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

DoseUnitRoute
6 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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 541.04 28.20 280 8885 158069 90461213
Neuropathy peripheral 432.65 28.20 230 8935 136740 90482542
Neutropenia 268.09 28.20 204 8961 224700 90394582
Off label use 244.46 28.20 413 8752 1101839 89517443
Myelosuppression 200.36 28.20 101 9064 53490 90565792
Polyneuropathy 193.46 28.20 73 9092 19268 90600014
Peripheral sensory neuropathy 122.63 28.20 43 9122 9207 90610075
Neutrophil count decreased 105.55 28.20 74 9091 71458 90547824
Thrombocytopenia 104.98 28.20 117 9048 208608 90410674
Pneumocystis jirovecii pneumonia 102.58 28.20 48 9117 21568 90597714
Pyrexia 101.99 28.20 213 8952 660272 89959010
Disease progression 93.18 28.20 96 9069 156519 90462763
White blood cell count decreased 89.75 28.20 97 9068 167012 90452270
Pancytopenia 70.19 28.20 73 9092 120190 90499092
Febrile bone marrow aplasia 66.76 28.20 28 9137 9710 90609572
Mucosal inflammation 65.57 28.20 51 9114 57574 90561708
Anaemia 64.09 28.20 122 9043 352680 90266602
Weight decreased 60.12 28.20 124 9041 379786 90239496
Cytopenia 56.81 28.20 30 9135 17419 90601863
Pneumonitis 56.67 28.20 42 9123 44128 90575154
Peripheral sensorimotor neuropathy 53.80 28.20 16 9149 2029 90617253
Ileus 52.60 28.20 28 9137 16518 90602764
Malignant neoplasm progression 50.38 28.20 58 9107 106812 90512470
Ectropion 49.64 28.20 10 9155 245 90619037
Neurotoxicity 48.38 28.20 29 9136 21438 90597844
Sepsis 46.81 28.20 73 9092 179741 90439541
Cytomegalovirus colitis 45.87 28.20 16 9149 3370 90615912
Neoplasm progression 45.52 28.20 37 9128 44449 90574833
Acute polyneuropathy 43.74 28.20 10 9155 451 90618831
Gamma-glutamyltransferase abnormal 42.03 28.20 10 9155 537 90618745
Peripheral motor neuropathy 41.51 28.20 13 9152 1960 90617322
Dermatitis exfoliative generalised 41.43 28.20 17 9148 5576 90613706
Headache 41.10 28.20 18 9147 862728 89756554
Procalcitonin abnormal 40.88 28.20 6 9159 18 90619264
Anaplastic large cell lymphoma T- and null-cell types recurrent 40.40 28.20 6 9159 20 90619262
Progressive multifocal leukoencephalopathy 40.16 28.20 23 9142 15632 90603650
Rash scarlatiniform 39.33 28.20 8 9157 206 90619076
Platelet count decreased 39.02 28.20 58 9107 136911 90482371
Bicytopenia 36.84 28.20 14 9151 3757 90615525
Blood lactate dehydrogenase increased 36.30 28.20 26 9139 25906 90593376
Tumour lysis syndrome 35.81 28.20 19 9146 11133 90608149
Lymphocyte count decreased 35.54 28.20 29 9136 35021 90584261
Pain 34.69 28.20 30 9135 996311 89622971
Guillain-Barre syndrome 34.10 28.20 14 9151 4598 90614684
Hepatitis G 32.76 28.20 6 9159 87 90619195
Lymphadenopathy 32.62 28.20 31 9134 45744 90573538
Meningitis aseptic 31.99 28.20 15 9150 6758 90612524
Hyperthermia 31.47 28.20 17 9148 10318 90608964
Chronic inflammatory demyelinating polyradiculoneuropathy 31.09 28.20 9 9156 1038 90618244
Drug hypersensitivity 30.79 28.20 5 9160 463604 90155678
Leukopenia 30.63 28.20 44 9121 100666 90518616
Blood uric acid increased 30.16 28.20 15 9150 7689 90611593
Cardiac failure 29.23 28.20 45 9120 109451 90509831
Swelling 29.02 28.20 4 9161 419054 90200228
Blood lactate dehydrogenase abnormal 28.36 28.20 7 9158 439 90618843

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
Off label use 314.45 21.49 611 11660 637724 41971340
Febrile neutropenia 273.40 21.49 300 11971 185403 42423661
Neuropathy peripheral 240.06 21.49 213 12058 101640 42507424
Myelosuppression 167.34 21.49 118 12153 40343 42568721
Polyneuropathy 160.90 21.49 87 12184 18574 42590490
Neutropenia 131.32 21.49 218 12053 199213 42409851
Cytomegalovirus chorioretinitis 129.24 21.49 49 12222 4562 42604502
Disease progression 122.45 21.49 177 12094 143479 42465585
Pyrexia 103.67 21.49 297 11974 393745 42215319
Peripheral sensory neuropathy 93.07 21.49 47 12224 8715 42600349
Thrombocytopenia 87.16 21.49 178 12093 190101 42418963
Neutrophil count decreased 76.89 21.49 93 12178 63322 42545742
Second primary malignancy 72.50 21.49 41 12230 9534 42599530
Malignant neoplasm progression 70.45 21.49 118 12153 108282 42500782
Pneumocystis jirovecii pneumonia 61.77 21.49 54 12217 25127 42583937
Acute myeloid leukaemia 61.28 21.49 51 12220 22205 42586859
Endocarditis noninfective 60.09 21.49 13 12258 151 42608913
Neoplasm progression 59.02 21.49 56 12215 28944 42580120
Pneumonitis 56.88 21.49 65 12206 41653 42567411
Peripheral motor neuropathy 56.09 21.49 22 12249 2242 42606822
Peripheral sensorimotor neuropathy 51.96 21.49 20 12251 1938 42607126
Myositis 49.30 21.49 38 12233 14828 42594236
Blindness 47.02 21.49 40 12231 17938 42591126
White blood cell count decreased 40.97 21.49 95 12176 110301 42498763
Hepatitis viral 39.21 21.49 13 12258 816 42608248
Anaplastic large-cell lymphoma 37.98 21.49 8 12263 81 42608983
Blood lactate dehydrogenase increased 36.15 21.49 41 12230 26040 42583024
Drug interaction 35.91 21.49 16 12255 266983 42342081
Haematopoietic stem cell mobilisation 35.75 21.49 10 12261 352 42608712
Peripheral T-cell lymphoma unspecified 34.76 21.49 11 12260 595 42608469
Cutaneous T-cell lymphoma 34.50 21.49 15 12256 1983 42607081
Guillain-Barre syndrome 34.26 21.49 23 12248 7240 42601824
Beta 2 microglobulin increased 34.14 21.49 10 12261 416 42608648
Hyperglycaemia 33.93 21.49 53 12218 45806 42563258
Therapy partial responder 33.93 21.49 35 12236 19986 42589078
Cytomegalovirus infection 33.73 21.49 44 12227 32262 42576802
Peripheral blood stem cell apheresis 33.51 21.49 8 12263 148 42608916
Leukopenia 33.01 21.49 69 12202 74677 42534387
Septic shock 31.94 21.49 77 12194 91595 42517469
Lymphoma 31.72 21.49 29 12242 14292 42594772
Molluscum contagiosum 31.36 21.49 9 12262 348 42608716
Anaemia 31.17 21.49 161 12110 280117 42328947
Dizziness 30.40 21.49 17 12254 249237 42359827
Sepsis 29.88 21.49 125 12146 199209 42409855
Febrile bone marrow aplasia 29.41 21.49 24 12247 10157 42598907
Anaplastic large cell lymphoma T- and null-cell types recurrent 28.92 21.49 6 12265 56 42609008
Type IV hypersensitivity reaction 28.62 21.49 14 12257 2423 42606641
Anaplastic large cell lymphoma T- and null-cell types refractory 28.61 21.49 4 12267 0 42609064
Product use in unapproved indication 27.90 21.49 116 12155 184340 42424724
T-cell lymphoma stage IV 27.63 21.49 7 12264 167 42608897
Gamma-glutamyltransferase increased 27.51 21.49 40 12231 32457 42576607
Pain 26.69 21.49 19 12252 244829 42364235
Cancer fatigue 26.49 21.49 7 12264 198 42608866
Cutaneous T-cell lymphoma refractory 25.91 21.49 5 12266 31 42609033
Ileal perforation 25.10 21.49 10 12261 1061 42608003
Apoptotic colonopathy 24.98 21.49 6 12265 114 42608950
Visual acuity reduced transiently 24.41 21.49 6 12265 126 42608938
Peripheral T-cell lymphoma unspecified recurrent 24.27 21.49 5 12266 45 42609019
Demyelinating polyneuropathy 24.21 21.49 11 12260 1613 42607451
Pulmonary toxicity 24.16 21.49 20 12251 8635 42600429
Colitis 24.16 21.49 46 12225 46526 42562538
Haemoglobin abnormal 24.09 21.49 16 12255 4948 42604116
Neutropenic sepsis 23.69 21.49 26 12245 15920 42593144
Haemophagocytic lymphohistiocytosis 22.50 21.49 27 12244 18195 42590869
Adenocarcinoma gastric 22.40 21.49 10 12261 1408 42607656
Depression 21.99 21.49 3 12268 111360 42497704
Vasogenic cerebral oedema 21.96 21.49 9 12262 1027 42608037
Dermatitis exfoliative generalised 21.78 21.49 16 12255 5808 42603256
Cytopenia 21.73 21.49 26 12245 17471 42591593
Blood albumin abnormal 21.58 21.49 7 12264 410 42608654

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 655.16 22.34 500 19075 316267 110253457
Neuropathy peripheral 556.20 22.34 363 19212 178914 110390810
Off label use 467.14 22.34 894 18681 1499291 109070433
Myelosuppression 354.67 22.34 216 19359 94124 110475600
Neutropenia 336.51 22.34 371 19204 374249 110195475
Polyneuropathy 280.22 22.34 129 19446 31883 110537841
Disease progression 254.71 22.34 262 19313 243772 110325952
Neutrophil count decreased 198.01 22.34 167 19408 120774 110448950
Thrombocytopenia 195.66 22.34 273 19302 348612 110221112
Pyrexia 186.79 22.34 457 19118 897808 109671916
Peripheral sensory neuropathy 180.47 22.34 78 19497 16602 110553122
Pneumocystis jirovecii pneumonia 179.01 22.34 105 19470 42630 110527094
Malignant neoplasm progression 136.09 22.34 161 19414 174406 110395318
Cytomegalovirus chorioretinitis 131.63 22.34 49 19526 7079 110562645
White blood cell count decreased 124.68 22.34 177 19398 229213 110340511
Anaemia 111.80 22.34 277 19298 546809 110022915
Peripheral sensorimotor neuropathy 106.68 22.34 36 19539 3907 110565817
Febrile bone marrow aplasia 97.93 22.34 52 19523 17413 110552311
Neoplasm progression 95.09 22.34 84 19491 64511 110505213
Pneumonitis 92.24 22.34 89 19486 76442 110493282
Second primary malignancy 82.56 22.34 47 19528 18021 110551703
Sepsis 82.36 22.34 180 19395 327166 110242558
Mucosal inflammation 82.11 22.34 93 19482 96048 110473676
Acute myeloid leukaemia 69.33 22.34 56 19519 38054 110531670
Pancytopenia 69.07 22.34 129 19446 209484 110360240
Pain 68.97 22.34 42 19533 954913 109614811
Joint swelling 65.74 22.34 3 19572 442842 110126882
Blood lactate dehydrogenase increased 63.93 22.34 57 19518 44277 110525447
Septic shock 63.59 22.34 106 19469 157422 110412302
Dermatitis exfoliative generalised 62.45 22.34 33 19542 10939 110558785
Cytomegalovirus infection 59.43 22.34 60 19515 54384 110515340
Endocarditis noninfective 58.35 22.34 13 19562 292 110569432
Guillain-Barre syndrome 57.45 22.34 31 19544 10713 110559011
Headache 56.77 22.34 44 19531 882333 109687391
Drug hypersensitivity 56.43 22.34 7 19568 454083 110115641
Cytopenia 56.36 22.34 45 19530 30071 110539653
Platelet count decreased 55.96 22.34 125 19450 230318 110339406
Weight decreased 55.95 22.34 196 19379 467861 110101863
Progressive multifocal leukoencephalopathy 54.80 22.34 41 19534 24915 110544809
Arthralgia 53.89 22.34 36 19539 779596 109790128
Peripheral motor neuropathy 53.87 22.34 22 19553 4064 110565660
Hyperthermia 53.64 22.34 38 19537 21234 110548490
Tumour lysis syndrome 53.37 22.34 44 19531 30757 110538967
Peripheral swelling 53.33 22.34 5 19570 404029 110165695
Nasopharyngitis 51.73 22.34 5 19570 394356 110175368
Therapy partial responder 50.19 22.34 46 19529 37015 110532709
Leukopenia 49.52 22.34 92 19483 148699 110421025
Blindness 48.99 22.34 45 19530 36314 110533410
Peripheral T-cell lymphoma unspecified 48.97 22.34 14 19561 877 110568847
Lymphocyte count decreased 48.22 22.34 55 19520 57188 110512536
Dizziness 47.22 22.34 33 19542 698160 109871564
Hypertension 46.74 22.34 16 19559 510068 110059656
Acute polyneuropathy 46.43 22.34 13 19562 755 110568969
Bicytopenia 46.31 22.34 23 19552 6701 110563023
Lymphoma 46.22 22.34 34 19541 20137 110549587
Neutropenic sepsis 45.26 22.34 40 19535 30706 110539018
Myositis 44.85 22.34 40 19535 31076 110538648
Swelling 44.62 22.34 5 19570 351036 110218688
Drug interaction 43.61 22.34 17 19558 500166 110069558
Alanine aminotransferase increased 42.72 22.34 98 19477 183675 110386049
Venoocclusive disease 41.61 22.34 21 19554 6329 110563395
Ileus 41.34 22.34 38 19537 30691 110539033
Abdominal discomfort 40.39 22.34 10 19565 393848 110175876
Chronic inflammatory demyelinating polyradiculoneuropathy 40.20 22.34 15 19560 2180 110567544
Anaplastic large-cell lymphoma 39.83 22.34 9 19566 216 110569508
Cancer fatigue 39.68 22.34 10 19565 386 110569338
Colitis 38.82 22.34 67 19508 102256 110467468
Haematopoietic stem cell mobilisation 38.79 22.34 10 19565 423 110569301
Hepatitis viral 38.07 22.34 13 19562 1462 110568262
Neurotoxicity 38.02 22.34 42 19533 42165 110527559
Multiple organ dysfunction syndrome 37.60 22.34 83 19492 151627 110418097
Peripheral blood stem cell apheresis 37.23 22.34 8 19567 151 110569573
Lymphadenopathy 37.20 22.34 51 19524 63784 110505940
Cutaneous T-cell lymphoma 37.17 22.34 16 19559 3368 110566356
Graft versus host disease 37.12 22.34 29 19546 18777 110550947
Ectropion 36.79 22.34 10 19565 520 110569204
Hyperglycaemia 36.67 22.34 59 19516 85031 110484693
Gamma-glutamyltransferase increased 35.76 22.34 49 19526 61260 110508464
Haemophagocytic lymphohistiocytosis 34.84 22.34 35 19540 31524 110538200
Depression 34.66 22.34 7 19568 317328 110252396
Beta 2 microglobulin increased 34.02 22.34 10 19565 691 110569033
Anxiety 33.05 22.34 10 19565 345068 110224656
Blood pressure increased 32.03 22.34 4 19571 258369 110311355
Ileus paralytic 32.01 22.34 22 19553 11715 110558009
Hypoalbuminaemia 31.74 22.34 32 19543 28942 110540782
Cytomegalovirus colitis 31.27 22.34 18 19557 7043 110562681
Anaplastic large cell lymphoma T- and null-cell types recurrent 31.20 22.34 6 19569 63 110569661
T-cell lymphoma stage IV 30.66 22.34 7 19568 176 110569548
Molluscum contagiosum 30.60 22.34 9 19566 623 110569101
Anaplastic large cell lymphoma T- and null-cell types refractory 30.56 22.34 4 19571 0 110569724
Rash scarlatiniform 30.55 22.34 8 19567 360 110569364
Bone marrow failure 30.42 22.34 44 19531 57804 110511920
Anaphylactic shock 29.76 22.34 41 19534 51505 110518219
Apoptotic colonopathy 29.74 22.34 7 19568 202 110569522
Aspartate aminotransferase increased 29.43 22.34 78 19497 159858 110409866
Chills 29.23 22.34 87 19488 190493 110379231
Pain in extremity 29.15 22.34 26 19549 487092 110082632
Asthma 28.44 22.34 5 19570 250286 110319438
Product use in unapproved indication 28.43 22.34 155 19420 447222 110122502
Haematotoxicity 28.22 22.34 26 19549 21056 110548668
Meningitis aseptic 28.10 22.34 19 19556 9851 110559873
Hepatitis G 28.09 22.34 6 19569 110 110569614
Contusion 28.00 22.34 4 19571 233357 110336367
Discomfort 27.42 22.34 3 19572 214704 110355020
Lower respiratory tract infection 27.31 22.34 5 19570 243101 110326623
Respiratory failure 27.26 22.34 92 19483 215240 110354484
Ileal perforation 27.23 22.34 10 19565 1390 110568334
Hypogonadism 27.19 22.34 11 19564 1983 110567741
Wheezing 27.10 22.34 6 19569 255224 110314500
Muscle spasms 26.74 22.34 8 19567 278149 110291575
Post transplant lymphoproliferative disorder 26.41 22.34 22 19553 15591 110554133
Product dose omission issue 26.32 22.34 12 19563 321770 110247954
Pulmonary toxicity 25.94 22.34 23 19552 17723 110552001
Peripheral T-cell lymphoma unspecified recurrent 25.78 22.34 5 19570 55 110569669
Pericarditis 25.73 22.34 4 19571 219110 110350614
Type IV hypersensitivity reaction 25.71 22.34 15 19560 6018 110563706
Axonal and demyelinating polyneuropathy 25.31 22.34 5 19570 61 110569663
Neoplasm recurrence 24.95 22.34 14 19561 5218 110564506
Somnolence 24.47 22.34 11 19564 297438 110272286
Electrocardiogram high voltage 24.12 22.34 4 19571 16 110569708
Meningoencephalitis amoebic 23.65 22.34 6 19569 238 110569486
Adenocarcinoma gastric 23.39 22.34 10 19565 2069 110567655
Acute respiratory distress syndrome 23.07 22.34 37 19538 53161 110516563
Cutaneous T-cell lymphoma recurrent 23.04 22.34 5 19570 99 110569625
Drug intolerance 22.78 22.34 23 19552 406489 110163235
Demyelinating polyneuropathy 22.64 22.34 10 19565 2239 110567485
Blood cholesterol increased 22.56 22.34 3 19572 184782 110384942

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 D000074322 Antineoplastic Agents, Immunological
MeSH PA D000922 Immunotoxins
MeSH PA D000970 Antineoplastic Agents
MeSH PA D007155 Immunologic Factors
FDA MoA N0000182966 CD30-directed Antibody Interactions
FDA EPC N0000182967 CD30-directed Immunoconjugate
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

L01FX Other monoclonal antibodies and antibody drug conjugates 29 drugs

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
CHEBI:750074 CHEBI
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 34 sections
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 34 sections