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

Stem definition	Drug id	CAS RN
cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) receptors	5091	706808-37-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
12.50	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
June 17, 2011	EMA
June 15, 2011	FDA	BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
T-lymphocyte activation antigen CD80	Surface antigen	P33681	CD80_HUMAN	INHIBITOR				DRUG LABEL	DRUG LABEL
T-lymphocyte activation antigen CD86	Surface antigen	P42081	CD86_HUMAN	INHIBITOR				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NULOJIX	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0371	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	250 mg	INTRAVENOUS	BLA	30 sections