belatacept 🐶 Veterinary Use | 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	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 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	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 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	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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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:

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
713475001	SNOMEDCT_US
714777004	SNOMEDCT_US
013827	NDDF

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