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

Stem definitionDrug idCAS RN
cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) receptors 5091 706808-37-9

Description:

MoleculeDescription

Synonyms:

  • belatacept
  • BMS-224818
  • nulojix
  • BMS 224818
Belatacept, a selective T-cell (lymphocyte) costimulation blocker, binds to CD80 and CD86 on antigen-presenting cells thereby blocking CD28 mediated costimulation of T lymphocytes. In vitro, belatacept inhibits T lymphocyte proliferation and the production of the cytokines interleukin-2, interferon-gamma, interleukin-4, and TNF-alfa. Activated T lymphocytes are the predominant mediators of immunologic rejection
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
12.50 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 17, 2011 EMA
June 15, 2011 FDA BRISTOL MYERS SQUIBB

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
Kidney transplant rejection 199.80 46.08 41 1448 3946 50599689
Transplant rejection 153.94 46.08 39 1450 9570 50594065
Graft loss 108.72 46.08 17 1472 340 50603295
Cytomegalovirus infection 100.17 46.08 32 1457 17930 50585705
Thrombotic microangiopathy 71.74 46.08 21 1468 8770 50594865
Eye infection toxoplasmal 61.06 46.08 10 1479 270 50603365
Cytomegalovirus gastrointestinal infection 60.57 46.08 10 1479 284 50603351
Tonsil cancer 56.42 46.08 9 1480 205 50603430
Polyomavirus viraemia 55.97 46.08 10 1479 456 50603179
Haemolytic uraemic syndrome 55.37 46.08 13 1476 2306 50601329
Herpes simplex meningitis 52.29 46.08 7 1482 43 50603592
Intentional product use issue 50.06 46.08 30 1459 76888 50526747

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
Kidney transplant rejection 303.13 37.36 75 2022 6930 29565500
Transplant rejection 172.51 37.36 51 2046 9161 29563269
Graft loss 90.51 37.36 19 2078 829 29571601
Post transplant lymphoproliferative disorder 75.43 37.36 24 2073 5469 29566961
Cytomegalovirus infection 73.91 37.36 35 2062 23180 29549250
COVID-19 70.19 37.36 39 2058 35975 29536455
BK virus infection 58.21 37.36 19 2078 4688 29567742
Thrombotic microangiopathy 57.40 37.36 22 2075 8659 29563771
Retinal artery occlusion 43.91 37.36 12 2085 1611 29570819
Off label use 40.06 37.36 74 2023 300726 29271704
Progressive multifocal leukoencephalopathy 40.02 37.36 17 2080 8702 29563728
Skin papilloma 38.49 37.36 11 2086 1738 29570692
Brain abscess 38.08 37.36 12 2085 2643 29569787
Epstein-Barr virus infection 37.47 37.36 15 2082 6614 29565816

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
Kidney transplant rejection 422.56 34.56 97 3070 9414 64486151
Transplant rejection 235.60 34.56 69 3098 17332 64478233
Graft loss 168.87 34.56 31 3136 976 64494589
Cytomegalovirus infection 162.49 34.56 63 3104 37136 64458429
Thrombotic microangiopathy 108.91 34.56 38 3129 16617 64478948
Pneumocystis jirovecii pneumonia 100.35 34.56 41 3126 27593 64467972
COVID-19 96.58 34.56 52 3115 65088 64430477
Post transplant lymphoproliferative disorder 83.03 34.56 27 3140 9517 64486048
BK virus infection 68.68 34.56 22 3145 7390 64488175
Progressive multifocal leukoencephalopathy 65.98 34.56 27 3140 18205 64477360
Off label use 59.85 34.56 109 3058 632697 63862868
Eye infection toxoplasmal 56.49 34.56 11 3156 476 64495089
Cytomegalovirus colitis 54.93 34.56 16 3151 3912 64491653
Respiratory failure 54.12 34.56 52 3115 161131 64334434
Cytomegalovirus gastrointestinal infection 51.06 34.56 10 3157 446 64495119
Herpes simplex meningitis 48.03 34.56 7 3160 48 64495517
Cytomegalovirus viraemia 45.98 34.56 18 3149 10810 64484755
Haemolytic uraemic syndrome 45.89 34.56 14 3153 4007 64491558
Cervicitis 45.72 34.56 8 3159 190 64495375
Acute kidney injury 44.36 34.56 79 3088 449161 64046404
Polyomavirus viraemia 41.74 34.56 10 3157 1152 64494413
Retinal artery occlusion 41.36 34.56 12 3155 2891 64492674
Epstein-Barr virus infection 40.14 34.56 17 3150 12471 64483094
Cytomegalovirus chorioretinitis 39.10 34.56 13 3154 4899 64490666
Tonsil cancer 38.33 34.56 9 3158 951 64494614
Complications of transplanted kidney 37.81 34.56 13 3154 5422 64490143
Brain abscess 37.05 34.56 12 3155 4169 64491396
Aspergillus infection 35.71 34.56 17 3150 16362 64479203

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA28 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D018501 Antirheumatic Agents
MeSH PA D000082082 Immune Checkpoint Inhibitors
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
FDA MoA N0000182150 CD80-directed Antibody Interactions
FDA MoA N0000182151 CD86-directed Antibody Interactions
FDA PE N0000182829 T Lymphocyte Costimulation Activity Blockade
FDA EPC N0000182830 Selective T Cell Costimulation Blocker

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

DiseaseRelationSNOMED_IDDOID
Renal transplant rejection indication 236570004




🐶 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
T-lymphocyte activation antigen CD80 Surface antigen INHIBITOR DRUG LABEL DRUG LABEL
T-lymphocyte activation antigen CD86 Surface antigen INHIBITOR DRUG LABEL DRUG LABEL

External reference:

IDSource
E3B2GI648A UNII
D03222 KEGG_DRUG
4030905 VANDF
C1619962 UMLSCUI
CHEMBL1742990 ChEMBL_ID
DB06681 DRUGBANK_ID
D000069594 MESH_DESCRIPTOR_UI
8627 INN_ID
6892 IUPHAR_LIGAND_ID
1112973 RXNORM
183036 MMSL
27948 MMSL
d07787 MMSL
713475001 SNOMEDCT_US
714777004 SNOMEDCT_US
013827 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NULOJIX HUMAN PRESCRIPTION DRUG LABEL 1 0003-0371 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS BLA 30 sections