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Identification
NameInfliximab
Accession NumberDB00065  (BTD00004, BIOD00004)
TypeBiotech
GroupsApproved
DescriptionTumor necrosis factor (TNF-alpha) binding antibody (chimeric IgG1). It is composed of human constant and murine variable regions. Infliximab is produced by a recombinant cell line cultured by continuous perfusion
Protein structureDb00065
Related Articles
Protein chemical formulaC6428H9912N1694O1987S46
Protein average weight144190.3 Da
SequencesNot Available
Synonyms
Ig gamma-1 chain C region
External Identifiers
  • ABP 710
  • BOW015
  • CT-P-13
  • CT-P13
  • TA-650
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FlixabiInjection, powder, for solution100 mgIntravenousSamsung Bioepis Uk Limited (Sbuk)2016-05-26Not applicableEu
FlixabiInjection, powder, for solution100 mgIntravenousSamsung Bioepis Uk Limited (Sbuk)2016-05-26Not applicableEu
FlixabiInjection, powder, for solution100 mgIntravenousSamsung Bioepis Uk Limited (Sbuk)2016-05-26Not applicableEu
FlixabiInjection, powder, for solution100 mgIntravenousSamsung Bioepis Uk Limited (Sbuk)2016-05-26Not applicableEu
FlixabiInjection, powder, for solution100 mgIntravenousSamsung Bioepis Uk Limited (Sbuk)2016-05-26Not applicableEu
InflectraInjection, powder, for solution100 mgIntravenousHospira Uk Limited2013-09-10Not applicableEu
InflectraInjection, powder, lyophilized, for solution100 mg/10mLIntravenousPfizer Laboratories Div Pfizer Inc2016-11-21Not applicableUs
InflectraInjection, powder, for solution100 mgIntravenousHospira Uk Limited2013-09-10Not applicableEu
InflectraInjection, powder, for solution100 mgIntravenousHospira Uk Limited2013-09-10Not applicableEu
InflectraPowder, for solution100 mgIntravenousCelltrion Healthcare Co Ltd2014-09-04Not applicableCanada
InflectraInjection, powder, for solution100 mgIntravenousHospira Uk Limited2013-09-10Not applicableEu
InflectraInjection, powder, for solution100 mgIntravenousHospira Uk Limited2013-09-10Not applicableEu
RemicadeInjection, powder, lyophilized, for solution100 mg/10mLIntravenousJanssen Biotech, Inc.1998-08-24Not applicableUs
RemicadeInjection, powder, for solution100 mgIntravenousJanssen Biologics B.V.  1999-08-13Not applicableEu
RemicadePowder, for solution100 mgIntravenousJanssen Inc2001-06-14Not applicableCanada
RemicadeInjection, powder, for solution100 mgIntravenousJanssen Biologics B.V.  1999-08-13Not applicableEu
RemicadeInjection, powder, for solution100 mgIntravenousJanssen Biologics B.V.  1999-08-13Not applicableEu
RemicadeInjection, powder, for solution100 mgIntravenousJanssen Biologics B.V.  1999-08-13Not applicableEu
RemicadeInjection, powder, for solution100 mgIntravenousJanssen Biologics B.V.  1999-08-13Not applicableEu
RemsimaPowder, for solution100 mgIntravenousCelltrion Healthcare Co Ltd2014-09-18Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIB72HH48FLU
CAS number170277-31-3
Pharmacology
IndicationTo manage the signs and symptoms, as well as to induce and maintain clinical remission in adults with moderate to severe active Crohn's disease or ulcerative colitis. Also used to manage signs and symptoms of rheumatoid arthritis (in conjunction with methotrexate), ankylosing spondylitis, psoriatic arthritis, and juvenile arthritis.
Structured Indications
PharmacodynamicsInfliximab is a chimeric human-murine anti-human tumor necrosis factor (TNF) monoclonal antibody. It binds to tumor necrosis factor alpha (TNFa) and inhibits binding of TNFa with its receptors. This reduces production of pro-inflammatory cytokines such as interleukins (IL) 1 and 6. This also limits leukocyte migration and expression of adhesion molecules by endothelial cells and leukocytes. Infliximab also limits the activation of neutrophil and eosinophil functional activity, reduces production of tissue degrading enzymes produced by synoviocytes and/or chondrocytes. Infliximab decreases synovitis and joint erosions in collagen-induced arthritis and allows eroded joints to heal.
Mechanism of actionInfliximab neutralizes the biological activity of TNFa by binding with high affinity to the soluble and transmembrane forms of TNFa and inhibits binding of TNFa with its receptors. Infliximab does not neutralize TNFb (lymphotoxin a), a related cytokine that utilizes the same receptors as TNFa. TNFa activation normally induces the release of proinflammatory cytokines, the enhancement of leukocyte migration and activation of neutrophils among others. Neutralization of the biological activity of TNFa leads to an overall reduction in inflammation.
TargetKindPharmacological actionActionsOrganismUniProt ID
Tumor necrosis factorProteinyes
inhibitor
HumanP01375 details
Related Articles
AbsorptionOnset of action occurs in about 2 weeks in Crohn's disease.
Volume of distribution

3-6 L

Protein bindingNot Available
Metabolism

Most likely removed by opsonization via the reticuloendothelial system when bound to T lymphocytes, or by human antimurine antibody production. Not metabolized by the CYP enzymes.

Route of eliminationNot Available
Half life9.5 days (7-12 days) in patients with Crohn's disease, plaque psoriasis and rheumatoid arthritis
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Low affinity immunoglobulin gamma Fc region receptor III-A
Gene symbol: FCGR3A
UniProt: P08637
rs1801274 Not AvailableCC Allele (homozygous)Better ACR20 response18930989
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbataceptThe risk or severity of adverse effects can be increased when Infliximab is combined with Abatacept.Approved
AdalimumabAdalimumab may increase the immunosuppressive activities of Infliximab.Approved
ALT-110The risk or severity of adverse effects can be increased when Infliximab is combined with ALT-110.Investigational
AnakinraThe risk or severity of adverse effects can be increased when Infliximab is combined with Anakinra.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Infliximab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Infliximab is combined with Belimumab.Approved
CanakinumabThe risk or severity of adverse effects can be increased when Infliximab is combined with Canakinumab.Approved, Investigational
CDX-110The risk or severity of adverse effects can be increased when Infliximab is combined with CDX-110.Investigational
Certolizumab pegolInfliximab may increase the immunosuppressive activities of Certolizumab pegol.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Infliximab.Approved
EtanerceptEtanercept may increase the immunosuppressive activities of Infliximab.Approved, Investigational
FingolimodInfliximab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Infliximab is combined with G17DT.Investigational
GI-5005The risk or severity of adverse effects can be increased when Infliximab is combined with GI-5005.Investigational
GolimumabGolimumab may increase the immunosuppressive activities of Infliximab.Approved
INGN 201The risk or severity of adverse effects can be increased when Infliximab is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Infliximab is combined with INGN 225.Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Infliximab is combined with Leflunomide.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Infliximab is combined with Natalizumab.Approved, Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Infliximab.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Infliximab is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Infliximab.Approved
RilonaceptThe risk or severity of adverse effects can be increased when Infliximab is combined with Rilonacept.Approved
RituximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Rituximab.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Infliximab.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Infliximab.Approved
SRP 299The risk or severity of adverse effects can be increased when Infliximab is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Infliximab.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Infliximab is combined with TG4010.Investigational
TocilizumabTocilizumab may increase the immunosuppressive activities of Infliximab.Approved
TofacitinibThe risk or severity of adverse effects can be increased when Infliximab is combined with Tofacitinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Infliximab.Approved, Investigational
UstekinumabUstekinumab may increase the immunosuppressive activities of Infliximab.Approved, Investigational
VedolizumabThe risk or severity of adverse effects can be increased when Infliximab is combined with Vedolizumab.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Knight DM, Trinh H, Le J, Siegel S, Shealy D, McDonough M, Scallon B, Moore MA, Vilcek J, Daddona P, et al.: Construction and initial characterization of a mouse-human chimeric anti-TNF antibody. Mol Immunol. 1993 Nov;30(16):1443-53. [PubMed:8232330 ]
  2. Dubinsky MC, Fleshner PP: Treatment of Crohn's Disease of Inflammatory, Stenotic, and Fistulizing Phenotypes. Curr Treat Options Gastroenterol. 2003 Jun;6(3):183-200. [PubMed:12744819 ]
  3. Present DH, Rutgeerts P, Targan S, Hanauer SB, Mayer L, van Hogezand RA, Podolsky DK, Sands BE, Braakman T, DeWoody KL, Schaible TF, van Deventer SJ: Infliximab for the treatment of fistulas in patients with Crohn's disease. N Engl J Med. 1999 May 6;340(18):1398-405. [PubMed:10228190 ]
  4. Sands BE, Anderson FH, Bernstein CN, Chey WY, Feagan BG, Fedorak RN, Kamm MA, Korzenik JR, Lashner BA, Onken JE, Rachmilewitz D, Rutgeerts P, Wild G, Wolf DC, Marsters PA, Travers SB, Blank MA, van Deventer SJ: Infliximab maintenance therapy for fistulizing Crohn's disease. N Engl J Med. 2004 Feb 26;350(9):876-85. [PubMed:14985485 ]
  5. Hanauer SB: Crohn's disease: step up or top down therapy. Best Pract Res Clin Gastroenterol. 2003 Feb;17(1):131-7. [PubMed:12617888 ]
  6. Link [Link]
  7. Link [Link]
External Links
ATC CodesL04AB02
AHFS Codes
  • 92:00.00
PDB Entries
FDA labelDownload (1.21 MB)
MSDSNot Available
Pharmacoeconomics
Manufacturers
  • J&J and Mitsubisi Tanabe
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous100 mg
Injection, powder, lyophilized, for solutionIntravenous100 mg/10mL
Powder, for solutionIntravenous100 mg
Prices
Unit descriptionCostUnit
Remicade 100 mg Solution Vial821.02USD vial
Remicade 100 mg vial789.44USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2106299 No2001-02-062012-03-18Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.441Not Available
isoelectric point8.25Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Tumor necrosis factor receptor binding
Specific Function:
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs ...
Gene Name:
TNF
Uniprot ID:
P01375
Molecular Weight:
25644.15 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Mimura T: [Selection of one of the TNF blockers; infliximab and etanercept]. Nihon Rinsho. 2007 Jul;65(7):1282-6. [PubMed:17642244 ]
  3. Braun J, Baraliakos X, Listing J, Sieper J: Decreased incidence of anterior uveitis in patients with ankylosing spondylitis treated with the anti-tumor necrosis factor agents infliximab and etanercept. Arthritis Rheum. 2005 Aug;52(8):2447-51. [PubMed:16052578 ]
  4. Danese S, Sans M, Scaldaferri F, Sgambato A, Rutella S, Cittadini A, Pique JM, Panes J, Katz JA, Gasbarrini A, Fiocchi C: TNF-alpha blockade down-regulates the CD40/CD40L pathway in the mucosal microcirculation: a novel anti-inflammatory mechanism of infliximab in Crohn's disease. J Immunol. 2006 Feb 15;176(4):2617-24. [PubMed:16456024 ]
  5. Magro F, Pereira P, Carneiro F, Veloso FT: Reactive hepatitis in a patient with Crohn's disease successfully treated with infliximab: does tumor necrosis factor alpha play a role in reactive hepatitis? Inflamm Bowel Dis. 2005 Jan;11(1):88-90. [PubMed:15674127 ]
  6. Mori S, Imamura F, Kiyofuji C, Ito K, Koga Y, Honda I, Sugimoto M: Pneumocystis jiroveci pneumonia in a patient with rheumatoid arthritis as a complication of treatment with infliximab, anti-tumor necrosis factor alpha neutralizing antibody. Mod Rheumatol. 2006;16(1):58-62. [PubMed:16622728 ]
  7. Maini RN, Feldmann M: How does infliximab work in rheumatoid arthritis? Arthritis Res. 2002;4 Suppl 2:S22-8. Epub 2002 Mar 27. [PubMed:12110154 ]
  8. Sapienza MS, Cohen S, Dimarino AJ: Treatment of pyoderma gangrenosum with infliximab in Crohn's disease. Dig Dis Sci. 2004 Sep;49(9):1454-7. [PubMed:15481318 ]
  9. Tobin AM, Kirby B: TNF alpha inhibitors in the treatment of psoriasis and psoriatic arthritis. BioDrugs. 2005;19(1):47-57. [PubMed:15691217 ]
  10. Shen C, Assche GV, Colpaert S, Maerten P, Geboes K, Rutgeerts P, Ceuppens JL: Adalimumab induces apoptosis of human monocytes: a comparative study with infliximab and etanercept. Aliment Pharmacol Ther. 2005 Feb 1;21(3):251-8. [PubMed:15691299 ]
  11. Popa C, Netea MG, Barrera P, Radstake TR, van Riel PL, Kullberg BJ, Van der Meer JW: Cytokine production of stimulated whole blood cultures in rheumatoid arthritis patients receiving short-term infliximab therapy. Cytokine. 2005 Apr 21;30(2):72-7. [PubMed:15804598 ]
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Drug created on June 13, 2005 07:24 / Updated on December 02, 2016 09:13