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

Stem definitionDrug idCAS RN
monoclonal antibodies (human origin); immunomodulator 5690 745013-59-6

Description:

MoleculeDescription

Molfile

Synonyms:

  • tremelimumab
  • tremelimumab-actl
  • CP-675206
  • imjudo
  • tremelimumab (genetical recombination)
CTLA-4 is a negative regulator of T-cell activity. Tremelimumab-actl is a monoclonal antibody that binds to CTLA-4 and blocks the interaction with its ligands CD80 and CD86, releasing CTLA-4-mediated inhibition of T-cell activation. In synergistic mouse tumor models, blocking CTLA-4 activity resulted in decreased tumor growth and increased proliferation of T cells in tumors.
  • 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
Oct. 21, 2022 FDA ASTRAZENECA AB
Feb. 20, 2023 EMA ASTRAZENECA AB
Dec. 23, 2023 PMDA AstraZeneca K.K.

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
Biliary tract infection 234.13 61.28 34 1356 810 90626247
Embolism 104.05 61.28 25 1365 9456 90617601
Urinary tract obstruction 101.08 61.28 19 1371 2230 90624827
Pyrexia 93.04 61.28 78 1312 660407 89966650
Bile duct stenosis 80.07 61.28 15 1375 1727 90625330
Colitis 78.08 61.28 32 1358 69910 90557147
Small intestinal obstruction 71.18 61.28 22 1368 21212 90605845
Cholangitis infective 69.80 61.28 11 1379 454 90626603
Immune-mediated enterocolitis 65.04 61.28 15 1375 4742 90622315
Bacillus infection 61.85 61.28 11 1379 948 90626109

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
Immune-mediated hepatitis 170.35 41.10 41 2667 3733 42614894
Immune-mediated enterocolitis 130.31 41.10 36 2672 5641 42612986
Colitis 124.13 41.10 60 2648 46512 42572115
Pneumonitis 118.01 41.10 56 2652 41662 42576965
Biliary tract infection 111.20 41.10 22 2686 796 42617831
Enterocolitis infectious 102.22 41.10 24 2684 1959 42616668
Immune-mediated hepatic disorder 62.56 41.10 17 2691 2497 42616130
Enterocolitis 60.44 41.10 23 2685 9906 42608721
Malignant neoplasm progression 52.40 41.10 48 2660 108352 42510275
Myocarditis 52.15 41.10 25 2683 18913 42599714
Hypopituitarism 51.79 41.10 15 2693 2776 42615851
Drug-induced liver injury 50.49 41.10 31 2677 38242 42580385
Death 47.82 41.10 97 2611 471088 42147539
Adrenal insufficiency 46.17 41.10 23 2685 18901 42599726
Pyrexia 44.61 41.10 85 2623 393957 42224670
Liver disorder 44.51 41.10 29 2679 39615 42579012
Immune-mediated myocarditis 41.96 41.10 12 2696 2122 42616505
Cytokine release syndrome 41.45 41.10 29 2679 44498 42574129

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
Biliary tract infection 324.13 45.02 56 4026 1668 110583549
Immune-mediated hepatitis 226.61 45.02 52 4030 6659 110578558
Immune-mediated enterocolitis 200.11 45.02 51 4031 10134 110575083
Colitis 193.72 45.02 88 3994 102235 110482982
Pneumonitis 164.57 45.02 72 4010 76459 110508758
Pyrexia 123.80 45.02 158 3924 898107 109687110
Myocarditis 108.31 45.02 41 4041 30014 110555203
Bile duct stenosis 86.36 45.02 20 4062 2656 110582561
Adrenal insufficiency 84.94 45.02 38 4044 42352 110542865
Embolism 84.11 45.02 29 4053 16260 110568957
Drug-induced liver injury 80.76 45.02 52 4030 120015 110465202
Immune-mediated hepatic disorder 76.25 45.02 20 4062 4430 110580787
Cytokine release syndrome 72.18 45.02 40 4042 70266 110514951
Hepatic infection 71.26 45.02 15 4067 1284 110583933
Malignant neoplasm progression 69.67 45.02 55 4027 174512 110410705
Presyncope 67.76 45.02 34 4048 48853 110536364
Immune-mediated myocarditis 66.13 45.02 17 4065 3481 110581736
Febrile neutropenia 65.59 45.02 69 4013 316698 110268519
Sepsis 65.47 45.02 70 4012 327276 110257941
Hepatic function abnormal 63.31 45.02 40 4042 89255 110495962
Hypopituitarism 62.30 45.02 17 4065 4373 110580844
Urinary tract obstruction 59.53 45.02 17 4065 5160 110580057
Cholangitis infective 53.65 45.02 11 4071 828 110584389
Platelet count decreased 52.72 45.02 53 4029 230390 110354827
Enterocolitis infectious 51.97 45.02 14 4068 3430 110581787
Liver carcinoma ruptured 50.47 45.02 9 4073 321 110584896
Small intestinal obstruction 49.37 45.02 24 4058 32189 110553028
Diarrhoea 48.62 45.02 120 3962 1139385 109445832
Bacillus infection 46.48 45.02 11 4071 1603 110583614
Death 45.03 45.02 87 3995 698782 109886435

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FX20 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D000970 Antineoplastic Agents
FDA PE N0000182157 Increased T Lymphocyte Activation
FDA MoA N0000182634 CTLA-4-directed Antibody Interactions
FDA EPC N0000182635 CTLA-4-directed Blocking Antibody
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
amivantamabbelantamab mafodotinblinatumomabbrentuximab vedotincatumaxomabdatopotamab deruxtecanelotuzumabelranatamabenfortumab vedotinepcoritamabgemtuzumab ozogamicinglofitamab show all 29 →

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

DiseaseRelationSNOMED_IDDOID
Liver cell carcinoma indication 109841003 DOID:684
Non-small cell lung cancer, negative for epidermal growth factor receptor expression indication 427038005
Metastatic non-small cell lung cancer with no anaplastic lymphoma kinase genomic tumor aberrations indication 830055006




🐶 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
Cytotoxic T-lymphocyte protein 4 Surface antigen BINDING AGENT Kd 8.23 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
CHEBI:753608 CHEBI
CHEMBL2108658 ChEMBL_ID
C520704 MESH_SUPPLEMENTAL_RECORD_UI
8462 IUPHAR_LIGAND_ID
DB11771 DRUGBANK_ID
2054101000122107 SNOMEDCT_US
4041790 VANDF
4041791 VANDF
C2351038 UMLSCUI
8716 INN_ID
D06657 KEGG_DRUG
362315 MMSL
40997 MMSL
d09937 MMSL
019215 NDDF
QEN1X95CIX UNII
2619312 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
IMJUDO HUMAN PRESCRIPTION DRUG LABEL 1 0310-4505 INJECTION, SOLUTION 25 mg INTRAVENOUS BLA 24 sections
IMJUDO HUMAN PRESCRIPTION DRUG LABEL 1 0310-4535 INJECTION, SOLUTION 300 mg INTRAVENOUS BLA 24 sections