belatacept 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 207.47 40.22 42 1236 4076 46680708
Transplant rejection 141.90 40.22 36 1242 9560 46675224
Graft loss 101.23 40.22 16 1262 371 46684413
Cytomegalovirus infection 69.78 40.22 24 1254 18120 46666664
Eye infection toxoplasmal 61.16 40.22 10 1268 288 46684496
Tonsil cancer 57.24 40.22 9 1269 201 46684583
Thrombotic microangiopathy 56.68 40.22 17 1261 8289 46676495
Haemolytic uraemic syndrome 55.27 40.22 13 1265 2501 46682283
Herpes simplex meningitis 54.02 40.22 7 1271 35 46684749
Polyomavirus viraemia 51.61 40.22 9 1269 384 46684400
Off label use 49.52 40.22 56 1222 379785 46304999
Cytomegalovirus gastrointestinal infection 47.50 40.22 8 1270 277 46684507
Pneumocystis jirovecii pneumonia 42.85 40.22 16 1262 15232 46669552
Varicella zoster virus infection 40.60 40.22 10 1268 2333 46682451
Disseminated cryptococcosis 40.43 40.22 7 1271 286 46684498

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 311.27 40.11 74 1590 7435 29943379
Transplant rejection 109.55 40.11 34 1630 9172 29941642
Graft loss 94.66 40.11 19 1645 851 29949963
Post transplant lymphoproliferative disorder 73.31 40.11 22 1642 5284 29945530
COVID-19 66.71 40.11 28 1636 17850 29932964
BK virus infection 59.87 40.11 18 1646 4346 29946468
Thrombotic microangiopathy 51.54 40.11 19 1645 8591 29942223
Retinal artery occlusion 46.39 40.11 12 1652 1672 29949142

Pharmacologic Action:

SourceCodeDescription
ATC L04AA28 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D000970 Antineoplastic Agents
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Renal transplant rejection indication 236570004

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
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