tocilizumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
humanized origin	4933	375823-41-9

Description:

Molecule	Description
Synonyms: tocilizumab MRA RoActemra actemra R-1569 tocilizumab (genetical recombination)	A humanised anti-interleukin-6 receptor monoclonal antibody. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

tocilizumab
MRA
RoActemra
actemra
R-1569
tocilizumab (genetical recombination)

A humanised anti-interleukin-6 receptor monoclonal antibody. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19.

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

Dose	Unit	Route
20	mg	P

ADMET properties:

None

Approvals:

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Date	Agency	Company
Jan. 16, 2009	EMA	Chugai Pharmaceutical Co., Ltd
Jan. 8, 2010	FDA	GENENTECH
March 6, 2008	PMDA	Chugai Pharmaceutical Co., Ltd

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FDA Adverse Event Reporting System (Female)

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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
Drug ineffective	4995.80	15.06	16833	410976	1027932	62033281
Contraindicated product administered	4428.58	15.06	6335	421474	211313	62849900
Joint swelling	3444.61	15.06	7113	420696	320553	62740660
Drug intolerance	3278.23	15.06	6730	421079	301931	62759282
Synovitis	3227.98	15.06	5042	422767	181876	62879337
Treatment failure	3123.66	15.06	5140	422669	193903	62867310
Arthropathy	2671.79	15.06	5272	422537	229520	62831693
Therapeutic product effect decreased	2431.70	15.06	4529	423280	188658	62872555
Pemphigus	2391.25	15.06	4370	423439	179356	62881857
Systemic lupus erythematosus	2222.47	15.06	4563	423246	204355	62856858

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FDA Adverse Event Reporting System (Male)

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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
Off label use	1880.79	14.44	3023	62285	416501	34475122
Drug ineffective	1683.17	14.44	3017	62291	453734	34437889
Joint swelling	1063.82	14.44	886	64422	59004	34832619
Synovitis	802.19	14.44	431	64877	13635	34877988
Contraindicated product administered	800.45	14.44	499	64809	20982	34870641
No adverse event	778.02	14.44	502	64806	22425	34869198
Intentional product use issue	691.42	14.44	696	64612	59120	34832503
Rheumatoid arthritis	619.32	14.44	537	64771	37701	34853922
Apparent death	576.24	14.44	227	65081	3417	34888206
Treatment failure	566.41	14.44	558	64750	46139	34845484

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FDA Adverse Event Reporting System (Geriatric)

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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
Drug ineffective	4423.85	13.99	12781	350349	1068132	78313126
Synovitis	3881.99	13.99	4073	359057	146661	79234597
Joint swelling	3831.63	13.99	5583	357547	283063	79098195
Contraindicated product administered	3797.63	13.99	4110	359020	153428	79227830
Drug intolerance	3645.46	13.99	5205	357925	258914	79122344
Treatment failure	2889.29	13.99	3715	359415	166771	79214487
Arthropathy	2693.55	13.99	3660	359470	173451	79207807
Therapeutic product effect decreased	2416.83	13.99	3337	359793	160526	79220732
Arthralgia	1819.23	13.99	6221	356909	565582	78815676
Hand deformity	1685.82	13.99	2218	360912	101701	79279557

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AC07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Interleukin inhibitors
FDA EPC	N0000190480	Interleukin-6 Receptor Antagonist
FDA MoA	N0000190478	Interleukin 6 Receptor Antagonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Rheumatoid arthritis	indication	69896004	DOID:7148
Castleman's disease	indication	207036003	DOID:0111157
Juvenile idiopathic arthritis	indication	410502007
Still's disease	indication	410794002
Juvenile rheumatoid arthritis	indication	410795001
Juvenile seropositive polyarthritis	indication	410796000
Juvenile seronegative polyarthritis	indication	410797009
Juvenile idiopathic arthritis, extended oligoarthritis	indication	410800006
Giant cell arteritis	indication	414341000	DOID:13375
Cytokine release syndrome induced by tumor-specific T-cell infusion therapy	indication	710027002

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🐶 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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Interleukin-6 receptor	Membrane receptor	P08887 P40189	IL6RA_HUMAN IL6RB_HUMAN	ANTIBODY BINDING				DRUG LABEL	DRUG LABEL

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External reference:

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ID	Source
013198	NDDF
10150081	PUBCHEM_CID
169600	MMSL
26778	MMSL
4029705	VUID
4029705	VANDF
444648007	SNOMEDCT_US
444649004	SNOMEDCT_US
612865	RXNORM
6881	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-135	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-135	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-135	INJECTION, SOLUTION, CONCENTRATE	80 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-135	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-136	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-136	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-136	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-136	INJECTION, SOLUTION, CONCENTRATE	200 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-137	INJECTION, SOLUTION, CONCENTRATE	20 mg	INTRAVENOUS	BLA	33 sections
ACTEMRA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-137	INJECTION, SOLUTION, CONCENTRATE	400 mg	INTRAVENOUS	BLA	33 sections

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