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
Transplant rejection	228.22	38.90	55	1863	10725	63476379
Kidney transplant rejection	207.40	38.90	43	1875	4228	63482876
Polyomavirus viraemia	143.86	38.90	24	1894	710	63486394
Cytomegalovirus infection	135.27	38.90	42	1876	20910	63466194
Graft loss	107.51	38.90	17	1901	356	63486748
Thrombotic microangiopathy	106.86	38.90	30	1888	10531	63476573
Pneumocystis jirovecii pneumonia	80.81	38.90	27	1891	16887	63470217
Cytomegalovirus gastrointestinal infection	73.92	38.90	12	1906	298	63486806
Cervicitis	61.37	38.90	11	1907	497	63486607
Eye infection toxoplasmal	60.26	38.90	10	1908	285	63486819
Cytomegalovirus viraemia	56.89	38.90	16	1902	5633	63481471
Tonsil cancer	55.49	38.90	9	1909	222	63486882
Off label use	55.00	38.90	83	1835	674379	62812725
Post transplant lymphoproliferative disorder	54.09	38.90	15	1903	5016	63482088
Haemolytic uraemic syndrome	54.03	38.90	13	1905	2490	63484614
Herpes simplex meningitis	51.83	38.90	7	1911	45	63487059
Haemophagocytic lymphohistiocytosis	46.93	38.90	16	1902	10611	63476493
Nephropathy toxic	44.72	38.90	15	1903	9464	63477640
Diffuse large B-cell lymphoma	41.33	38.90	13	1905	6699	63480405
Cytomegalovirus colitis	39.48	38.90	10	1908	2362	63484742

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	293.42	34.10	75	2554	7422	34946880
Transplant rejection	215.56	34.10	63	2566	10248	34944054
Cytomegalovirus infection	110.98	34.10	49	2580	26086	34928216
COVID-19	90.99	34.10	62	2567	77488	34876814
Graft loss	88.61	34.10	19	2610	864	34953438
Post transplant lymphoproliferative disorder	73.86	34.10	25	2604	6503	34947799
Thrombotic microangiopathy	72.51	34.10	28	2601	10602	34943700
Alternaria infection	71.96	34.10	14	2615	389	34953913
BK virus infection	65.01	34.10	22	2607	5716	34948586
Pneumocystis jirovecii pneumonia	58.86	34.10	29	2600	19681	34934621
Mycobacterium haemophilum infection	54.20	34.10	9	2620	98	34954204
Off label use	47.82	34.10	100	2529	419424	34534878
Epstein-Barr virus infection	44.66	34.10	18	2611	7610	34946692
Retinal artery occlusion	41.43	34.10	12	2617	1873	34952429
Skin papilloma	40.13	34.10	12	2617	2091	34952211
Complications of transplanted kidney	38.16	34.10	14	2615	4595	34949707
Transplant dysfunction	37.41	34.10	12	2617	2637	34951665
Disseminated blastomycosis	37.33	34.10	7	2622	159	34954143
Progressive multifocal leukoencephalopathy	37.20	34.10	17	2612	9747	34944555
Polyomavirus-associated nephropathy	36.80	34.10	13	2616	3831	34950471
Brain abscess	35.46	34.10	12	2617	3113	34951189
Cytomegalovirus viraemia	34.95	34.10	15	2614	7415	34946887

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	418.86	32.60	99	4094	10147	79730048
Transplant rejection	346.77	32.60	97	4096	19340	79720855
Cytomegalovirus infection	234.39	32.60	87	4106	42557	79697638
Pneumocystis jirovecii pneumonia	166.40	32.60	63	4130	32445	79707750
Graft loss	165.63	32.60	31	4162	1012	79739183
Post transplant lymphoproliferative disorder	149.92	32.60	45	4148	11419	79728776
Thrombotic microangiopathy	144.01	32.60	50	4143	20119	79720076
COVID-19	133.72	32.60	90	4103	157584	79582611
Polyomavirus viraemia	115.90	32.60	25	4168	1682	79738513
Off label use	82.87	32.60	160	4033	907055	78833140
Cytomegalovirus viraemia	77.11	32.60	28	4165	12793	79727402
BK virus infection	75.26	32.60	25	4168	8779	79731416
Alternaria infection	69.60	32.60	14	4179	668	79739527
Progressive multifocal leukoencephalopathy	64.24	32.60	28	4165	20572	79719623
Cervicitis	62.92	32.60	11	4182	242	79739953
Complications of transplanted kidney	62.18	32.60	20	4173	6346	79733849
Cytomegalovirus gastrointestinal infection	61.24	32.60	12	4181	500	79739695
Eye infection toxoplasmal	60.34	32.60	12	4181	540	79739655
Mycobacterium haemophilum infection	55.19	32.60	9	4184	128	79740067
Haemophagocytic lymphohistiocytosis	53.23	32.60	25	4168	21812	79718383
Epstein-Barr virus infection	52.91	32.60	22	4171	14394	79725801
Acute kidney injury	51.29	32.60	95	4098	519309	79220886
Kidney fibrosis	51.07	32.60	15	4178	3520	79736675
Cytomegalovirus colitis	51.05	32.60	16	4177	4669	79735526
Respiratory failure	49.52	32.60	54	4139	180857	79559338
Herpes simplex meningitis	46.71	32.60	7	4186	55	79740140
Disseminated tuberculosis	44.39	32.60	14	4179	4169	79736026
Transplant dysfunction	44.27	32.60	16	4177	7205	79732990
Polyomavirus-associated nephropathy	44.21	32.60	15	4178	5612	79734583
Renal tubular necrosis	44.16	32.60	23	4170	25016	79715179
Epstein-Barr viraemia	43.81	32.60	12	4181	2193	79738002
Haemolytic uraemic syndrome	43.54	32.60	14	4179	4435	79735760
Diffuse large B-cell lymphoma	42.77	32.60	18	4175	12131	79728064
Cytomegalovirus chorioretinitis	40.65	32.60	14	4179	5476	79734719
Pulmonary nocardiosis	39.85	32.60	10	4183	1301	79738894
Nephropathy toxic	39.61	32.60	20	4173	20399	79719796
Retinal artery occlusion	39.05	32.60	12	4181	3282	79736913
Disseminated blastomycosis	38.66	32.60	7	4186	189	79740006
Klebsiella infection	38.32	32.60	18	4175	15702	79724493
Disseminated cryptococcosis	36.52	32.60	10	4183	1824	79738371
Opportunistic infection	36.05	32.60	11	4182	2939	79737256
Tonsil cancer	35.96	32.60	9	4184	1159	79739036
Blastomycosis	34.88	32.60	8	4185	711	79739484
Adenovirus infection	34.78	32.60	14	4179	8433	79731762
Brain abscess	34.28	32.60	12	4181	4924	79735271

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