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

Stem definitionDrug idCAS RN
human origin 5221 1537032-82-8

Description:

MoleculeDescription

Synonyms:

  • avelumab
  • bavencio
  • MSB0010718C
  • MSB0010682
Avelumab is a programmed death ligand-1 (PD-L1) blocking antibody. Avelumab is a human IgG1 lambda monoclonal antibody that has a molecular weight of approximately 147 kDa. PD-L1 may be expressed on tumor cells and tumor-infiltrating immune cells and can contribute to the inhibition of the anti-tumor immune response in the tumor microenvironment. Binding of PD-L1 to the PD-1 and B7.1 receptors found on T cells and antigen presenting cells suppresses cytotoxic T-cell activity, T-cell proliferation and cytokine production. Avelumab binds PD-L1 and blocks the interaction between PD-L1 and its receptors PD-1 and B7.1. This interaction releases the inhibitory effects of PD-L1 on the immune response resulting in the restoration of immune responses, including anti-tumor immune responses. Avelumab has also been shown to induce antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
57.10 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Sept. 18, 2017 EMA Merck Europe B.V.
Sept. 27, 2017 PMDA Merck Serono Co., Ltd.
March 23, 2017 FDA EMD SERONO INC

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
Disease progression 257.10 41.69 97 1448 156518 90470384
Neoplasm progression 85.08 41.69 31 1514 44455 90582447
Death 67.11 41.69 58 1487 456493 90170409
Hypothyroidism 46.05 41.69 21 1524 53106 90573796

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
Disease progression 384.94 30.84 216 4124 143440 42473555
Neoplasm progression 171.16 30.84 75 4265 28925 42588070
Death 131.85 30.84 197 4143 470988 42146007
Infusion related reaction 118.81 30.84 75 4265 60731 42556264
Interstitial lung disease 110.59 30.84 79 4261 78383 42538612
Chills 73.29 30.84 67 4273 93999 42522996
Skin toxicity 62.73 30.84 24 4316 6525 42610470
Hypothyroidism 58.65 30.84 38 4302 32046 42584949
Adrenal insufficiency 54.38 30.84 30 4310 18894 42598101
Myocarditis 54.36 30.84 30 4310 18908 42598087
General physical health deterioration 41.41 30.84 63 4277 151183 42465812
Myositis 41.15 30.84 23 4317 14843 42602152
Lymphoma transformation 37.08 30.84 9 4331 523 42616472
Transaminases increased 37.03 30.84 29 4311 32856 42584139
Dysphonia 36.23 30.84 27 4313 28423 42588572
Neuropathy peripheral 34.55 30.84 47 4293 101806 42515189
Polymyalgia rheumatica 31.49 30.84 11 4329 2312 42614683

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
Disease progression 617.35 32.44 285 5543 243749 110339722
Death 259.88 32.44 245 5583 698624 109884847
Neoplasm progression 249.04 32.44 102 5726 64493 110518978
Interstitial lung disease 146.01 32.44 91 5737 139243 110444228
Hypothyroidism 100.82 32.44 57 5771 72842 110510629
Infusion related reaction 81.15 32.44 100 5728 381062 110202409
Myocarditis 75.02 32.44 35 5793 30020 110553451
Myositis 67.79 32.44 33 5795 31083 110552388
Chills 66.69 32.44 65 5763 190515 110392956
Skin toxicity 64.38 32.44 24 5804 11759 110571712
Adrenal insufficiency 60.89 32.44 34 5794 42356 110541115
Palmar-plantar erythrodysaesthesia syndrome 53.79 32.44 31 5797 40994 110542477
Hepatic function abnormal 48.28 32.44 39 5789 89256 110494215
Neuropathy peripheral 48.01 32.44 53 5775 179224 110404247
Lymphoma transformation 47.54 32.44 10 5818 594 110582877
Immune-mediated hepatitis 45.37 32.44 16 5812 6695 110576776
Myasthenia gravis 44.42 32.44 22 5806 21489 110561982
Pneumonitis 42.59 32.44 34 5794 76497 110506974
Thyroiditis 41.89 32.44 15 5813 6558 110576913
Transaminases increased 41.47 32.44 31 5797 63359 110520112
General physical health deterioration 37.03 32.44 74 5754 425221 110158250
Immune-mediated myositis 35.26 32.44 13 5815 6173 110577298
Tumour hyperprogression 34.28 32.44 7 5821 359 110583112
Haematuria 34.14 32.44 31 5797 82974 110500497
Pyrexia 33.92 32.44 114 5714 898151 109685320
Dysphonia 32.49 32.44 29 5799 75900 110507571

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FF04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
PD-1/PD-L1 (Programmed cell death protein 1/death ligand 1) inhibitors
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D000970 Antineoplastic Agents
FDA CS M0001357 Antibodies, Monoclonal
FDA MoA N0000193336 Programmed Death Ligand-1-directed Antibody Interactions
FDA MoA N0000193337 Programmed Death Ligand-1 Antagonists
FDA EPC N0000193338 Programmed Death Ligand-1 Blocker
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:233423 antifibrotic agent

Related Drugs by ATC class:

L01FF PD-1/PD-L1 (Programmed cell death protein 1/death ligand 1) inhibitors 11 drugs
atezolizumabcemiplimabdostarlimabdurvalumabnivolumabpembrolizumabretifanlimabserplulimabsugemalimabtislelizumabtoripalimab

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

DiseaseRelationSNOMED_IDDOID
Maintenance therapy of unresectable urothelial carcinoma in patients who have received chemotherapy indication 27090000 DOID:2671
Merkel cell carcinoma indication 253001006
Renal cell carcinoma indication 702391001 DOID:4450




🐶 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
Programmed cell death 1 ligand 1 CD molecules ANTIBODY BINDING UNKNOWN DRUG LABEL

External reference:

IDSource
KXG2PJ551I UNII
4036553 VANDF
C4055417 UMLSCUI
CHEBI:755952 CHEBI
CHEMBL3833373 ChEMBL_ID
DB11945 DRUGBANK_ID
D10817 KEGG_DRUG
10062 INN_ID
C000609138 MESH_SUPPLEMENTAL_RECORD_UI
8735 IUPHAR_LIGAND_ID
733055009 SNOMEDCT_US
763506002 SNOMEDCT_US
254791 MMSL
32511 MMSL
d08537 MMSL
017142 NDDF
1875534 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BAVENCIO HUMAN PRESCRIPTION DRUG LABEL 1 44087-3535 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS BLA 30 sections