antineovascularisation agents
FDA EPC N0000193543 Vascular Endothelial Growth Factor Inhibitor
FDA MoA N0000193542 Vascular Endothelial Growth Factor Inhibitors

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Central retinal vein occlusion with macular edema indication 232039004
Branch retinal vein occlusion with macular edema indication 232048009
Diabetic macular edema indication 312912001 DOID:9191
Metastasis from malignant tumor of colon indication 314998002
Exudative age-related macular degeneration indication 414173003 DOID:10873

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:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vascular endothelial growth factor B Secreted INHIBITOR Kd 11.72 DRUG LABEL DRUG LABEL
Placenta growth factor Secreted INHIBITOR Kd 10.41 DRUG LABEL DRUG LABEL
Vascular endothelial growth factor A Secreted INHIBITOR Kd 12.30 DRUG LABEL DRUG LABEL

External reference:

scroll-->
IDSource
6786 IUPHAR_LIGAND_ID
D09574 KEGG_DRUG
4031234 VUID
N0000184016 NUI
C1134659 UMLSCUI
15C2VL427D UNII
8739 INN_ID
1232150 RXNORM
014044 NDDF
28208 MMSL
4031234 VANDF
N0000184016 NDFRT
703840003 SNOMEDCT_US
714627007 SNOMEDCT_US
DB08885 DRUGBANK_ID
CHEMBL1742982 ChEMBL_ID
C533178 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
ZALTRAP HUMAN PRESCRIPTION DRUG LABEL 1 0024-5840 SOLUTION, CONCENTRATE 100 mg INTRAVENOUS BLA 18 sections
ZALTRAP HUMAN PRESCRIPTION DRUG LABEL 1 0024-5841 SOLUTION, CONCENTRATE 200 mg INTRAVENOUS BLA 18 sections
EYLEA HUMAN PRESCRIPTION DRUG LABEL 1 61755-005 INJECTION, SOLUTION 40 mg INTRAVITREAL BLA 16 sections