Identification

Name
Tocilizumab
Accession Number
DB06273
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

Tocilizumab is a recombinant humanized monoclonal antibody IL-6 receptor inhibitor used to treat inflammatory and autoimmune conditions.6 It was first described in the literature in 2003 when Chugai, a subsidiary of Roche began developing IL-6 inhibiting monoclonal antibodies.2 It is currently being investigated to treat severely ill patients with COVID-19.1,7,8

Tocilizumab was granted FDA approval on 8 January 2010.6

Protein structure
Db06273
Protein chemical formula
C6428H9976N1720O2018S42
Protein average weight
148000.0 Da
Sequences
>Tocilizumab light chain:
DIQMTQSPSSLSASVGDRVTITCRASQDISSYLNWYQQKPGKAPKLLIYYTSRLHSGVPS
RFSGSGSGTDFTFTISSLQPEDIATYYCQQGNTLPYTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
References:
  1. US Patent US10323095B2: Antibody-fynomer conjugates [Link]
>Tocilizumab heavy chain:
QVQLQESGPGLVRPSQTLSLTCTVSGYSITSDHAWSWVRQPPGRGLEWIGYISYSGITTY
NPSLKSRVTMLRDTSKNQFSLRLSSVTAADTAVYYCARSLARTTAMDYWGQGSLVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPG
References:
  1. US Patent US10323095B2: Antibody-fynomer conjugates [Link]
Download FASTA Format
Synonyms
  • Atlizumab
External IDs
MRA / MSB-11456 / MSB11456 / R-1569 / RG-1569 / RHPM-1 / RO-4877533
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ActemraInjection, solution, concentrate20 mg/1mLIntravenousGenentech, Inc.2010-01-08Not applicableUs
ActemraInjection, solution, concentrate20 mg/1mLIntravenousGenentech, Inc.2010-01-08Not applicableUs
ActemraSolution162 mgSubcutaneousHoffmann La Roche2019-01-15Not applicableCanada
ActemraSolution162 mgSubcutaneousHoffmann La Roche2014-05-30Not applicableCanada
ActemraSolution400 mgIntravenousHoffmann La Roche2010-05-26Not applicableCanada
ActemraSolution200 mgIntravenousHoffmann La Roche2010-05-26Not applicableCanada
ActemraSolution80 mgIntravenousHoffmann La Roche2010-05-26Not applicableCanada
ActemraInjection, solution180 mg/1mLSubcutaneousGenentech, Inc.2013-10-21Not applicableUs
ActemraInjection, solution, concentrate20 mg/1mLIntravenousGenentech, Inc.2010-01-08Not applicableUs
Actemra ACTPenInjection, solution180 mg/1mLSubcutaneousGenentech, Inc.2018-11-19Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
RoActemra
Categories
UNII
I031V2H011
CAS number
375823-41-9

Pharmacology

Indication

Tocilizumab is indicated to treat moderate to severe rheumatoid arthritis, giant cell arteritis, polyarticular juvenile idiopathic arthritis, systemic juvenile idiopathic arthritis, and cytokine release syndrome.6

Associated Conditions
Pharmacodynamics

Tocilizumab is an IL-6 inhibiting monoclonal antibody used to treat autoimmune and inflammatory conditions.6 Tocilizumab has a long duration of action as it is generally given every 4 weeks and has a wide therapeutic index.6 Patients should be counselled regarding the risk of infections, GI perforation, and hepatotoxicity.6

Mechanism of action

Interleukin 6 (IL-6) is a pro-inflammatory cytokine produced by cells including T-cells, B-cells, lymphocytes, monocytes, fibroblasts.6 IL-6 rapidly induces C-reactive protein, serum amyloid A, fibrinogen, haptoglobin, and α-1-antichymotrypsin while inhibiting production of fibronectin, albumin, and transferrin.4 IL-6 also induces antibody production, induces cytotoxic T-cell differentiation, and inhibits regulatory T-cell differentiation.4 Tocilizumab binds soluble and membrane bound IL-6 receptors, preventing IL-6 mediated inflammation.6

TargetActionsOrganism
AInterleukin-6 receptor subunit alpha
inhibitor
antibody
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

A 162mg subcutaneous dose given weekly has a Cmax of 51.3±23.2µg/mL and an AUC of 8254±3833µg*h/mL.5 A 162mg subcutaneous dose given every 2 weeks has a Cmax of 13±8.3µg/mL and an AUC of 3460±2530µg*h/mL.5 A 162mg subcutaneous dose given every 4 weeks has a Cmax of 154±42µg/mL and an AUC of 39216±14304µg*h/mL.5

Volume of distribution

In rheumatoid arthritis patients, the central volume of distribution is 3.5L, the peripheral volume of distribution is 2.9L, and the volume of distribution at steady state is 6.4L.6 In giant cell arteritis patients, the central volume of distribution is 4.09L, the peripheral volume of distribution if 3.37L, and the volume of distribution at steady state is 7.46L.6 In pediatric patients with polyarticular juvenile arthritis, the central volume of distribution is 1.98L, the peripheral volume of distribution is 2.1L, and the volume of distribution at steady state is 4.08L.6 In pediatric patients with systemic juvenile idiopathic arthritis, the central volume of distribution is 1.87L, the peripheral volume of distribution is 2.14L, and the volume of distribution at steady state is 4.01L.6

Protein binding

Data regarding the serum protein binding of tocilizumab is not readily available.6

Metabolism

Tocilizumab, like other monoclonal antibodies, is expected to be metabolized to smaller proteins and amino acids by proteolytic enzymes.3

Route of elimination

Data regarding the exact route of elimination of monoclonal antibodies is not readily available.3,6

Half life

The half life of tocilizumab is concentration dependent.6 The terminal half life in rheumatoid arthritis patients is 21.5 days.6 The absorption half life in rheumatoid arthritis and giant cell arteritis patients was 4 days, and in polyarticular juvenile idiopathic arthritis patients and systemic juvenile idiopathic arthritis patients was 2 days.6

Clearance

The linear clearance in rheumatoid arthritis patients is 12.5mL/h, in giant cell arteritis patients is 6.7mL/h, in polyarticular juvenile idiopathic arthritis patients is 5.8mL/h, and in systemic juvenile idiopathic arthritis is 5.7mL/h.6 Clearance is dose dependent and changes from non linear at low doses to linear at higher doses.6

Toxicity

Data regarding overdoses of tocilizumab are not readily available.6 Patients experiencing an overdose may develop neutropenia.6 In case of overdose, monitor patients for signs of adverse reactions and provide symptomatic and supportive treatment.6

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be increased when combined with Tocilizumab.
(S)-WarfarinThe metabolism of (S)-Warfarin can be increased when combined with Tocilizumab.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Tocilizumab.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be increased when combined with Tocilizumab.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be increased when combined with Tocilizumab.
5-methoxy-N,N-dimethyltryptamineThe metabolism of 5-methoxy-N,N-dimethyltryptamine can be increased when combined with Tocilizumab.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be increased when combined with Tocilizumab.
8-azaguanineThe metabolism of 8-azaguanine can be increased when combined with Tocilizumab.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be increased when combined with Tocilizumab.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Tocilizumab is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
No interactions found.

References

General References
  1. Cellina M, Orsi M, Bombaci F, Sala M, Marino P, Oliva G: Favorable changes of CT findings in a patient with COVID-19 pneumonia after treatment with tocilizumab. Diagn Interv Imaging. 2020 Mar 31. pii: S2211-5684(20)30087-5. doi: 10.1016/j.diii.2020.03.010. [PubMed:32278585]
  2. Ding C, Jones G: Technology evaluation: MRA, Chugai. Curr Opin Mol Ther. 2003 Feb;5(1):64-9. [PubMed:12669473]
  3. Keizer RJ, Huitema AD, Schellens JH, Beijnen JH: Clinical pharmacokinetics of therapeutic monoclonal antibodies. Clin Pharmacokinet. 2010 Aug;49(8):493-507. doi: 10.2165/11531280-000000000-00000. [PubMed:20608753]
  4. Tanaka T, Narazaki M, Kishimoto T: IL-6 in inflammation, immunity, and disease. Cold Spring Harb Perspect Biol. 2014 Sep 4;6(10):a016295. doi: 10.1101/cshperspect.a016295. [PubMed:25190079]
  5. Abdallah H, Hsu JC, Lu P, Fettner S, Zhang X, Douglass W, Bao M, Rowell L, Burmester GR, Kivitz A: Pharmacokinetic and Pharmacodynamic Analysis of Subcutaneous Tocilizumab in Patients With Rheumatoid Arthritis From 2 Randomized, Controlled Trials: SUMMACTA and BREVACTA. J Clin Pharmacol. 2017 Apr;57(4):459-468. doi: 10.1002/jcph.826. Epub 2016 Nov 17. [PubMed:27599663]
  6. FDA Approved Drug Products: Actemra Tocilizumab Intravenous or Subcutaneous Injection [Link]
  7. Clinical Trials: TOCIVID-19 [Link]
  8. Clinical Trials: COVACTA [Link]
External Links
KEGG Drug
D02596
PubChem Substance
347910344
RxNav
612865
ChEMBL
CHEMBL1237022
PharmGKB
PA165292659
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Tocilizumab
ATC Codes
L04AC07 — Tocilizumab
AHFS Codes
  • 92:36.00 — Disease-modifying Antirheumatic Agents
FDA label
Download (512 KB)
MSDS
Download (482 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentAdamantinomatous Craniopharyngioma1
0WithdrawnTreatmentMultiple Myeloma (MM)1
1Active Not RecruitingTreatmentChronic Leukemias / Leukemia, Acute / Malignant Lymphomas / Myelodysplastic Syndromes (MDS)1
1Active Not RecruitingTreatmentGiant Cell Arteritis (GCA)1
1Active Not RecruitingTreatmentJuvenile Idiopathic Arthritis (JIA)1
1Active Not RecruitingTreatmentRheumatoid Arthritis1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceRheumatoid Arthritis1
1CompletedTreatmentCastleman's Disease1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentJuvenile Idiopathic Arthritis (JIA)2
1CompletedTreatmentJuvenile Idiopathic Arthritis (JIA) / Juvenile Idiopathic Arthritis, Rheumatoid Arthritis / Systemic Juvenile Idiopathic Arthritis (SJIA)1
1CompletedTreatmentPharmacokinetics1
1CompletedTreatmentRheumatoid Arthritis3
1CompletedTreatmentSchizophrenia1
1CompletedTreatmentTumors, Solid2
1Not Yet RecruitingTreatmentBiliary Tract Cancer / Hepatic Metastases / Hepatocellular,Carcinoma / Secondary Liver Cancer1
1Not Yet RecruitingTreatmentFollicular Lymphoma (FL)1
1Not Yet RecruitingTreatmentGraft Versus Host Disease (GVHD) / Steroid Refractory GVHD1
1RecruitingTreatmentBreast Cancer1
1RecruitingTreatmentCD19 Positive / CD20 Positive / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic, recurrent Lymphocytic Leukemia / Recurrent Diffuse Large B-Cell Lymphoma / Recurrent Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Primary Mediastinal (Thymic) Large B-Cell Cell Lymphoma / Recurrent Small Lymphocytic Lymphoma / Refractory Diffuse Large B Cell Lymphoma / Refractory Follicular Lymphoma / Refractory Mantle Cell Lymphoma / Refractory Primary Mediastinal (Thymic) Large B-Cell Cell Lymphoma / Refractory Small Lymphocytic Lymphoma1
1RecruitingTreatmentColorectal Cancers1
1RecruitingTreatmentLymphoma, B-Cell1
1RecruitingTreatmentLymphoma, B-Cell / Non-Hodgkin's Lymphoma (NHL)1
1RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL)3
1RecruitingTreatmentPsychotic Disorder NOS / Schizophrenia1
1TerminatedTreatmentAcute Myeloid Leukemia (AML)1
1TerminatedTreatmentB-Cell Chronic Lymphocytic Leukemia / Chronic Lymphocytic Leukaemia (CLL)1
1, 2Active Not RecruitingBasic ScienceHuman Immunodeficiency Virus (HIV) Infections1
1, 2Active Not RecruitingTreatmentChorioretinitis / Non-infectious Intermediate, Posterior, or Pan-uveitis / Pan-uveitis / Uveitis, Intermediate1
1, 2CompletedTreatmentEnd Stage Renal Disease (ESRD)1
1, 2CompletedTreatmentNeuromyelitis Optica / Neuromyelitis Optica Spectrum Disorders1
1, 2CompletedTreatmentRecurrent Ovarian Cancer1
1, 2Not Yet RecruitingTreatmentHepatocellular,Carcinoma1
1, 2RecruitingPreventionCytokine Release Syndrome / Stem Cell Transplant Complications1
1, 2RecruitingTreatmentAcute Lymphocytic Leukemia, Pediatric / B-cell Acute Lymphoblastic Leukemia1
1, 2RecruitingTreatmentB-Cell Non-Hodgkin Lymphomas(NHL)2
1, 2RecruitingTreatmentChronic Subdural Hematomas1
1, 2RecruitingTreatmentDiffuse Large B-Cell Lymphoma (DLBCL)1
1, 2RecruitingTreatmentGiant Cell Arteritis (GCA)1
1, 2RecruitingTreatmentLiving-Donor Kidney Transplants / Renal Transplant Recipient Patients1
1, 2RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1, 2RecruitingTreatmentTransitional Cell Carcinoma1
1, 2RecruitingTreatmentTransplantation, Kidney1
1, 2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
1, 2TerminatedTreatmentGraft Versus Host Disease, Acute1
1, 2TerminatedTreatmentJuvenile Idiopathic Arthritis Associated Uveitis1
2Active Not RecruitingTreatmentCastleman's Disease / Giant Lymph Node Hyperplasia / Multicentric Castleman Disease1
2Active Not RecruitingTreatmentCoronary Heart Disease (CHD) / Myocardial Infarction1
2Active Not RecruitingTreatmentHeart Arrest / Out-Of-Hospital Cardiac Arrest / Systemic Inflammatory Response Syndrome (SIRS)1
2Active Not RecruitingTreatmentInfections, Coronavirus / Novel Coronavirus Infectious Disease (COVID-19)1
2Active Not RecruitingTreatmentMalignancies, Hematologic1
2Active Not RecruitingTreatmentNew-onset Type 1 Diabetes Mellitus / T1D / T1DM / Type 1 Diabetes Mellitus1
2Active Not RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19) / SARS Pneumonia1
2CompletedPreventionAcute Graft Versus Host Disease After Allogeneic Hematopoietic Stem Cell Transplantation / Hematopoietic Stem Cell Transplantation (HSCT)1
2CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS) / Lou Gehrig's Disease / Motor Neurone Disease1
2CompletedTreatmentDermatomyositis / Polymyositis1
2CompletedTreatmentFibrous Dysplasia of Bone1
2CompletedTreatmentGiant Cell Arteritis (GCA)2
2CompletedTreatmentLate Complication From Kidney Transplant1
2CompletedTreatmentNon-ST Elevation Myocardial Infarction1
2CompletedTreatmentNovel Coronavirus Infectious Disease (COVID-19)1
2CompletedTreatmentPolymyalgia Rheumatica (PMR)1
2CompletedTreatmentPulmonary Arterial Hypertension (PAH)1
2CompletedTreatmentRheumatoid Arthritis5
2CompletedTreatmentSchnitzler's Syndrome1
2Enrolling by InvitationTreatmentNovel Coronavirus Infectious Disease (COVID-19) / Respiratory Failure / Viral Pneumonia1
2Not Yet RecruitingTreatmentAdvanced Solid Tumors / Immune-Related Adverse Events1
2Not Yet RecruitingTreatmentAutoimmune Diseases / Inflammatory Diseases1
2Not Yet RecruitingTreatmentBone Marrow Transplant (BMT) / Malignancies, Hematologic1
2Not Yet RecruitingTreatmentCytokine Release Syndrome / Novel Coronavirus Infectious Disease (COVID-19)1
2Not Yet RecruitingTreatmentGiant Cell Arteritis (GCA) / Ischemic Optic Neuropathy1
2Not Yet RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingOtherHematopoietic and Lymphoid Cell Neoplasm / Malignant Solid Neoplasm / Novel Coronavirus Infectious Disease (COVID-19) / Pneumonia / Pneumonitis / Severe Acute Respiratory Distress Syndrome / Symptomatic COVID-19 Infection Laboratory-Confirmed1
2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Acute Myeloid Leukemia (AML) / Leukemia, Acute / Leukemias / Lymphoma, Hodgkins / Myelodysplastic Syndromes (MDS) / Myelodysplastic-Myeloproliferative Diseases / Myeloproliferative Disorders / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentAdenocarcinoma, Prostate1
2RecruitingTreatmentBehcet's Syndrome / Uveitis1
2RecruitingTreatmentBiotherapy / Uveitis1
2RecruitingTreatmentCOVID-19 Pneumonia / Novel Coronavirus Infectious Disease (COVID-19)1
2RecruitingTreatmentCardiac Transplant1
2RecruitingTreatmentCorona Virus Disease / Novel Coronavirus Infectious Disease (COVID-19)1
2RecruitingTreatmentFamilial Mediterranean Fever (FMF )1
2RecruitingTreatmentInfections, Coronavirus / Macrophage Activation Syndrome / Novel Coronavirus Infectious Disease (COVID-19) / Virus Diseases1
2RecruitingTreatmentLeukemias1
2RecruitingTreatmentLymphohistiocytosis, Hemophagocytic1
2RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentMalignant Neoplasm of Pancreas1
2RecruitingTreatmentMelanoma1
2RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19)7
2RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19) / Viral Pneumonia1
2RecruitingTreatmentUnresectable Pancreatic Carcinoma1
2SuspendedTreatmentAdvanced or Metastatic Hematological or Solid Tumor / Novel Coronavirus Infectious Disease (COVID-19) / SARS-CoV-2 (COVID-19) Infection1
2TerminatedTreatmentBehcet's Syndrome1
2TerminatedTreatmentCOVID-19 Pneumonia / Novel Coronavirus Infectious Disease (COVID-19)1
2TerminatedTreatmentErdheim-Chester Disease (ECD)1
2TerminatedTreatmentGlucocorticosteroid Refractory Acute GVHD1
2TerminatedTreatmentRheumatoid Arthritis1
2Unknown StatusTreatmentAdult's Still Disease1
2WithdrawnSupportive CareGraft Versus Host Disease (GVHD)1
2WithdrawnTreatmentDiabetic Macular Edema (DME)1
2WithdrawnTreatmentRelapsing Polychondritis1
2, 3CompletedTreatmentNeuromyelitis Optica / Neuromyelitis Optica Spectrum Disorders1
2, 3CompletedTreatmentPrimary Sjögren's Syndrome (pSS)1
2, 3Enrolling by InvitationTreatmentCoVid 19 Positive / Novel Coronavirus Infectious Disease (COVID-19)1
2, 3RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19) / Severe Acute Respiratory Syndrome1
3Active Not RecruitingSupportive CarePolymyalgia Rheumatica1
3Active Not RecruitingTreatmentCOVID-19 Pneumonia / Novel Coronavirus Infectious Disease (COVID-19)1
3Active Not RecruitingTreatmentJuvenile Idiopathic Arthritis (JIA)1
3Active Not RecruitingTreatmentRheumatoid Arthritis1
3CompletedTreatmentGiant Cell Arteritis (GCA)2
3CompletedTreatmentJuvenile Idiopathic Arthritis (JIA)5
3CompletedTreatmentOsteoarthritis of the Hands1
3CompletedTreatmentPolyarticular Juvenile Idiopathic Arthritis1
3CompletedTreatmentRheumatoid Arthritis67
3CompletedTreatmentSclerosis, Progressive Systemic2
3CompletedTreatmentSystemic Juvenile Idiopathic Arthritis (SJIA)3
3CompletedTreatmentThyroid Associated Ophthalmopathy / Thyroid Eye Disease1
3Not Yet RecruitingTreatmentDiffuse Large B-Cell Lymphoma (DLBCL)1
3Not Yet RecruitingTreatmentInfections, Coronavirus / Inflammatory Reaction / Novel Coronavirus Infectious Disease (COVID-19) / Severe Acute Respiratory Syndrome Coronavirus 21
3Not Yet RecruitingTreatmentIntensive Care Units / Novel Coronavirus Infectious Disease (COVID-19)1
3Not Yet RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19)2
3RecruitingTreatmentCOVID-19 Pneumonia / Novel Coronavirus Infectious Disease (COVID-19)2
3RecruitingTreatmentGiant Cell Arteritis (GCA) / Patients Diagnosed of Giant-cell Arteritis1
3RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19)2
3RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19) / SARS-CoV 21
3RecruitingTreatmentPolymyalgia Rheumatica1
3RecruitingTreatmentRheumatoid Arthritis2
3RecruitingTreatmentTakayasu's Disease1
3TerminatedTreatmentAnkylosing Spondylitis (AS)2
3TerminatedTreatmentJuvenile Idiopathic Arthritis (JIA)1
3TerminatedTreatmentRheumatoid Arthritis1
3WithdrawnTreatmentCerebrovascular Accident / Chronic Obstructive Pulmonary Disease (COPD) / Chronic Renal Failure (CRF) / Coronary Artery Disease (CAD) / Diabetes Mellitus / Neoplasms, Malignant / Novel Coronavirus Infectious Disease (COVID-19) / SARS Coronavirus 2 Infection1
4Active Not RecruitingBasic ScienceRheumatoid Arthritis1
4Active Not RecruitingTreatmentRheumatoid Arthritis3
4CompletedNot AvailableHealthy Volunteers1
4CompletedDevice FeasibilityRheumatoid Arthritis1
4CompletedOtherRheumatoid Arthritis1
4CompletedTreatmentCardiovascular Disease, Rheumatoid Arthritis / Rheumatoid Arthritis1
4CompletedTreatmentJuvenile Idiopathic Arthritis (JIA)1
4CompletedTreatmentRheumatoid Arthritis17
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia1
4Enrolling by InvitationTreatmentRheumatoid Arthritis1
4Not Yet RecruitingTreatmentRheumatoid Arthritis of Knee1
4RecruitingTreatmentAdalimumab / Takayasu's Disease / Tocilizumab / Treatments1
4RecruitingTreatmentCOVID19 Pneumonia / Novel Coronavirus Infectious Disease (COVID-19)1
4RecruitingTreatmentGiant Cell Arteritis (GCA)2
4RecruitingTreatmentJuvenile Idiopathic Arthritis (JIA)1
4RecruitingTreatmentRheumatoid Arthritis7
4RecruitingTreatmentRheumatoid Arthritis / Tocilizumab1
4TerminatedTreatmentRheumatoid Arthritis3
4Unknown StatusTreatmentRheumatoid Arthritis1
4WithdrawnTreatmentRheumatoid Arthritis1
Not AvailableActive Not RecruitingTreatmentLymphoblastic Leukemia, Acute, Childhood1
Not AvailableCompletedNot AvailablePolymyalgia Rheumatica1
Not AvailableCompletedNot AvailablePsoriatic Arthritis / Rheumatoid Arthritis / Spondyloarthritis1
Not AvailableCompletedNot AvailableRheumatoid Arthritis21
Not AvailableCompletedPreventionBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentArthritis / Colitis / Tumors, Solid1
Not AvailableCompletedTreatmentMyocardial Infarction1
Not AvailableCompletedTreatmentRelapsing Polychondritis1
Not AvailableCompletedTreatmentRheumatoid Arthritis3
Not AvailableNo Longer AvailableNot AvailableJuvenile Idiopathic Arthritis (JIA)1
Not AvailableNot Yet RecruitingNot AvailableInfection / Rheumatoid Arthritis1
Not AvailableNot Yet RecruitingNot AvailableNovel Coronavirus Infectious Disease (COVID-19) / Severe Pneumonia1
Not AvailableNot Yet RecruitingNot AvailableRheumatoid Arthritis1
Not AvailableRecruitingNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableRecruitingNot AvailableCarcinoma, Colorectal / Non-Small Cell Lung Carcinoma (NSCLC)1
Not AvailableRecruitingNot AvailableCoronavirus (SARS-CoV) / Cytokine Release Syndrome / Cytokine Storm / Novel Coronavirus Infectious Disease (COVID-19) / Tocilizumab1
Not AvailableRecruitingNot AvailableInflammatory Reaction / Rheumatoid Arthritis1
Not AvailableRecruitingNot AvailableMechanisms, Defense / Outcomes / Pregnancy Related / Takayasu's Disease / Treatment Refusal1
Not AvailableRecruitingNot AvailableRheumatoid Arthritis2
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Healthy Volunteers1
Not AvailableRecruitingOtherAdiposity1
Not AvailableRecruitingSupportive CareCytokine Storm / Novel Coronavirus Infectious Disease (COVID-19) / Viral Pneumonia1
Not AvailableRecruitingSupportive CareNovel Coronavirus Infectious Disease (COVID-19) / Viral Pneumonia1
Not AvailableRecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19)1
Not AvailableTerminatedOtherEnd Stage Renal Disease (ESRD) / End-Stage Renal Disease (ESRD) / Hla-incompatible Kidney Transplant Candidates / Transplantation, Kidney1
Not AvailableTerminatedTreatmentRheumatoid Arthritis, Juvenile / Still's Disease, Juvenile Onset1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous180 mg/1mL
Injection, solution, concentrateIntravenous20 mg/1mL
SolutionIntravenous200 mg
SolutionIntravenous400 mg
SolutionIntravenous80 mg
SolutionSubcutaneous162 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2201781No2010-01-122015-06-07Canada
CA1341152No2000-12-122017-12-12Canada
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Antibody
General Function
Protein homodimerization activity
Specific Function
Part of the receptor for interleukin 6. Binds to IL6 with low affinity, but does not transduce a signal. Signal activation necessitate an association with IL6ST. Activation may lead to the regulati...
Gene Name
IL6R
Uniprot ID
P08887
Uniprot Name
Interleukin-6 receptor subunit alpha
Molecular Weight
51547.015 Da
References
  1. Smolen JS, Maini RN: Interleukin-6: a new therapeutic target. Arthritis Res Ther. 2006;8 Suppl 2:S5. Epub 2006 Jul 28. [PubMed:16899109]
  2. Betts BC, St Angelo ET, Kennedy M, Young JW: Anti-IL6-receptor-alpha (tocilizumab) does not inhibit human monocyte-derived dendritic cell maturation or alloreactive T-cell responses. Blood. 2011 Nov 10;118(19):5340-3. doi: 10.1182/blood-2011-06-363390. Epub 2011 Sep 22. [PubMed:21940820]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Long TJ, Cosgrove PA, Dunn RT 2nd, Stolz DB, Hamadeh H, Afshari C, McBride H, Griffith LG: Modeling Therapeutic Antibody-Small Molecule Drug-Drug Interactions Using a Three-Dimensional Perfusable Human Liver Coculture Platform. Drug Metab Dispos. 2016 Dec;44(12):1940-1948. doi: 10.1124/dmd.116.071456. Epub 2016 Sep 12. [PubMed:27621203]
  2. FDA Approved Drug Products: Actemra Tocilizumab Intravenous or Subcutaneous Injection [Link]

Drug created on March 19, 2008 10:20 / Updated on July 09, 2020 11:59

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