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

Stem definitionDrug idCAS RN
synthetic derivatives of dolastatin series 4964 914088-09-8

Description:

MoleculeDescription

Synonyms:

  • brentuximab vedotin
  • adcetris
  • SGN-35
  • cAC10-vcMMAE
  • brentuximab vedotin (genetical recombination)
a CD30-directed antibody-drug conjugate consisting of three components: the chimeric IgG1 antibody cAC10, specific for human CD30, the microtubule disrupting agent MMAE, and a protease-cleavable linker that covalently attaches MMAE to cAC10
  • Molecular weight:
  • Formula: Brentuximab(C68H106N11O15S)3-5
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Oct. 25, 2012 EMA Takeda Pharma A/S
Aug. 19, 2011 FDA SEATTLE GENETICS
Jan. 17, 2014 PMDA Takeda Pharmaceutical Company Limited

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
Febrile neutropenia 255.64 27.29 149 5593 118300 63364980
Neuropathy peripheral 234.73 27.29 139 5603 113528 63369752
Off label use 152.60 27.29 240 5502 674222 62809058
Neutropenia 150.20 27.29 125 5617 174880 63308400
Disease progression 99.60 27.29 85 5657 122673 63360607
Pneumocystis jirovecii pneumonia 95.49 27.29 41 5701 16873 63466407
Polyneuropathy 87.78 27.29 37 5705 14552 63468728
Thrombocytopenia 82.61 27.29 84 5658 151073 63332207
Pyrexia 71.33 27.29 141 5601 470337 63012943
Neutrophil count decreased 53.89 27.29 43 5699 56363 63426917
Ileus 52.65 27.29 26 5716 14699 63468581
Peripheral sensory neuropathy 48.52 27.29 20 5722 7431 63475849
Myelosuppression 46.15 27.29 28 5714 23675 63459605
Pancytopenia 44.23 27.29 49 5693 96884 63386396
Pneumonitis 42.79 27.29 31 5711 35191 63448089
Malignant neoplasm progression 41.82 27.29 44 5698 82077 63401203
Procalcitonin abnormal 41.55 27.29 6 5736 18 63483262
Peripheral motor neuropathy 40.59 27.29 12 5730 1669 63481611
Tumour lysis syndrome 38.59 27.29 18 5724 8972 63474308
Sepsis 37.66 27.29 57 5685 153066 63330214
Cytopenia 37.11 27.29 19 5723 11582 63471698
Blood uric acid increased 36.97 27.29 15 5727 5352 63477928
Mucosal inflammation 36.96 27.29 32 5710 46896 63436384
Gamma-glutamyltransferase abnormal 36.55 27.29 8 5734 331 63482949
Cytomegalovirus colitis 36.52 27.29 12 5730 2360 63480920
White blood cell count decreased 33.09 27.29 51 5691 139053 63344227
Weight decreased 32.55 27.29 75 5667 276723 63206557
Blood lactate dehydrogenase abnormal 30.35 27.29 7 5735 368 63482912
Neurotoxicity 30.35 27.29 19 5723 16971 63466309
Tumour flare 30.11 27.29 7 5735 381 63482899
Ectropion 29.28 27.29 6 5736 180 63483100
Anaemia 28.62 27.29 74 5668 293356 63189924
Headache 28.31 27.29 11 5731 633230 62850050
Chronic inflammatory demyelinating polyradiculoneuropathy 27.93 27.29 7 5735 524 63482756
Serum ferritin abnormal 27.73 27.29 6 5736 235 63483045
Dermatitis exfoliative generalised 27.46 27.29 11 5731 3796 63479484

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 177.18 21.65 148 7749 83115 34865919
Off label use 173.71 21.65 325 7572 419199 34529835
Febrile neutropenia 145.09 21.65 166 7731 136683 34812351
Cytomegalovirus chorioretinitis 109.10 21.65 38 7859 3551 34945483
Disease progression 102.56 21.65 124 7773 107953 34841081
Polyneuropathy 96.63 21.65 53 7844 14843 34934191
Neutropenia 88.54 21.65 140 7757 156638 34792396
Pneumocystis jirovecii pneumonia 73.10 21.65 49 7848 19661 34929373
Pyrexia 68.83 21.65 197 7700 332816 34616218
Endocarditis noninfective 65.29 21.65 13 7884 127 34948907
Peripheral sensory neuropathy 60.91 21.65 30 7867 6730 34942304
Neutrophil count decreased 55.62 21.65 63 7834 51041 34897993
Acute myeloid leukaemia 55.06 21.65 40 7857 18230 34930804
Therapy partial responder 50.98 21.65 30 7867 9586 34939448
Malignant neoplasm progression 47.32 21.65 77 7820 87969 34861065
Myositis 47.14 21.65 31 7866 12039 34936995
Thrombocytopenia 46.18 21.65 106 7791 156141 34792893
Guillain-Barre syndrome 46.04 21.65 24 7873 6063 34942971
Cutaneous T-cell lymphoma 45.64 21.65 16 7881 1522 34947512
Blindness 43.32 21.65 32 7865 14954 34934080
Peripheral motor neuropathy 42.96 21.65 16 7881 1810 34947224
Cytomegalovirus infection 42.51 21.65 40 7857 26095 34922939
Molluscum contagiosum 40.28 21.65 10 7887 282 34948752
Anaplastic large-cell lymphoma 39.65 21.65 8 7889 84 34948950
Type IV hypersensitivity reaction 39.06 21.65 14 7883 1420 34947614
Myelosuppression 36.24 21.65 32 7865 19233 34929801
Cancer fatigue 34.23 21.65 7 7890 79 34948955
Sepsis 33.67 21.65 98 7799 166463 34782571
Pneumonitis 30.61 21.65 38 7859 33840 34915194
Second primary malignancy 30.17 21.65 20 7877 7866 34941168
Hepatitis viral 29.01 21.65 9 7888 584 34948450
Septic shock 28.46 21.65 55 7842 71779 34877255
Peripheral sensorimotor neuropathy 27.06 21.65 11 7886 1571 34947463
Product use in unapproved indication 26.52 21.65 72 7825 117427 34831607
Neutropenic sepsis 26.16 21.65 23 7874 13744 34935290
Tumour lysis syndrome 25.63 21.65 25 7872 17034 34932000
Peripheral T-cell lymphoma unspecified recurrent 25.48 21.65 5 7892 45 34948989
Gamma-glutamyltransferase abnormal 24.85 21.65 7 7890 324 34948710
Drug interaction 24.85 21.65 10 7887 225936 34723098
Hypogonadism 23.31 21.65 11 7886 2244 34946790
Adenocarcinoma gastric 22.56 21.65 9 7888 1224 34947810
Febrile bone marrow aplasia 22.53 21.65 17 7880 8192 34940842
Demyelinating polyneuropathy 22.44 21.65 9 7888 1242 34947792
Blood alkaline phosphatase abnormal 22.20 21.65 7 7890 479 34948555
Anaplastic large cell lymphoma T- and null-cell types refractory 22.19 21.65 3 7894 0 34949034
Pancytopenia 22.16 21.65 59 7838 95098 34853936
Visual acuity reduced transiently 21.78 21.65 5 7892 100 34948934

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
Febrile neutropenia 328.24 20.98 276 11963 230723 79501426
Neuropathy peripheral 327.11 20.98 226 12013 141079 79591070
Off label use 238.15 20.98 464 11775 906751 78825398
Disease progression 214.75 20.98 197 12042 184165 79547984
Neutropenia 205.23 20.98 236 12003 287474 79444675
Pneumocystis jirovecii pneumonia 158.42 20.98 84 12155 32424 79699725
Polyneuropathy 127.91 20.98 66 12173 24085 79708064
Neutrophil count decreased 124.24 20.98 108 12131 93851 79638298
Thrombocytopenia 115.82 20.98 171 12068 265088 79467061
Pyrexia 115.66 20.98 293 11946 678416 79053733
Peripheral sensory neuropathy 106.63 20.98 48 12191 12985 79719164
Cytomegalovirus chorioretinitis 103.84 20.98 37 12202 5453 79726696
Malignant neoplasm progression 89.06 20.98 107 12132 135883 79596266
Myelosuppression 84.93 20.98 61 12178 40235 79691914
Sepsis 70.05 20.98 138 12101 269290 79462859
Cytomegalovirus infection 68.72 20.98 55 12184 42589 79689560
Endocarditis noninfective 63.80 20.98 13 12226 218 79731931
Guillain-Barre syndrome 57.77 20.98 28 12211 8937 79723212
Tumour lysis syndrome 56.85 20.98 39 12200 23900 79708249
Acute myeloid leukaemia 56.62 20.98 43 12196 30842 79701307
Pancytopenia 53.19 20.98 93 12146 165652 79566497
Cancer fatigue 49.17 20.98 10 12229 166 79731983
Pneumonitis 48.42 20.98 53 12186 60807 79671342
Therapy partial responder 47.71 20.98 31 12208 17366 79714783
Pain 45.27 20.98 26 12213 703776 79028373
Myositis 44.98 20.98 31 12208 19137 79713012
White blood cell count decreased 43.60 20.98 92 12147 188196 79543953
Peripheral motor neuropathy 42.92 20.98 17 12222 3350 79728799
Chronic inflammatory demyelinating polyradiculoneuropathy 42.69 20.98 13 12226 1172 79730977
Septic shock 42.13 20.98 71 12168 122730 79609419
Hyperthermia 41.92 20.98 29 12210 18008 79714141
Graft versus host disease 41.76 20.98 27 12212 14999 79717150
Anaemia 41.46 20.98 156 12083 444859 79287290
Peripheral sensorimotor neuropathy 41.19 20.98 16 12223 2994 79729155
Anaplastic large-cell lymphoma 40.68 20.98 9 12230 227 79731922
Headache 39.46 20.98 26 12213 653746 79078403
Cutaneous T-cell lymphoma 39.24 20.98 15 12224 2688 79729461
Mucosal inflammation 39.19 20.98 53 12186 75527 79656622
Molluscum contagiosum 39.00 20.98 10 12229 479 79731670
Blood lactate dehydrogenase increased 38.12 20.98 38 12201 39132 79693017
Ileus 36.36 20.98 31 12208 26180 79705969
Ileus paralytic 36.24 20.98 21 12218 9599 79722550
Drug interaction 35.32 20.98 10 12229 415173 79316976
Febrile bone marrow aplasia 35.21 20.98 23 12216 12997 79719152
Neutropenic sepsis 33.50 20.98 30 12209 27034 79705115
Joint swelling 33.29 20.98 3 12236 288643 79443506
Type IV hypersensitivity reaction 33.27 20.98 15 12224 4066 79728083
Arthralgia 32.81 20.98 24 12215 571779 79160370
Drug hypersensitivity 32.19 20.98 4 12235 298912 79433237
Product use in unapproved indication 31.39 20.98 97 12142 250262 79481887
Second primary malignancy 30.85 20.98 22 12217 14328 79717821
Peripheral swelling 30.57 20.98 3 12236 269614 79462535
Multiple organ dysfunction syndrome 30.46 20.98 61 12178 120185 79611964
General physical health deterioration 30.31 20.98 102 12137 275136 79457013
Hypogonadism 30.05 20.98 11 12228 1749 79730400
Neoplasm progression 29.50 20.98 38 12201 51644 79680505
Lymphoma 29.14 20.98 23 12216 17437 79714712
Dizziness 29.04 20.98 23 12216 526418 79205731
Venoocclusive disease 28.61 20.98 14 12225 4559 79727590
Blindness 28.48 20.98 28 12211 28355 79703794
Cytomegalovirus colitis 28.29 20.98 14 12225 4671 79727478
Peripheral T-cell lymphoma unspecified recurrent 27.31 20.98 5 12234 46 79732103
Hepatitis viral 27.30 20.98 9 12230 1049 79731100
Acute respiratory distress syndrome 26.10 20.98 33 12206 44034 79688115
Cytopenia 26.03 20.98 23 12216 20360 79711789
Platelet count decreased 25.87 20.98 77 12162 194587 79537562
Bicytopenia 25.40 20.98 13 12226 4657 79727492
Dermatitis exfoliative generalised 25.16 20.98 15 12224 7226 79724923
Haemophagocytic lymphohistiocytosis 24.67 20.98 23 12216 21814 79710335
Hypertension 24.62 20.98 10 12229 330982 79401167
Nasopharyngitis 23.75 20.98 5 12234 253876 79478273
Anaplastic large cell lymphoma T- and null-cell types refractory 23.35 20.98 3 12236 0 79732149
Abdominal discomfort 23.32 20.98 5 12234 250722 79481427
Hyperglycaemia 23.22 20.98 40 12199 70295 79661854
Blood uric acid increased 23.16 20.98 18 12221 13342 79718807
Anaphylactic shock 22.99 20.98 28 12211 35968 79696181
Adenocarcinoma gastric 22.82 20.98 9 12230 1752 79730397
Leukopenia 22.52 20.98 53 12186 116460 79615689
Peripheral T-cell lymphoma unspecified 22.45 20.98 7 12232 683 79731466
Stem cell transplant 22.16 20.98 11 12228 3693 79728456
Aplasia 21.60 20.98 14 12225 7806 79724343
Ectropion 21.16 20.98 6 12233 422 79731727

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FX05 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates
FDA CS M0028142 Immunoconjugates
FDA PE N0000175085 Microtubule Inhibition
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D018796 Immunoconjugates
MeSH PA D007155 Immunologic Factors
MeSH PA D000922 Immunotoxins
MeSH PA D009676 Noxae
FDA MoA N0000182966 CD30-directed Antibody Interactions
FDA EPC N0000182967 CD30-directed Immunoconjugate

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

DiseaseRelationSNOMED_IDDOID
CD30-positive peripheral T-cell lymphoma indication 109977009
Hodgkin's disease indication 118599009
Cutaneous Tcell lymphoma indication 400122007
Anaplastic large T-cell systemic malignant lymphoma indication 404134006




🐶 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
Tumor necrosis factor receptor superfamily member 8 Membrane receptor BINDING AGENT DRUG LABEL DRUG LABEL
Tubulin beta Tumour-associated antigen INHIBITOR DRUG LABEL DRUG LABEL

External reference:

IDSource
D09587 KEGG_DRUG
4031047 VUID
N0000183555 NUI
4031047 VANDF
CHEMBL1742994 ChEMBL_ID
6772 IUPHAR_LIGAND_ID
DB08870 DRUGBANK_ID
1147320 RXNORM
185268 MMSL
28063 MMSL
d07799 MMSL
013904 NDDF
713395006 SNOMEDCT_US
714671006 SNOMEDCT_US
C2973446 UMLSCUI
D000079963 MESH_DESCRIPTOR_UI
9144 INN_ID
117723179 PUBCHEM_CID
7XL5ISS668 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 27 sections
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 27 sections
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 27 sections
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 27 sections