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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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
Transplant rejection 348.94 41.61 81 2823 12677 90612866
Kidney transplant rejection 256.66 41.61 53 2851 4804 90620739
Cytomegalovirus infection 235.83 41.61 69 2835 26533 90599010
Polyomavirus viraemia 180.41 41.61 32 2872 1285 90624258
Thrombotic microangiopathy 153.45 41.61 44 2860 15699 90609844
Graft loss 110.05 41.61 18 2886 441 90625102
Pneumocystis jirovecii pneumonia 95.38 41.61 33 2871 21583 90603960
Post transplant lymphoproliferative disorder 83.98 41.61 23 2881 6926 90618617
Cytomegalovirus gastrointestinal infection 83.38 41.61 14 2890 404 90625139
Cytomegalovirus viraemia 81.98 41.61 23 2881 7563 90617980
Cervicitis 79.09 41.61 14 2890 554 90624989
Haemophagocytic lymphohistiocytosis 77.58 41.61 26 2878 15433 90610110
Haemolytic uraemic syndrome 72.23 41.61 17 2887 2794 90622749
Acute kidney injury 69.51 41.61 67 2837 320320 90305223
Polyomavirus-associated nephropathy 68.94 41.61 16 2888 2474 90623069
Off label use 68.43 41.61 124 2780 1102128 89523415
Herpes simplex meningitis 57.00 41.61 8 2896 66 90625477
Eye infection toxoplasmal 56.09 41.61 10 2894 412 90625131
Nephropathy toxic 54.51 41.61 19 2885 12669 90612874
Cytomegalovirus colitis 54.18 41.61 14 2890 3372 90622171
Tonsil cancer 52.11 41.61 9 2895 308 90625235
Bacillary angiomatosis 52.02 41.61 8 2896 130 90625413
Complications of transplanted kidney 51.45 41.61 13 2891 2865 90622678
Progressive multifocal leukoencephalopathy 47.00 41.61 18 2886 15637 90609906
Leukopenia 44.78 41.61 32 2872 100678 90524865
Kidney fibrosis 44.48 41.61 11 2893 2223 90623320
Pulmonary nocardiosis 43.81 41.61 9 2895 789 90624754
COVID-19 41.67 41.61 38 2866 168805 90456738

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 325.00 31.69 88 3948 8595 42608704
Transplant rejection 269.15 31.69 84 3952 13504 42603795
Cytomegalovirus infection 175.12 31.69 77 3959 32229 42585070
Mycobacterium haemophilum infection 147.20 31.69 27 4009 425 42616874
Post transplant lymphoproliferative disorder 146.00 31.69 48 3988 9072 42608227
Thrombotic microangiopathy 105.89 31.69 43 3993 14739 42602560
Epstein-Barr virus infection 89.78 31.69 34 4002 9684 42607615
Complications of transplanted kidney 84.94 31.69 28 4008 5322 42611977
Graft loss 83.55 31.69 19 4017 896 42616403
Alternaria infection 74.13 31.69 16 4020 592 42616707
BK virus infection 71.38 31.69 28 4008 8756 42608543
Cytomegalovirus viraemia 70.24 31.69 29 4007 10348 42606951
COVID-19 67.38 31.69 68 3968 115880 42501419
Plasmodium falciparum infection 60.59 31.69 10 4026 81 42617218
Pneumocystis jirovecii pneumonia 58.86 31.69 34 4002 25147 42592152
Off label use 54.48 31.69 157 3879 638178 41979121
Disseminated tuberculosis 53.89 31.69 17 4019 2807 42614492
Polyomavirus-associated nephropathy 49.52 31.69 19 4017 5596 42611703
Progressive multifocal leukoencephalopathy 48.24 31.69 23 4013 11513 42605786
Transplant dysfunction 47.11 31.69 16 4020 3327 42613972
Human herpesvirus 8 infection 45.90 31.69 13 4023 1484 42615815
Cytomegalovirus chorioretinitis 42.09 31.69 16 4020 4595 42612704
Skin papilloma 41.85 31.69 14 4022 2780 42614519
Cytomegalovirus colitis 40.66 31.69 15 4021 3966 42613333
Enterocolitis fungal 40.57 31.69 6 4030 21 42617278
Disseminated blastomycosis 40.33 31.69 9 4027 389 42616910
Brain abscess 39.59 31.69 15 4021 4269 42613030
New onset diabetes after transplantation 39.53 31.69 8 4028 215 42617084
Acute kidney injury 38.79 31.69 98 3938 367239 42250060
Retinal artery occlusion 36.79 31.69 12 4024 2203 42615096
Product preparation issue 35.99 31.69 10 4026 1065 42616234
Enterococcal infection 35.63 31.69 19 4017 12020 42605279
Blastomycosis 35.22 31.69 9 4027 695 42616604
Polyomavirus viraemia 33.30 31.69 11 4025 2101 42615198
Inferior vena cava stenosis 32.91 31.69 6 4030 91 42617208
Renal transplant failure 32.66 31.69 10 4026 1495 42615804

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
Transplant rejection 516.20 30.53 143 6400 24424 110558332
Kidney transplant rejection 497.54 30.53 120 6423 11867 110570889
Cytomegalovirus infection 385.16 30.53 138 6405 54306 110528450
Post transplant lymphoproliferative disorder 251.70 30.53 74 6469 15539 110567217
Thrombotic microangiopathy 221.49 30.53 78 6465 29071 110553685
Polyomavirus viraemia 181.77 30.53 42 6501 3432 110579324
Pneumocystis jirovecii pneumonia 175.40 30.53 73 6470 42662 110540094
Graft loss 160.46 30.53 32 6511 1296 110581460
Mycobacterium haemophilum infection 147.33 30.53 27 6516 692 110582064
Cytomegalovirus viraemia 132.83 30.53 47 6496 17717 110565039
COVID-19 118.02 30.53 105 6438 244955 110337801
Complications of transplanted kidney 114.31 30.53 34 6509 7408 110575348
Epstein-Barr virus infection 111.89 30.53 42 6501 18696 110564060
Off label use 108.29 30.53 258 6285 1499927 109082829
Progressive multifocal leukoencephalopathy 106.97 30.53 44 6499 24912 110557844
Acute kidney injury 101.80 30.53 154 6389 635276 109947480
Disseminated tuberculosis 94.46 30.53 27 6516 5119 110577637
Polyomavirus-associated nephropathy 90.17 30.53 29 6514 8172 110574584
BK virus infection 87.89 30.53 32 6511 13074 110569682
Haemophagocytic lymphohistiocytosis 87.64 30.53 41 6502 31518 110551238
Cytomegalovirus colitis 81.87 30.53 26 6517 7035 110575721
Cervicitis 78.65 30.53 14 6529 303 110582453
Alternaria infection 73.49 30.53 16 6527 996 110581760
Cytomegalovirus gastrointestinal infection 67.11 30.53 14 6529 710 110582046
Transplant dysfunction 65.93 30.53 23 6520 8305 110574451
Cytomegalovirus chorioretinitis 65.46 30.53 22 6521 7106 110575650
Haemolytic uraemic syndrome 64.66 30.53 20 6523 4965 110577791
JC virus infection 59.36 30.53 19 6524 5271 110577485
Nephropathy toxic 59.15 30.53 30 6513 27448 110555308
Plasmodium falciparum infection 58.69 30.53 10 6533 166 110582590
Kidney fibrosis 58.57 30.53 18 6525 4374 110578382
Leukopenia 58.45 30.53 57 6486 148734 110434022
Epstein-Barr viraemia 57.79 30.53 17 6526 3562 110579194
Eye infection toxoplasmal 55.10 30.53 12 6531 748 110582008
Focal segmental glomerulosclerosis 51.11 30.53 16 6527 4129 110578627
Brain abscess 50.91 30.53 18 6525 6756 110576000
Respiratory failure 50.63 30.53 63 6480 215269 110367487
Herpes simplex meningitis 49.53 30.53 8 6535 94 110582662
Human herpesvirus 8 infection 49.08 30.53 13 6530 1858 110580898
Diffuse large B-cell lymphoma 48.33 30.53 22 6521 15876 110566880
Enterococcal infection 46.07 30.53 23 6520 20343 110562413
Posterior reversible encephalopathy syndrome 45.28 30.53 27 6516 33834 110548922
Oesophageal candidiasis 44.91 30.53 19 6524 11515 110571241
Pulmonary nocardiosis 44.70 30.53 13 6530 2616 110580140
Renal transplant failure 44.46 30.53 13 6530 2667 110580089
Histoplasmosis disseminated 43.73 30.53 14 6529 3885 110578871
Disseminated blastomycosis 42.77 30.53 9 6534 476 110582280
Hepatitis B reactivation 41.86 30.53 16 6527 7468 110575288
Opportunistic infection 40.88 30.53 13 6530 3530 110579226
Enterocolitis fungal 40.74 30.53 6 6537 36 110582720
Klebsiella infection 40.61 30.53 21 6522 19988 110562768
Renal vein thrombosis 40.20 30.53 10 6533 1115 110581641
Blastomycosis 40.11 30.53 10 6533 1125 110581631
Renal tubular necrosis 39.97 30.53 24 6519 30451 110552305
Bacillary angiomatosis 39.11 30.53 8 6535 368 110582388
Delayed graft function 38.53 30.53 13 6530 4244 110578512
New onset diabetes after transplantation 38.21 30.53 8 6535 413 110582343
Hospitalisation 37.23 30.53 44 6499 142449 110440307
Skin papilloma 35.92 30.53 14 6529 6882 110575874
Disseminated cryptococcosis 35.90 30.53 11 6532 2646 110580110
Retinal artery occlusion 34.65 30.53 12 6531 4237 110578519
Inferior vena cava stenosis 34.35 30.53 6 6537 116 110582640
Tonsil cancer 33.90 30.53 9 6534 1297 110581459
Meningitis cryptococcal 33.31 30.53 12 6531 4750 110578006
Renal tubular atrophy 33.22 30.53 10 6533 2266 110580490
Aspergillus infection 33.14 30.53 20 6523 25596 110557160
Pre-eclampsia 32.85 30.53 14 6529 8636 110574120
Kaposi sarcoma inflammatory cytokine syndrome 32.05 30.53 6 6537 173 110582583
Pain 31.14 30.53 9 6534 954946 109627810
Lymphocele 30.70 30.53 9 6534 1862 110580894

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA28 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D000082082 Immune Checkpoint Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
MeSH PA D018501 Antirheumatic 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
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:76595 nephroprotective agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L04AA Selective immunosuppressants 10 drugs
abataceptalefaceptapremilastbelumosudilcladribinegusperimusimlifidasemycophenolic acidnerandomilastremibrutinib

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
CHEBI:750070 CHEBI
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
013827 NDDF
713475001 SNOMEDCT_US
714777004 SNOMEDCT_US

Pharmaceutical products:

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