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

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

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Bayer Yakuhin, Ltd
Nov. 22, 2012 EMA
Nov. 18, 2011 FDA REGENERON PHARMACEUTICALS

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
Visual acuity reduced 629.12 29.59 186 6753 21640 63460443
Endophthalmitis 620.12 29.59 129 6810 3463 63478620
Blindness 501.15 29.59 156 6783 21543 63460540
Visual impairment 348.18 29.59 174 6765 84272 63397811
Eye inflammation 345.41 29.59 87 6852 5512 63476571
Vitreous floaters 320.40 29.59 83 6856 5883 63476200
Vitritis 294.17 29.59 56 6883 936 63481147
Non-infectious endophthalmitis 256.58 29.59 39 6900 144 63481939
Blindness transient 215.17 29.59 55 6884 3689 63478394
Blindness unilateral 205.07 29.59 59 6880 6182 63475901
Retinal haemorrhage 195.12 29.59 54 6885 4915 63477168
Anterior chamber cell 194.77 29.59 36 6903 508 63481575
Vitreous opacities 178.84 29.59 31 6908 296 63481787
Uveitis 172.10 29.59 61 6878 12492 63469591
Eye pain 160.82 29.59 77 6862 33777 63448306
Detachment of retinal pigment epithelium 159.82 29.59 29 6910 367 63481716
Death 132.00 29.59 182 6757 374199 63107884
Retinal vasculitis 128.19 29.59 28 6911 946 63481137
Vitreous haemorrhage 127.07 29.59 32 6907 2018 63480065
Subretinal fluid 124.03 29.59 24 6915 438 63481645
Vitrectomy 118.42 29.59 20 6919 161 63481922
Hypopyon 113.01 29.59 24 6915 708 63481375
Hypertension 110.84 29.59 144 6795 279159 63202924
Vision blurred 106.96 29.59 85 6854 91839 63390244
Anterior chamber inflammation 106.61 29.59 20 6919 307 63481776
Retinal oedema 102.63 29.59 22 6917 679 63481404
Vitreous disorder 100.18 29.59 16 6923 87 63481996
Keratic precipitates 97.80 29.59 17 6922 165 63481918
Proteinuria 92.24 29.59 44 6895 19101 63462982
Neutropenia 86.68 29.59 101 6838 174904 63307179
Eye haemorrhage 75.25 29.59 30 6909 8466 63473617
Age-related macular degeneration 74.41 29.59 17 6922 706 63481377
Vitreous haze 71.45 29.59 11 6928 45 63482038
Product use issue 69.70 29.59 102 6837 220418 63261665
Retinal artery occlusion 69.66 29.59 19 6920 1634 63480449
Polypoidal choroidal vasculopathy 68.39 29.59 11 6928 63 63482020
Hypertensive crisis 67.19 29.59 33 6906 15253 63466830
Iritis 65.54 29.59 21 6918 3154 63478929
Choroidal neovascularisation 64.02 29.59 13 6926 306 63481777
Intra-ocular injection complication 63.55 29.59 9 6930 17 63482066
Disease progression 60.96 29.59 71 6868 122687 63359396
Retinal pigment epithelial tear 60.63 29.59 12 6927 247 63481836
Intraocular pressure increased 59.22 29.59 23 6916 6055 63476028
Macular oedema 57.54 29.59 20 6919 3857 63478226
Retinal vascular occlusion 54.65 29.59 12 6927 415 63481668
Hypotony of eye 53.77 29.59 10 6929 146 63481937
Metamorphopsia 51.97 29.59 14 6925 1149 63480934
Visual field defect 50.67 29.59 21 6918 6540 63475543
Iridocyclitis 49.27 29.59 16 6923 2506 63479577
Vitreal cells 48.35 29.59 8 6931 56 63482027
Retinal depigmentation 47.48 29.59 10 6929 283 63481800
Macular hole 46.64 29.59 12 6927 824 63481259
Diarrhoea 44.05 29.59 174 6765 715192 62766891
Retinal vein occlusion 43.52 29.59 14 6925 2129 63479954
Retinal ischaemia 40.04 29.59 9 6930 347 63481736
Anterior chamber flare 39.47 29.59 7 6932 77 63482006
Retinal exudates 38.59 29.59 10 6929 706 63481377
Stomatitis haemorrhagic 38.33 29.59 6 6933 28 63482055
Retinal disorder 38.28 29.59 12 6927 1678 63480405
Multiple-drug resistance 38.08 29.59 16 6923 5154 63476929
Neovascular age-related macular degeneration 38.03 29.59 8 6931 225 63481858
Ocular hyperaemia 37.48 29.59 27 6912 25117 63456966
Retinal detachment 35.87 29.59 16 6923 5953 63476130
Vena cava thrombosis 35.24 29.59 12 6927 2175 63479908
Cataract 33.42 29.59 36 6903 57017 63425066
Choroidal effusion 32.34 29.59 8 6931 468 63481615
Cardiac myxoma 32.31 29.59 7 6932 227 63481856
Bacterial endophthalmitis 30.77 29.59 6 6933 114 63481969
Stomatitis 29.86 29.59 54 6885 138671 63343412

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
Visual acuity reduced 750.82 28.18 239 8238 15910 34932544
Endophthalmitis 416.67 28.18 108 8369 3400 34945054
Retinal haemorrhage 315.04 28.18 94 8383 4995 34943459
Eye inflammation 257.06 28.18 67 8410 2151 34946303
Polypoidal choroidal vasculopathy 242.13 28.18 41 8436 129 34948325
Vitritis 228.03 28.18 51 8426 840 34947614
Subretinal fluid 200.08 28.18 40 8437 370 34948084
Blindness 190.14 28.18 86 8391 14900 34933554
Non-infectious endophthalmitis 189.72 28.18 33 8444 127 34948327
Detachment of retinal pigment epithelium 179.13 28.18 38 8439 482 34947972
Blindness transient 177.11 28.18 50 8427 2176 34946278
Vitreous opacities 174.27 28.18 35 8442 332 34948122
Age-related macular degeneration 141.41 28.18 29 8448 308 34948146
Proteinuria 140.48 28.18 75 8402 18567 34929887
Blindness unilateral 138.20 28.18 49 8428 4493 34943961
Vitreous floaters 129.64 28.18 44 8433 3541 34944913
Retinal oedema 127.76 28.18 30 8447 618 34947836
Visual impairment 127.20 28.18 89 8388 35713 34912741
Hypertension 115.23 28.18 153 8324 136290 34812164
Eye pain 112.33 28.18 58 8419 13404 34935050
Intraocular pressure increased 112.19 28.18 44 8433 5339 34943115
Anterior chamber inflammation 110.12 28.18 23 8454 269 34948185
Disease progression 108.28 28.18 132 8345 107945 34840509
Vitrectomy 107.49 28.18 20 8457 121 34948333
Vitreous haemorrhage 105.33 28.18 34 8443 2339 34946115
Macular hole 104.75 28.18 21 8456 197 34948257
Choroidal neovascularisation 96.87 28.18 20 8457 220 34948234
Macular oedema 94.61 28.18 33 8444 2881 34945573
Colitis microscopic 93.68 28.18 31 8446 2306 34946148
Retinal pigment epithelial tear 93.59 28.18 20 8457 263 34948191
Anterior chamber cell 93.40 28.18 21 8456 354 34948100
Dry age-related macular degeneration 91.20 28.18 17 8460 104 34948350
Neutropenia 90.52 28.18 147 8330 156631 34791823
Intra-ocular injection complication 90.30 28.18 13 8464 6 34948448
Vision blurred 87.13 28.18 79 8398 45884 34902570
Proteus infection 84.16 28.18 24 8453 1082 34947372
Diarrhoea 83.21 28.18 244 8233 389668 34558786
Uveitis 82.28 28.18 39 8438 7496 34940958
Hypopyon 81.58 28.18 19 8458 377 34948077
Retinal detachment 74.91 28.18 33 8444 5358 34943096
Eye haemorrhage 68.49 28.18 29 8448 4276 34944178
Prothrombin level decreased 66.14 28.18 20 8457 1108 34947346
Retinal vasculitis 64.80 28.18 16 8461 410 34948044
Induration 64.60 28.18 19 8458 956 34947498
Vitreous disorder 62.37 28.18 12 8465 89 34948365
Necrotising fasciitis 58.97 28.18 25 8452 3697 34944757
Corneal oedema 58.50 28.18 19 8458 1332 34947122
Clostridial infection 56.27 28.18 24 8453 3603 34944851
Neovascular age-related macular degeneration 53.78 28.18 12 8465 195 34948259
Keratic precipitates 51.17 28.18 11 8466 149 34948305
Serous retinal detachment 49.82 28.18 14 8463 598 34947856
Iritis 49.41 28.18 17 8460 1424 34947030
Stomatitis 49.20 28.18 56 8421 42458 34905996
Death 48.96 28.18 208 8269 397841 34550613
Retinal artery occlusion 44.95 28.18 17 8460 1868 34946586
Neutrophilia 40.88 28.18 20 8457 4117 34944337
Macular degeneration 39.06 28.18 16 8461 2170 34946284
Drug interaction 37.97 28.18 5 8472 225941 34722513
Klebsiella infection 36.92 28.18 24 8453 8507 34939947
Mucosal inflammation 36.66 28.18 46 8431 38576 34909878
Stoma site haemorrhage 36.44 28.18 12 8465 878 34947576
Intestinal perforation 35.61 28.18 24 8453 9036 34939418
Ocular hyperaemia 34.96 28.18 26 8451 11426 34937028
Blood lactic acid increased 34.31 28.18 21 8456 6707 34941747
Retinal degeneration 33.94 28.18 10 8467 506 34947948
Retinal scar 33.92 28.18 9 8468 309 34948145
Diaphragmatic operation 33.21 28.18 6 8471 30 34948424
Skin toxicity 32.53 28.18 18 8459 4766 34943688
Visual acuity reduced transiently 32.34 28.18 7 8470 98 34948356
Retinal depigmentation 31.24 28.18 6 8471 44 34948410
Tenderness 31.22 28.18 20 8457 6914 34941540
Ocular hypertension 29.10 28.18 10 8467 834 34947620
Dysphonia 29.09 28.18 32 8445 23351 34925103
Pelvic fluid collection 28.87 28.18 7 8470 166 34948288
Hiccups 28.80 28.18 22 8455 10060 34938394
Retinal vein occlusion 28.74 28.18 12 8465 1707 34946747
Epistaxis 28.68 28.18 51 8426 58200 34890254
Vitreous detachment 28.60 28.18 10 8467 878 34947576
Anterior chamber flare 28.35 28.18 6 8471 75 34948379

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
Visual acuity reduced 1216.74 24.61 368 13425 29101 79701494
Endophthalmitis 794.36 24.61 191 13602 6237 79724358
Eye inflammation 534.28 24.61 139 13654 6274 79724321
Vitritis 478.21 24.61 100 13693 1694 79728901
Retinal haemorrhage 450.07 24.61 128 13665 8089 79722506
Vitreous opacities 378.03 24.61 70 13723 605 79729990
Vitreous floaters 330.66 24.61 98 13695 7158 79723437
Polypoidal choroidal vasculopathy 305.45 24.61 50 13743 187 79730408
Non-infectious endophthalmitis 288.76 24.61 50 13743 281 79730314
Blindness transient 264.17 24.61 75 13718 4701 79725894
Detachment of retinal pigment epithelium 261.44 24.61 53 13740 763 79729832
Subretinal fluid 260.42 24.61 53 13740 779 79729816
Blindness 259.38 24.61 117 13676 28266 79702329
Anterior chamber cell 259.25 24.61 54 13739 895 79729700
Blindness unilateral 240.73 24.61 79 13714 8067 79722528
Death 226.37 24.61 373 13420 566141 79164454
Eye pain 225.23 24.61 116 13677 37462 79693133
Proteinuria 220.16 24.61 109 13684 32393 79698202
Hypertension 213.97 24.61 274 13519 330718 79399877
Vitreous haemorrhage 213 24.61 60 13733 3653 79726942
Anterior chamber inflammation 212.16 24.61 42 13751 532 79730063
Uveitis 201.59 24.61 84 13709 16746 79713849
Retinal oedema 190.41 24.61 42 13751 923 79729672
Intra-ocular injection complication 188.71 24.61 27 13766 26 79730569
Intraocular pressure increased 177.84 24.61 65 13728 9140 79721455
Vitrectomy 175.08 24.61 31 13762 202 79730393
Age-related macular degeneration 173.56 24.61 39 13754 935 79729660
Neutropenia 169.95 24.61 228 13565 287482 79443113
Retinal artery occlusion 169.92 24.61 49 13744 3245 79727350
Visual impairment 169.91 24.61 135 13658 91996 79638599
Retinal vasculitis 165.94 24.61 40 13753 1313 79729282
Hypopyon 162.11 24.61 38 13755 1104 79729491
Disease progression 160.75 24.61 178 13615 184184 79546411
Vision blurred 145.51 24.61 131 13662 105767 79624828
Retinal pigment epithelial tear 141.18 24.61 29 13764 447 79730148
Vitreous disorder 139.33 24.61 26 13767 235 79730360
Choroidal neovascularisation 129.63 24.61 27 13766 447 79730148
Macular hole 120.13 24.61 28 13765 793 79729802
Diarrhoea 119.81 24.61 378 13415 880111 78850484
Keratic precipitates 112.86 24.61 23 13770 340 79730255
Vitreal cells 111.56 24.61 18 13775 60 79730535
Macular oedema 110.74 24.61 40 13753 5434 79725161
Eye haemorrhage 101.23 24.61 44 13749 9713 79720882
Retinal detachment 96.92 24.61 42 13751 9205 79721390
Colitis microscopic 90.78 24.61 42 13751 10726 79719869
Iritis 81.10 24.61 29 13764 3826 79726769
Corneal oedema 75.73 24.61 25 13768 2595 79728000
Retinal vascular occlusion 74.71 24.61 18 13775 589 79730006
Proteus infection 72.60 24.61 23 13770 2095 79728500
Vitreous haze 71.99 24.61 13 13780 96 79730499
Neovascular age-related macular degeneration 65.61 24.61 15 13778 389 79730206
Dry age-related macular degeneration 64.66 24.61 14 13779 281 79730314
Retinal depigmentation 63.31 24.61 14 13779 311 79730284
Stomatitis 61.32 24.61 99 13694 146658 79583937
Prothrombin level decreased 61.14 24.61 19 13774 1625 79728970
Anterior chamber flare 60.53 24.61 12 13781 153 79730442
Visual field defect 60.20 24.61 30 13763 9015 79721580
Visual acuity reduced transiently 59.94 24.61 13 13780 263 79730332
Multiple use of single-use product 57.87 24.61 16 13777 908 79729687
Metamorphopsia 56.86 24.61 17 13776 1276 79729319
Retinal ischaemia 55.66 24.61 15 13778 773 79729822
Retinal vein occlusion 55.16 24.61 21 13772 3302 79727293
Induration 53.92 24.61 18 13775 1934 79728661
Necrotising fasciitis 52.25 24.61 24 13769 6026 79724569
Serous retinal detachment 51.63 24.61 15 13778 1019 79729576
Clostridial infection 50.39 24.61 23 13770 5691 79724904
Dysphonia 49.58 24.61 55 13738 56817 79673778
Mucosal inflammation 49.24 24.61 63 13730 75517 79655078
Epistaxis 49.00 24.61 77 13716 111438 79619157
Hypertensive crisis 48.31 24.61 35 13758 20735 79709860
Ocular hyperaemia 46.99 24.61 39 13754 28167 79702428
Iridocyclitis 46.06 24.61 19 13774 3685 79726910
Drug interaction 44.26 24.61 9 13784 415174 79315421
Retinal disorder 41.56 24.61 15 13778 2032 79728563
Proctalgia 40.87 24.61 24 13769 9977 79720618
Retinal exudates 40.63 24.61 13 13780 1222 79729373
Pseudoendophthalmitis 39.22 24.61 7 13786 48 79730547
Retinal scar 39.14 24.61 10 13783 418 79730177
Joint swelling 38.57 24.61 3 13790 288643 79441952
Arthralgia 38.36 24.61 26 13767 571777 79158818
Nephrotic syndrome 35.91 24.61 23 13770 11151 79719444
Klebsiella infection 35.44 24.61 26 13767 15694 79714901
Intestinal perforation 35.23 24.61 27 13766 17399 79713196
Diaphragmatic operation 35.23 24.61 6 13787 30 79730565
Rash 34.09 24.61 30 13763 578328 79152267
Cataract 33.15 24.61 47 13746 62073 79668522
Vena cava thrombosis 33.14 24.61 14 13779 2881 79727714
Hiccups 33.11 24.61 21 13772 10010 79720585
Vitreous detachment 32.96 24.61 13 13780 2246 79728349
Cerebral infarction 32.82 24.61 40 13753 45636 79684959
Retinal degeneration 32.31 24.61 11 13782 1255 79729340
Neutrophilia 32.28 24.61 19 13774 7932 79722663
Stoma site haemorrhage 31.41 24.61 12 13781 1904 79728691
Pain 31.18 24.61 46 13747 703756 79026839
Retinal perivascular sheathing 31.16 24.61 6 13787 65 79730530
Diabetic retinal oedema 30.93 24.61 8 13785 351 79730244
Nasopharyngitis 30.39 24.61 4 13789 253877 79476718
General physical health deterioration 29.87 24.61 110 13683 275128 79455467
Drug intolerance 29.68 24.61 5 13788 264114 79466481
Macular fibrosis 29.61 24.61 9 13784 714 79729881
Gastrointestinal toxicity 29.35 24.61 18 13775 8091 79722504
Eye irritation 29.17 24.61 26 13767 20655 79709940
Pulmonary embolism 29.08 24.61 80 13713 171574 79559021
Ocular discomfort 28.72 24.61 15 13778 4968 79725627
Stomatitis haemorrhagic 28.65 24.61 6 13787 102 79730493
Hypotony of eye 28.43 24.61 7 13786 251 79730344
Glaucoma 28.18 24.61 25 13768 19736 79710859
Asthenia 27.77 24.61 167 13626 511522 79219073
Abdominal discomfort 27.62 24.61 5 13788 250722 79479873
Off label use 27.58 24.61 258 13535 906957 78823638
Rectal haemorrhage 27.22 24.61 48 13745 76252 79654343
Insomnia 26.77 24.61 5 13788 245165 79485430
Blood lactic acid increased 26.32 24.61 20 13773 12724 79717871
Retinal tear 26.14 24.61 10 13783 1592 79729003
Eye infection staphylococcal 25.53 24.61 6 13787 176 79730419
Palmar-plantar erythrodysaesthesia syndrome 25.41 24.61 30 13763 33104 79697491
Retinal occlusive vasculitis 24.79 24.61 5 13788 70 79730525
Conjunctival hyperaemia 24.63 24.61 13 13780 4400 79726195

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
MeSH PA D020533 Angiogenesis Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D006131 Growth Inhibitors
MeSH PA D006133 Growth Substances
FDA MoA N0000193542 Vascular Endothelial Growth Factor Inhibitors
FDA EPC N0000193543 Vascular Endothelial Growth Factor Inhibitor

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

DiseaseRelationSNOMED_IDDOID
Central retinal vein occlusion with macular edema indication 232039004
Branch retinal vein occlusion with macular edema indication 232048009
Neovascular glaucoma indication 232086000 DOID:1687
Macular edema due to diabetes mellitus indication 312912001 DOID:9191
Metastasis from malignant tumor of colon indication 314998002
Exudative age-related macular degeneration indication 414173003 DOID:10873
Retinopathy of prematurity indication 415297005 DOID:13025




🐶 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 12.30 DRUG LABEL DRUG LABEL
Placenta growth factor Secreted INHIBITOR Kd 10.41 DRUG LABEL DRUG LABEL
Vascular endothelial growth factor B Secreted INHIBITOR Kd 11.72 DRUG LABEL DRUG LABEL

External reference:

IDSource
15C2VL427D UNII
D09574 KEGG_DRUG
4031234 VUID
N0000184016 NUI
4031234 VANDF
4031980 VANDF
C1134659 UMLSCUI
CHEMBL1742982 ChEMBL_ID
DB08885 DRUGBANK_ID
8739 INN_ID
C533178 MESH_SUPPLEMENTAL_RECORD_UI
6786 IUPHAR_LIGAND_ID
1232150 RXNORM
186189 MMSL
192290 MMSL
28208 MMSL
28701 MMSL
d07888 MMSL
014044 NDDF
015046 NDDF
703840003 SNOMEDCT_US
714627007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ZALTRAP HUMAN PRESCRIPTION DRUG LABEL 1 0024-5840 SOLUTION, CONCENTRATE 100 mg INTRAVENOUS BLA 32 sections
ZALTRAP HUMAN PRESCRIPTION DRUG LABEL 1 0024-5841 SOLUTION, CONCENTRATE 200 mg INTRAVENOUS BLA 32 sections
EYLEA HUMAN PRESCRIPTION DRUG LABEL 1 61755-005 INJECTION, SOLUTION 40 mg INTRAVITREAL BLA 30 sections
EYLEA HUMAN PRESCRIPTION DRUG LABEL 1 61755-005 INJECTION, SOLUTION 40 mg INTRAVITREAL BLA 30 sections
EYLEA HUMAN PRESCRIPTION DRUG LABEL 1 61755-005 INJECTION, SOLUTION 40 mg INTRAVITREAL BLA 30 sections
EYLEA HD HUMAN PRESCRIPTION DRUG LABEL 1 61755-050 INJECTION, SOLUTION 8 mg INTRAVITREAL BLA 29 sections
EYLEA HD HUMAN PRESCRIPTION DRUG LABEL 1 61755-051 INJECTION, SOLUTION 8 mg INTRAVITREAL BLA 29 sections