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

Stem definitionDrug idCAS RN
human origin 5366 1346452-25-2

Description:

MoleculeDescription

Synonyms:

  • enfortumab
  • enfortumab vedotin
  • enfortumab-vedotin-ejfv
  • padcev
  • AGS-22CE
  • AGS-22ME
  • AGS-22M6E
  • enfortumab vedotin (genetical recombination)
Enfortumab vedotin-ejfv is an ADC. The antibody is a human IgG1 directed against Nectin-4, an adhesion protein located on the surface of cells. The small molecule, MMAE, is a microtubule-disrupting agent, attached to the antibody via a protease-cleavable linker. Nonclinical data suggest that the anticancer activity of enfortumab vedotin-ejfv is due to the binding of the ADC to Nectin-4-expressing cells, followed by internalization of the ADC-Nectin-4 complex, and the release of MMAE via proteolytic cleavage. Release of MMAE disrupts the microtubule network within the cell, subsequently inducing cell cycle arrest and apoptotic cell death.
  • 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
Dec. 18, 2019 FDA ASTELLAS
Sept. 27, 2021 PMDA ASTELLAS PHARMA INC.
April 13, 2022 EMA ASTELLAS PHARMA EUROPE B.V.

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
Malignant neoplasm progression 441.31 39.85 160 3160 106710 90518417
Neuropathy peripheral 284.14 39.85 125 3195 136845 90488282
Skin disorder 165.95 39.85 59 3261 36647 90588480
Rash 152.96 39.85 165 3155 795935 89829192
Taste disorder 104.45 39.85 49 3271 61497 90563630
Stevens-Johnson syndrome 74.39 39.85 31 3289 29345 90595782
Skin toxicity 72.50 39.85 21 3299 6758 90618369
Pruritus 63.65 39.85 88 3232 541437 90083690
Death 59.40 39.85 78 3242 456473 90168654
Decreased appetite 49.95 39.85 65 3255 376475 90248652

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
Neuropathy peripheral 859.84 26.31 458 11209 101395 42508273
Malignant neoplasm progression 819.19 26.31 453 11214 107947 42501721
Rash 555.93 26.31 515 11152 276439 42333229
Taste disorder 439.24 26.31 147 11520 10060 42599608
Skin disorder 401.58 26.31 157 11510 16787 42592881
Hyperglycaemia 278.78 26.31 167 11500 45692 42563976
Alopecia 249.31 26.31 133 11534 29143 42580525
Stevens-Johnson syndrome 189.43 26.31 101 11566 22077 42587591
Pruritus 150.15 26.31 219 11448 188552 42421116
Therapy partial responder 145.59 26.31 82 11585 19939 42589729
Toxic epidermal necrolysis 143.41 26.31 90 11577 26660 42583008
Decreased appetite 142.03 26.31 216 11451 192921 42416747
Dermatitis bullous 128.06 26.31 57 11610 8399 42601269
Myelosuppression 122.71 26.31 96 11571 40365 42569303
Interstitial lung disease 111.83 26.31 122 11545 78340 42531328
Skin toxicity 105.14 26.31 46 11621 6503 42603165
Pulmonary toxicity 92.89 26.31 46 11621 8609 42601059
Blister 84.99 26.31 66 11601 27424 42582244
Immune-mediated adverse reaction 83.95 26.31 24 11643 964 42608704
Skin reaction 74.18 26.31 37 11630 7030 42602638
Immune-mediated enterocolitis 72.51 26.31 34 11633 5643 42604025
Inappropriate schedule of product administration 58.89 26.31 99 11568 95803 42513865
Infusion site extravasation 58.42 26.31 29 11638 5452 42604216
Adrenal insufficiency 57.53 26.31 45 11622 18879 42590789
Hepatic function abnormal 56.33 26.31 70 11597 51497 42558171
Erythema 53.58 26.31 102 11565 108691 42500977
Drug interaction 52.28 26.31 6 11661 266993 42342675
Dry eye 51.80 26.31 39 11628 15467 42594201
KL-6 increased 51.22 26.31 11 11656 130 42609538
Hypoaesthesia 50.99 26.31 79 11588 71384 42538284
Diabetic ketoacidosis 50.95 26.31 45 11622 22322 42587346
Dry skin 48.65 26.31 63 11604 48275 42561393
Drug ineffective 45.56 26.31 64 11603 630133 41979535
Diarrhoea 42.39 26.31 242 11425 460607 42149061
Underdose 40.92 26.31 35 11632 16631 42593037
Headache 40.84 26.31 8 11659 239361 42370307
Drug eruption 40.19 26.31 40 11627 23035 42586633
Metastases to liver 39.50 26.31 34 11633 16292 42593376
Immune-mediated lung disease 38.87 26.31 19 11648 3454 42606214
Pyelonephritis 38.34 26.31 25 11642 7889 42601779
Hydronephrosis 37.77 26.31 29 11638 11836 42597832
Skin exfoliation 35.47 26.31 50 11617 41503 42568165
Rash pruritic 34.12 26.31 44 11623 33559 42576109
Dry mouth 34.06 26.31 48 11619 39831 42569837
Toxic erythema of chemotherapy 33.42 26.31 8 11659 158 42609510
Pneumonitis 32.40 26.31 48 11619 41670 42567998
Lacrimation increased 31.56 26.31 26 11641 11732 42597936
Metastases to lung 30.12 26.31 25 11642 11399 42598269
Peripheral sensory neuropathy 29.17 26.31 22 11645 8740 42600928
Immune-mediated hepatic disorder 28.88 26.31 14 11653 2500 42607168
Malaise 28.32 26.31 124 11543 212032 42397636
Product use in unapproved indication 27.83 26.31 8 11659 184448 42425220
Ocular toxicity 26.81 26.31 8 11659 374 42609294

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
Malignant neoplasm progression 1291.43 27.06 560 13220 174007 110401512
Neuropathy peripheral 1016.22 27.06 478 13302 178799 110396720
Skin disorder 556.65 27.06 207 13573 42706 110532813
Rash 467.77 27.06 540 13240 820424 109755095
Taste disorder 414.56 27.06 189 13591 65198 110510321
Hyperglycaemia 288.40 27.06 161 13619 84929 110490590
Decreased appetite 209.48 27.06 276 13504 475570 110099949
Therapy partial responder 197.19 27.06 95 13685 36966 110538553
Pruritus 183.57 27.06 288 13492 581272 109994247
Toxic epidermal necrolysis 172.34 27.06 100 13680 56627 110518892
Interstitial lung disease 172.24 27.06 141 13639 139193 110436326
Stevens-Johnson syndrome 164.94 27.06 91 13689 46810 110528709
Myelosuppression 164.01 27.06 117 13663 94223 110481296
Pulmonary toxicity 143.69 27.06 61 13719 17685 110557834
Skin toxicity 138.64 27.06 53 13727 11730 110563789
Dermatitis bullous 134.49 27.06 58 13722 17471 110558048
Alopecia 127.99 27.06 190 13590 364563 110210956
Immune-mediated adverse reaction 123.81 27.06 31 13749 1669 110573850
Hepatic function abnormal 103.26 27.06 87 13693 89208 110486311
Inappropriate schedule of product administration 100.06 27.06 125 13655 203512 110372007
Immune-mediated enterocolitis 95.91 27.06 39 13741 10146 110565373
Adrenal insufficiency 79.24 27.06 55 13725 42335 110533184
Dry skin 71.12 27.06 77 13703 107576 110467943
Death 68.83 27.06 217 13563 698652 109876867
Dry eye 67.87 27.06 56 13724 55737 110519782
Immune-mediated lung disease 66.51 27.06 25 13755 5278 110570241
Headache 65.40 27.06 15 13765 882362 109693157
Erythema 64.87 27.06 124 13656 291323 110284196
Drug eruption 63.49 27.06 53 13727 53606 110521913
Diabetic ketoacidosis 61.41 27.06 47 13733 42011 110533508
Metastases to liver 59.40 27.06 43 13737 35343 110540176
Skin exfoliation 58.42 27.06 63 13717 87588 110487931
Drug ineffective 55.50 27.06 65 13715 1520475 109055044
Diarrhoea 52.13 27.06 279 13501 1139226 109436293
Hydronephrosis 51.24 27.06 32 13748 20633 110554886
Neutrophil count decreased 51.15 27.06 69 13711 120872 110454647
Infusion site extravasation 50.53 27.06 26 13754 11608 110563911
Toxic erythema of chemotherapy 48.10 27.06 11 13769 401 110575118
KL-6 increased 45.38 27.06 10 13770 307 110575212
Drug hypersensitivity 44.88 27.06 3 13777 454087 110121432
Drug interaction 42.40 27.06 6 13774 500177 110075342
Metastases to lung 40.94 27.06 29 13751 23034 110552485
Rash pruritic 38.52 27.06 54 13726 98015 110477504
Weight decreased 37.69 27.06 136 13644 467921 110107598
Eastern Cooperative Oncology Group performance status worsened 37.25 27.06 14 13766 2955 110572564
Peripheral sensory neuropathy 36.81 27.06 24 13756 16656 110558863
Pyelonephritis 36.38 27.06 28 13752 25222 110550297
Ileus 35.61 27.06 30 13750 30699 110544820
Lacrimation increased 35.42 27.06 30 13750 30920 110544599
Blood pressure systolic increased 34.55 27.06 47 13733 82944 110492575
Drug intolerance 34.15 27.06 5 13775 406507 110169012
Skin reaction 33.91 27.06 25 13755 21119 110554400
Dry mouth 33.77 27.06 76 13704 199872 110375647
Pigmentation disorder 33.67 27.06 17 13763 7294 110568225
Hypoaesthesia 33.06 27.06 100 13680 314123 110261396
Dysgeusia 32.78 27.06 42 13738 69943 110505576
Joint swelling 31.81 27.06 8 13772 442837 110132682
Skin erosion 31.09 27.06 15 13765 5839 110569680
Product use in unapproved indication 30.41 27.06 9 13771 447368 110128151
Colitis 29.77 27.06 49 13731 102274 110473245
Hypersensitivity 29.60 27.06 7 13773 403991 110171528
Pyrexia 28.89 27.06 201 13579 898064 109677455
Depression 28.85 27.06 3 13777 317332 110258187
Immune-mediated hepatic disorder 28.57 27.06 13 13767 4437 110571082
Hypothyroidism 28.42 27.06 40 13740 72859 110502660
Pneumonitis 28.37 27.06 41 13739 76490 110499029
Dyspnoea 28.20 27.06 60 13720 1106812 109468707
Swelling 27.95 27.06 5 13775 351036 110224483
Immune-mediated nephritis 27.80 27.06 9 13771 1223 110574296
Arthralgia 27.60 27.06 34 13746 779598 109795921
Ocular toxicity 27.07 27.06 9 13771 1329 110574190

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FX13 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates
CHEBI has role CHEBI:35610 antineoplastic agent

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

DiseaseRelationSNOMED_IDDOID
Metastatic urothelial carcinoma indication




🐶 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
Tubulin beta Tumour-associated antigen BINDING AGENT UNKNOWN DRUG LABEL
Nectin-4 Tumour-associated antigen BINDING AGENT Ki 10.24 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4039044 VANDF
CHEBI:755272 CHEBI
CHEMBL3301589 ChEMBL_ID
D11525 KEGG_DRUG
C000632577 MESH_SUPPLEMENTAL_RECORD_UI
10738 IUPHAR_LIGAND_ID
DB13007 DRUGBANK_ID
836465002 SNOMEDCT_US
838468009 SNOMEDCT_US
C4519740 UMLSCUI
CHEMBL3301579 ChEMBL_ID
9821 INN_ID
1448664-46-7 SECONDARY_CAS_RN
328359 MMSL
37850 MMSL
37854 MMSL
d09466 MMSL
018235 NDDF
DLE8519RWM UNII
2268093 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PADCEVEJFV HUMAN PRESCRIPTION DRUG LABEL 1 51144-020 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS BLA 30 sections
PADCEVEJFV HUMAN PRESCRIPTION DRUG LABEL 1 51144-030 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 mg INTRAVENOUS BLA 30 sections