brentuximab vedotin 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
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
Aug. 19, 2011 FDA SEATTLE GENETICS

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 169.04 27.56 106 4177 94521 46587258
Off label use 164.79 27.56 187 4096 379654 46302125
Neuropathy peripheral 152.77 27.56 98 4185 90795 46590984
Neutropenia 108.88 27.56 96 4187 143108 46538671
Anaplastic large-cell lymphoma 100.15 27.56 16 4267 107 46681672
Pyrexia 68.86 27.56 118 4165 348684 46333095
Pneumocystis jirovecii pneumonia 63.46 27.56 30 4253 15218 46666561
Disease progression 60.96 27.56 57 4226 91243 46590536
Polyneuropathy 58.14 27.56 26 4257 11618 46670161
Peripheral T-cell lymphoma unspecified 45.19 27.56 9 4274 230 46681549
Malignant neoplasm progression 44.19 27.56 41 4242 64885 46616894
Thrombocytopenia 43.95 27.56 56 4227 126525 46555254
Mucosal inflammation 39.62 27.56 31 4252 38945 46642834
Ileus 38.92 27.56 21 4262 14043 46667736
Cutaneous T-cell lymphoma 38.39 27.56 11 4272 1352 46680427
Weight decreased 38.39 27.56 69 4214 210780 46470999
Neutrophil count decreased 36.67 27.56 31 4252 43395 46638384
Cytomegalovirus colitis 35.77 27.56 11 4272 1724 46680055
Pancytopenia 33.30 27.56 40 4243 85018 46596761
Chronic inflammatory demyelinating polyradiculoneuropathy 30.79 27.56 7 4276 340 46681439
Ectropion 29.53 27.56 6 4277 170 46681609
Neurotoxicity 28.55 27.56 17 4266 13700 46668079
Sepsis 27.95 27.56 47 4236 135967 46545812

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 212.00 22.20 254 5764 249036 29697424
Anaplastic large-cell lymphoma 150.54 22.20 27 5991 161 29946299
Neuropathy peripheral 122.25 22.20 106 5912 70369 29876091
Cytomegalovirus chorioretinitis 116.99 22.20 38 5980 3230 29943230
Febrile neutropenia 112.43 22.20 122 5896 106571 29839889
Disease progression 81.69 22.20 90 5928 79784 29866676
Anaplastic large cell lymphoma T- and null-cell types 80.57 22.20 15 6003 113 29946347
Cutaneous T-cell lymphoma 79.69 22.20 23 5995 1312 29945148
Peripheral T-cell lymphoma unspecified 74.58 22.20 18 6000 509 29945951
Neutropenia 68.62 22.20 105 5913 128435 29818025
Endocarditis noninfective 68.38 22.20 13 6005 111 29946349
Blindness 52.47 22.20 32 5986 12277 29934183
Pyrexia 46.60 22.20 147 5871 294342 29652118
Malignant neoplasm progression 42.70 22.20 62 5956 72225 29874235
Molluscum contagiosum 41.87 22.20 10 6008 270 29946190
Myositis 41.74 22.20 26 5992 10351 29936109
Pneumocystis jirovecii pneumonia 40.66 22.20 31 5987 17089 29929371
Product use in unapproved indication 38.93 22.20 60 5958 73633 29872827
Cytomegalovirus infection 37.70 22.20 34 5984 23640 29922820
Guillain-Barre syndrome 37.59 22.20 19 5999 5064 29941396
Polyneuropathy 36.26 22.20 25 5993 11798 29934662
Neutrophil count decreased 33.58 22.20 42 5976 42412 29904048
Peripheral sensory neuropathy 32.17 22.20 18 6000 5883 29940577
Type IV hypersensitivity reaction 31.75 22.20 11 6007 1137 29945323
Hepatitis viral 31.69 22.20 9 6009 484 29945976
Peripheral T-cell lymphoma unspecified recurrent 31.38 22.20 6 6012 53 29946407
Therapy partial responder 30.86 22.20 15 6003 3676 29942784
Acute myeloid leukaemia 28.94 22.20 26 5992 17980 29928480
Sepsis 27.68 22.20 78 5940 146317 29800143
Septic shock 27.09 22.20 47 5971 63560 29882900
Cancer fatigue 27.05 22.20 5 6013 36 29946424
Pneumonitis 26.37 22.20 30 5988 27424 29919036
Visual acuity reduced transiently 26.37 22.20 5 6013 42 29946418
Angioimmunoblastic T-cell lymphoma 24.89 22.20 7 6011 363 29946097
Adenocarcinoma gastric 24.19 22.20 9 6009 1142 29945318
Thrombocytopenia 23.95 22.20 71 5947 136973 29809487
Hyperthermia 23.34 22.20 18 6000 10081 29936379
Second primary malignancy 23.25 22.20 15 6003 6341 29940119
Peripheral sensorimotor neuropathy 23.16 22.20 9 6009 1286 29945174
Drug interaction 22.80 22.20 6 6012 199562 29746898
Cutaneous T-cell lymphoma refractory 22.54 22.20 3 6015 0 29946460
Febrile bone marrow aplasia 22.22 22.20 16 6002 8081 29938379

Pharmacologic Action:

SourceCodeDescription
ATC L01XC12 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Monoclonal antibodies
FDA CS M0028142 Immunoconjugates
FDA PE N0000175085 Microtubule Inhibition
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D000922 Immunotoxins
MeSH PA D009676 Noxae
FDA MoA N0000182966 CD30-directed Antibody Interactions
FDA EPC N0000182967 CD30-directed Immunoconjugate

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hodgkin's disease indication 118599009
Anaplastic large T-cell systemic malignant lymphoma indication 404134006

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 INHIBITOR DRUG LABEL DRUG LABEL
Tumor necrosis factor receptor superfamily member 8 Membrane receptor BINDING AGENT DRUG LABEL DRUG LABEL

External reference:

IDSource
7XL5ISS668 UNII
D09587 KEGG_DRUG
4031047 VUID
N0000183555 NUI
4031047 VANDF
C3192355 UMLSCUI
CHEMBL1742994 ChEMBL_ID
DB08870 DRUGBANK_ID
D000079963 MESH_DESCRIPTOR_UI
9144 INN_ID
6772 IUPHAR_LIGAND_ID
1147320 RXNORM
185268 MMSL
28063 MMSL
d07799 MMSL
013904 NDDF
713395006 SNOMEDCT_US
714671006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ADCETRIS HUMAN PRESCRIPTION DRUG LABEL 1 51144-050 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 26 sections