Identification
NameSecukinumab
Accession NumberDB09029
TypeBiotech
GroupsApproved
Description

Secukinumab (Cosentyx) is a human monoclonal antibody designed for the treatment of uveitis, rheumatoid arthritis, ankylosing spondylitis, and psoriasis. Secukinumab is an interleukin-17A (IL-17A) inhibitor marketed by Novartis. IL-17 is a group of proinflammatory cytokines released by cells of the immune system and and exist in higher levels in many immune conditions associated with chronic inflammation. By targeting IL-17A, secukinumab has shown excellent efficacy in psoriasis by normalizing skin histology and was approved by the United States Food and Drug Administration on January 21, 2015 to treat adults with moderate-to-severe plaque psoriasis.

Protein structureDb09029
Related Articles
Protein chemical formulaC6584H10134N1754O2042S44
Protein average weight147940.0 Da
Sequences
> Secukinumab Heavy Chain (CAS 875356-43-7)
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNYWMNWVRQAPGKGLEWVAAINQDGSEKYY
VGSVKGRFTISRDNAKNSLYLQMNSLRVEDTAVYYCVRDYYDILTDYYIHYWYFDLWGRG
TLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTF
PAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCP
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYT
LPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKL
TVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
> Secukinumab Light Chain (CAS 875356-44-8)
EIVLTQSPGTLSLSPGERATLSCRASQSVSSSYLAWYQQKPGQAPRLLIYGASSRATGIP
DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYGSSPCTFGQGTRLEIKRTVAAPSVFIFP
PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL
TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
SynonymsNot Available
External IDs AIN-457 / AIN457 / AIN457A
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CosentyxInjection150 mg/mLSubcutaneousNovartis2015-01-21Not applicableUs
CosentyxSolution150 mgSubcutaneousNovartis2015-04-10Not applicableCanada
CosentyxPowder, for solution150 mgSubcutaneousNovartisNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIIDLG4EML025
CAS number1229022-83-6
Pharmacology
Indication

For the treatment of moderate to severe plaque psoriasis in patients that are candidates for systemic therapy or phototherapy.

Structured Indications
PharmacodynamicsNot Available
Mechanism of action

Secukinumab is a human monoclonal antibody that targets IL-17A cytokine to downregulate inflammation in psoriasis, an autoimmune dermatological disease. The pathophysiology of psoriasis has not been fully established, however it is known that dysregulation of innate and adaptive immune responses plays part in the chronic inflammation associated with the disease. IL-17 represents is a six-membered family (IL-17A to F) of pleiotropic pro-inflammatory cytokines, expression of which is found to be elevated in psoriatic skin. These cytokines act on many different cell types and provide defense against different extracellular pathogens causing fungal or bacterial infections. IL-17 cytokines are produced by many cells involved in immune system defense, such as Th17, mast cells, neutrophils, and dendritic cells - all implicated in promoting inflammation. There is evidence linking IL-17 to pathogenesis of multiple autoimmune diseases including rheumatoid arthritis, spondyloarthritis, psoriasis, Crohn's disease, multiple sclerosis, and even atherosclerosis.

TargetKindPharmacological actionActionsOrganismUniProt ID
Interleukin-17AProteinyes
antagonist
HumanQ16552 details
Related Articles
Absorption

Bioavailability after subcutaneous administration was 55-77%.

Volume of distribution

Volume of distribution (Vd) in interstitial fluid of skin (+/- psoriasis) was 27-40% of that in serum after single subcutaneous dose of 300 mg. Vd increased at higher body weights.

Protein bindingNot Available
Metabolism

Mainly intracellular breakdown.

Route of eliminationNot Available
Half life

22-31 days

Clearance

Serum clearance was increased with higher body weights.

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Secukinumab.Approved
FingolimodSecukinumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Secukinumab is combined with G17DT.Investigational
INGN 201The risk or severity of adverse effects can be increased when Secukinumab is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Secukinumab is combined with INGN 225.Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Secukinumab is combined with Leflunomide.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Secukinumab is combined with Natalizumab.Approved, Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Secukinumab.Approved, Investigational
RindopepimutThe risk or severity of adverse effects can be increased when Secukinumab is combined with CDX-110.Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Secukinumab.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Secukinumab.Approved
SRP 299The risk or severity of adverse effects can be increased when Secukinumab is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab.Approved, Investigational
TofacitinibSecukinumab may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Secukinumab.Approved, Investigational
Food InteractionsNo interactions found.
References
Synthesis ReferenceNot Available
General References
  1. McInnes IB, Sieper J, Braun J, Emery P, van der Heijde D, Isaacs JD, Dahmen G, Wollenhaupt J, Schulze-Koops H, Kogan J, Ma S, Schumacher MM, Bertolino AP, Hueber W, Tak PP: Efficacy and safety of secukinumab, a fully human anti-interleukin-17A monoclonal antibody, in patients with moderate-to-severe psoriatic arthritis: a 24-week, randomised, double-blind, placebo-controlled, phase II proof-of-concept trial. Ann Rheum Dis. 2014 Feb;73(2):349-56. doi: 10.1136/annrheumdis-2012-202646. Epub 2013 Jan 29. [PubMed:23361084 ]
  2. Jaleel T, Elmets C, Weinkle A, Kassira S, Elewski B: Secukinumab (AIN-457) for the treatment of Psoriasis. Expert Rev Clin Pharmacol. 2016 Feb;9(2):187-202. doi: 10.1586/17512433.2016.1129894. [PubMed:26647300 ]
  3. Wong IT, Shojania K, Dutz J, Tsao NW: Clinical and economic review of secukinumab for moderate-to-severe plaque psoriasis. Expert Rev Pharmacoecon Outcomes Res. 2016 Apr;16(2):153-66. doi: 10.1586/14737167.2016.1133301. Epub 2016 Feb 2. [PubMed:26681527 ]
  4. Roman M, Madkan VK, Chiu MW: Profile of secukinumab in the treatment of psoriasis: current perspectives. Ther Clin Risk Manag. 2015 Dec 2;11:1767-77. doi: 10.2147/TCRM.S79053. eCollection 2015. [PubMed:26664127 ]
External Links
ATC CodesL04AC10 — Secukinumab
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentHidradenitis Suppurativa (HS)1
1Active Not RecruitingBasic ScienceModerate to Severe Plaque Psoriasis1
1CompletedBasic ScienceHealthy Volunteers / Psoriasis1
1, 2CompletedBasic ScienceHealthy Volunteers1
1, 2CompletedBasic SciencePlaque Psoriasis1
1, 2CompletedBasic ScienceRheumatoid Arthritis1
1, 2CompletedTreatmentChronic Plaque-type Psoriasis1
1, 2Not Yet RecruitingTreatmentPapulopustular Rosacea1
1, 2RecruitingTreatmentPyoderma Gangrenosum1
2CompletedNot AvailableAnkylosing Spondylitis (AS)1
2CompletedTreatmentActive Uveitis That is Not From an Infection1
2CompletedTreatmentAnkylosing Spondylitis (AS)1
2CompletedTreatmentChronic Plaque Psoriasis2
2CompletedTreatmentChronic Plaque-type Psoriasis2
2CompletedTreatmentDisseminated Sclerosis1
2CompletedTreatmentEye Dryness1
2CompletedTreatmentPlaque-Type Psoriasis1
2CompletedTreatmentPsoriasis, Plaque-type Psoriasis1
2CompletedTreatmentPsoriatic Arthritis2
2CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS) / RRMS1
2CompletedTreatmentRheumatoid Arthritis3
2RecruitingNot AvailablePsoriasis / Psoriatic Arthritis1
2RecruitingBasic SciencePsoriatic Arthritis1
2RecruitingTreatmentAutosomal Recessive Congenital Ichthyosis / Congenital Ichthyosiform Erythroderma / Epidermolytic Ichthyosis / Ichthyosis / Lamellar Ichthyosis / Netherton Syndrome1
2RecruitingTreatmentPsoriasis1
2RecruitingTreatmentModerate, refractory Atopic dermatitis1
2TerminatedTreatmentAlopecia Areata (AA)1
2TerminatedTreatmentAsthma Bronchial1
2TerminatedTreatmentCrohn's Disease (CD)1
2TerminatedTreatmentCrohn's Disease (CD) / Inflammatory Bowel Diseases (IBD)1
2TerminatedTreatmentDiabetes, Diabetes Mellitus Type 11
2TerminatedTreatmentDisseminated Sclerosis1
2TerminatedTreatmentInflammatory Diseases / Polymyalgia Rheumatica1
3Active Not RecruitingTreatmentAnklyosing Spondylitis1
3Active Not RecruitingTreatmentAnkylosing Spondylitis (AS)4
3Active Not RecruitingTreatmentModerate to Severe Chronic Plaque-Type Psoriasis1
3Active Not RecruitingTreatmentModerate to Severe Nail Psoriasis1
3Active Not RecruitingTreatmentModerate to Severe Plaque-type Psoriasis1
3Active Not RecruitingTreatmentPlaque Psoriasis1
3Active Not RecruitingTreatmentPlaque Type Psorisis1
3Active Not RecruitingTreatmentPsoriatic Arthritis4
3CompletedTreatmentAnkylosing Spondylitis (AS)1
3CompletedTreatmentBehcet's Syndrome1
3CompletedTreatmentChronic Plaque Psoriasis1
3CompletedTreatmentChronic Plaque Type Psoriasis1
3CompletedTreatmentChronic Scalp Psoriasis1
3CompletedTreatmentModerate to Severe Palmoplantar Psoriasis1
3CompletedTreatmentModerate to Severe Plaque-type Psoriasis4
3CompletedTreatmentPlaque-Type Psoriasis2
3CompletedTreatmentPsoriasis6
3CompletedTreatmentPsoriatic Arthritis1
3CompletedTreatmentRheumatoid Arthritis3
3Not Yet RecruitingTreatmentEnthesitis-related Arthritis / Juvenile psoriatic arthritis1
3Not Yet RecruitingTreatmentEnthesitis / Psoriatic Arthritis / Spondyloarthritis, Axial1
3Not Yet RecruitingTreatmentPsoriatic Arthritis1
3RecruitingTreatmentAllergic Contact Dermatitits1
3RecruitingTreatmentAnkylosing Spondyloarthritis1
3RecruitingTreatmentAxial Psoratic Arthritis1
3RecruitingTreatmentChronic Severe Plaque-type Psoriasis1
3RecruitingTreatmentNon-radiographic Spondyloarthritis1
3RecruitingTreatmentPlaque Psoriasis2
3RecruitingTreatmentPsoriasis1
3RecruitingTreatmentPsoriatic Arthritis2
3TerminatedTreatmentNon-Infectious Uveitis2
3TerminatedTreatmentRheumatoid Arthritis1
3TerminatedTreatmentUveitis3
3WithdrawnTreatmentUveitis1
4CompletedTreatmentPlaque Psoriasis1
4RecruitingBasic SciencePsoriasis1
4RecruitingTreatmentAnkylosing Spondylitis (AS)1
4RecruitingTreatmentChronic Plaque Psoriasis1
4RecruitingTreatmentModerate to Severe Plaque Psoriasis1
4RecruitingTreatmentPlaque Psoriasis2
4RecruitingTreatmentPsoriatic Arthritis1
Not AvailableRecruitingNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableRecruitingNot AvailablePsoriasis Vulgaris1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
InjectionSubcutaneous150 mg/mL
Powder, for solutionSubcutaneous150 mg
SolutionSubcutaneous150 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US20130202610 No2010-10-082020-10-08Us
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
antagonist
General Function:
Cytokine receptor binding
Specific Function:
Induces stromal cells to produce proinflammatory and hematopoietic cytokines. Enhances the surface expression of ICAM1/intracellular adhesion molecule 1 in fibroblasts.
Gene Name:
IL17A
Uniprot ID:
Q16552
Molecular Weight:
17503.92 Da
References
  1. Ohtsuki M, Morita A, Abe M, Takahashi H, Seko N, Karpov A, Shima T, Papavassilis C, Nakagawa H: Secukinumab efficacy and safety in Japanese patients with moderate-to-severe plaque psoriasis: subanalysis from ERASURE, a randomized, placebo-controlled, phase 3 study. J Dermatol. 2014 Dec;41(12):1039-46. doi: 10.1111/1346-8138.12668. Epub 2014 Oct 30. [PubMed:25354738 ]
Drug created on January 19, 2015 16:12 / Updated on August 17, 2016 12:24