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Identification
NameUstekinumab
Accession NumberDB05679
TypeBiotech
GroupsApproved, Investigational
DescriptionUstekinumab, is a human immunosuppressive drug developed by the biotechnology company Centocor. It is a laboratory-manufactured, monoclonal antibody directed against interleukins IL-12 and IL-23. Since 2009, ustekinumab has been approved in US, Canada, and Europe for the treatment of plaque psoriasis and psoriatic arthritis. In September 2016, Janssen announced that the FDA approved the medication for the treatment of moderate-severe Crohn's disease.
Protein structureDb05679
Related Articles
Protein chemical formulaAnti-(human interleukin 12 p40 subunit) (human monoclonal CNTO 1275 γ1-chain)-immunoglobulin G1 disulfide with human monoclonal CNTO 1275 κ-chain dimer
Protein average weightNot Available
SequencesNot Available
Synonyms
Stelera
External Identifiers
  • CNTO 1275
  • CNTO-1275
  • CNTO1275
  • L04AC05
  • TT 20
  • TT-20
  • TT20
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
StelaraInjection, solution90 mg/mLSubcutaneousJanssen Biotech, Inc.2009-09-25Not applicableUs
StelaraSolution45 mgSubcutaneousJanssen Inc2009-01-05Not applicableCanada
StelaraInjection, solution45 mgSubcutaneousJanssen Cilag International Nv2009-01-16Not applicableEu
StelaraSolution130 mg/26mLIntravenousJanssen Biotech, Inc.2016-09-23Not applicableUs
StelaraSolution90 mgSubcutaneousJanssen Inc2013-01-07Not applicableCanada
StelaraInjection, solution90 mgSubcutaneousJanssen Cilag International Nv2009-01-16Not applicableEu
StelaraInjection, solution45 mgSubcutaneousJanssen Cilag International Nv2009-01-16Not applicableEu
StelaraInjection, solution45 mg/.5mLSubcutaneousJanssen Biotech, Inc.2009-09-25Not applicableUs
StelaraInjection, solution90 mgSubcutaneousJanssen Cilag International Nv2009-01-16Not applicableEu
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
UNIIFU77B4U5Z0
CAS number815610-63-0
Pharmacology
IndicationUstekinumab is indicated for management of moderate to severe plaque psoriasis in adults who are candidates for systemic therapy or phototherapy; or is used alone or in conjunction with methotrexate for the management of active psoriatic arthritis in adults. The FDA approved the use of ustekinumab in September 2016 for the treatment of moderate to severe Crohn's disease. The use of ustekinumab may improve short term clinical response but not clinical remission in moderate to severe Crohn's disease.
Structured Indications
PharmacodynamicsNot Available
Mechanism of actionUstekinumab is a human IgG1-kappa monoclonal antibody designed to interfere with the triggering of the body's inflammatory response through the suppression of certain cytokines. Specifically, ustekinumab blocks interleukin IL-12 and IL-23 by binding with high affinity and specificity to the p40 subunit of IL-12 and IL-23, therefore disrupting the proinflammatory pathway that contributes to several chronic diseases. In a more minor role, ustekinumab also interferes with the expression of monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-alpha (TNF-α), interferon-inducible protein-10 (IP-10), and interleukin IL-8.
TargetKindPharmacological actionActionsOrganismUniProt ID
Interleukin-12 subunit betaProteinyes
antibody
HumanP29460 details
Interleukin-23Protein groupyesNot AvailableHumannot applicabledetails
Related Articles
AbsorptionFollowing a subcutaneous administration of a single 45 or 90mg dose (in patients with psoriasis), peak serum concentrations are achieved in a median of 13.5 or 7 days, respectively.
Volume of distribution

Plaque psoriasis and psoriatic arthritis dosing:
45mg: ~0.161L/kg
90mg: ~0.179L/kg

Protein bindingNot Available
Metabolism

Expected to be degraded into small peptides and amino acids.

Route of eliminationNot Available
Half lifeMean half-life: 14.9–45.6 days following IV and sub-Q administration in patients with psoriasis.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
ALT-110The risk or severity of adverse effects can be increased when Ustekinumab is combined with ALT-110.Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Ustekinumab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Belimumab.Approved
CDX-110The risk or severity of adverse effects can be increased when Ustekinumab is combined with CDX-110.Investigational
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Ustekinumab.Approved
FingolimodUstekinumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Ustekinumab is combined with G17DT.Investigational
GI-5005The risk or severity of adverse effects can be increased when Ustekinumab is combined with GI-5005.Investigational
InfliximabUstekinumab may increase the immunosuppressive activities of Infliximab.Approved
INGN 201The risk or severity of adverse effects can be increased when Ustekinumab is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Ustekinumab is combined with INGN 225.Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Leflunomide.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Natalizumab.Approved, Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ustekinumab.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Ustekinumab.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Ustekinumab.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Ustekinumab.Approved
SRP 299The risk or severity of adverse effects can be increased when Ustekinumab is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ustekinumab.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Ustekinumab is combined with TG4010.Investigational
TofacitinibUstekinumab may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Ustekinumab.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Wittig BM: Drug evaluation: CNTO-1275, a mAb against IL-12/IL-23p40 for the potential treatment of inflammatory diseases. Curr Opin Investig Drugs. 2007 Nov;8(11):947-54. [PubMed:17979029 ]
  2. Boker A, Kimball AB, Rolz-Cruz G: Biologicals in the treatment of psoriasis. Curr Opin Investig Drugs. 2007 Nov;8(11):939-46. [PubMed:17979028 ]
  3. Reddy M, Davis C, Wong J, Marsters P, Pendley C, Prabhakar U: Modulation of CLA, IL-12R, CD40L, and IL-2Ralpha expression and inhibition of IL-12- and IL-23-induced cytokine secretion by CNTO 1275. Cell Immunol. 2007 May;247(1):1-11. Epub 2007 Aug 29. [PubMed:17761156 ]
  4. Khanna R, Chande N, Vermeire S, Sandborn WJ, Parker CE, Feagan BG: The Next Wave of Biological Agents for the Treatment of IBD: Evidence from Cochrane Reviews. Inflamm Bowel Dis. 2016 Jul;22(7):1737-43. doi: 10.1097/MIB.0000000000000808. [PubMed:27306074 ]
  5. Engel T, Kopylov U: Ustekinumab in Crohn's disease: evidence to date and place in therapy. Ther Adv Chronic Dis. 2016 Jul;7(4):208-14. doi: 10.1177/2040622316653306. Epub 2016 Jul 6. [PubMed:27433311 ]
External Links
ATC CodesL04AC05
AHFS Codes
  • 84:92
PDB EntriesNot Available
FDA labelDownload (7.26 MB)
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous45 mg
Injection, solutionSubcutaneous45 mg/.5mL
Injection, solutionSubcutaneous90 mg
Injection, solutionSubcutaneous90 mg/mL
SolutionIntravenous130 mg/26mL
SolutionSubcutaneous45 mg
SolutionSubcutaneous90 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot 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
antibody
General Function:
Protein heterodimerization activity
Specific Function:
Cytokine that can act as a growth factor for activated T and NK cells, enhance the lytic activity of NK/lymphokine-activated killer cells, and stimulate the production of IFN-gamma by resting PBMC.Associates with IL23A to form the IL-23 interleukin, a heterodimeric cytokine which functions in innate and adaptive immunity. IL-23 may constitute with IL-17 an acute response to infection in periphe...
Gene Name:
IL12B
Uniprot ID:
P29460
Molecular Weight:
37168.645 Da
References
  1. Reddy M, Davis C, Wong J, Marsters P, Pendley C, Prabhakar U: Modulation of CLA, IL-12R, CD40L, and IL-2Ralpha expression and inhibition of IL-12- and IL-23-induced cytokine secretion by CNTO 1275. Cell Immunol. 2007 May;247(1):1-11. Epub 2007 Aug 29. [PubMed:17761156 ]
  2. Wittig BM: Drug evaluation: CNTO-1275, a mAb against IL-12/IL-23p40 for the potential treatment of inflammatory diseases. Curr Opin Investig Drugs. 2007 Nov;8(11):947-54. [PubMed:17979029 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
General Function:
Protein heterodimerization activity
Specific Function:
Cytokine that can act as a growth factor for activated T and NK cells, enhance the lytic activity of NK/lymphokine-activated killer cells, and stimulate the production of IFN-gamma by resting PBMC.Associates with IL23A to form the IL-23 interleukin, a heterodimeric cytokine which functions in innate and adaptive immunity. IL-23 may constitute with IL-17 an acute response to infection in peripheral tissues. IL-23 binds to a heterodimeric receptor complex composed of IL12RB1 and IL23R, activates the Jak-Stat signaling cascade, stimulates memory rather than naive T-cells and promotes production of proinflammatory cytokines. IL-23 induces autoimmune inflammation and thus may be responsible for autoimmune inflammatory diseases and may be important for tumorigenesis.
Components:
NameUniProt IDDetails
Interleukin-12 subunit betaP29460 Details
Interleukin-23 subunit alphaQ9NPF7 Details
References
  1. Engel T, Kopylov U: Ustekinumab in Crohn's disease: evidence to date and place in therapy. Ther Adv Chronic Dis. 2016 Jul;7(4):208-14. doi: 10.1177/2040622316653306. Epub 2016 Jul 6. [PubMed:27433311 ]
  2. Khanna R, Chande N, Vermeire S, Sandborn WJ, Parker CE, Feagan BG: The Next Wave of Biological Agents for the Treatment of IBD: Evidence from Cochrane Reviews. Inflamm Bowel Dis. 2016 Jul;22(7):1737-43. doi: 10.1097/MIB.0000000000000808. [PubMed:27306074 ]
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Drug created on November 18, 2007 11:26 / Updated on October 05, 2016 14:17